https://www.dolcera.com/wiki/api.php?action=feedcontributions&feedformat=atom&user=67.180.226.207 2026-04-27T02:23:38Z User contributions MediaWiki 1.24wmf12 https://www.dolcera.com/wiki/index.php?title=Quality_of_Service_on_CDMA_platforms&diff=1987 2006-07-10T16:53:44Z

<p>67.180.226.207: /* IP MAPs of Patent EP1385290 and EP1156616 */</p> <hr /> <div>== Cellular Communication ==<br /> A cellular mobile communications system uses a large number of low-power wireless transmitters to create cells — the basic geographic service area of a wireless communications system. Variable power levels allow cells to be sized according to the subscriber density and demand within a particular region. As mobile users travel from cell to cell, their conversations are handed off between cells to maintain seamless service. Channels (frequencies) used in one cell can be reused in another cell some distance away. Cells can be added to accommodate growth, creating new cells in unserved areas or overlaying cells in existing areas. [http://www.IEC.org Source]<br /> <br /> There are three main entities in cellular communication<br /> * Mobile Station (MS): A mobile station consists of 2 entities - equipment and SIM card<br /> * Base Transceiver station(BTS): A base transceiver station consists of 2 entities - a base transceiver (transmitter and receiver) station and a base station controller. The BTS is the antenna tower site.<br /> * Main Switching centre(MSC): The main switching centre is the heart of the network - the central switching office which controls all the base stations and provides connection with landline phones. It performs three main tasks. It:<br /> # connects calls from sender to receiver,<br /> # collects details of the calls made and received, and<br /> # supervises operation of the rest of the network components.<br /> <br /> == Cellular System Architecture ==<br /> Cellular systems are increasing in demand as more users are added to their systems. The amount of frequency spectrum available for mobile cellular use was limited, and efficient use of the required frequencies was needed for mobile cellular coverage. In modern cellular telephony, rural and urban regions are divided into areas according to specific provisioning guidelines. Provisioning for each region is planned according to an engineering plan that includes cells, clusters, frequency reuse, and handovers.<br /> <br /> ==== Cells ==== <br /> A cell is the basic geographic unit of a cellular system. Cells are base stations transmitting over small geographic areas that are represented as hexagons.<br /> <br /> ==== Clusters ==== <br /> A cluster is a group of cells. No channels are reused within a cluster. Normally a cluster has seven cells in it as shown below.<br /> <br /> ==== Frequency Reuse ====<br /> The number of radio channel frequencies is limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> ==== Cell Splitting ==== <br /> As a service area becomes full of users, this approach is used to split a single area into smaller ones. In this way, urban centers can be split into as many areas as necessary to provide acceptable service levels in heavy-traffic regions, while larger, less expensive cells can be used to cover remote rural regions.<br /> <br /> ==== Handoff ====<br /> <br /> The final obstacle in the development of the cellular network involved the problem created when a mobile subscriber traveled from one cell to another during a call. As adjacent areas do not use the same radio channels, a call must either be dropped or transferred from one radio channel to another when a user crosses the line between adjacent cells. Because dropping the call is unacceptable, the process of handoff was created. Handoff occurs when the mobile telephone network automatically transfers a call from radio channel to radio channel as a mobile crosses adjacent cells.<br /> <br /> ==Evolution of Cellular Systems==<br /> [[Image:cdma1.jpg|500 px|center]]<br /> == Multiple Access Methods ==<br /> There are predominantly three types of multiple access methods.<br /> === Frequency Division Multiple Access ===<br /> In this system, each user is allotted a different set of frequencies to operate upon. The uplink(mobile to base station) frequency is different from downlink frequency(base station to mobile).<br /> [[Image:cdma6.jpg|thumb|700px|center|[http://www.ai.u-hyogo.ac.jp/~thai-proj/presen/20051222-Ishikawa.ppt FDMA]]]<br /> === Time Division Multiple Access ===<br /> In this system, each user is allocated a different time slot. Forward link frequency and reverse link frequency is the same. A synchronous switch is responsible for the time switching.<br /> [[Image:cdma10.jpg|thumb|600px|center|TDMA]]<br /> <br /> === Code Division Multiple Access ===<br /> There is no restriction on time and frequency in this scheme. All the users can transmit at all times and at all frequencies. Because users are isolated by code, they can share the same carrier frequency, eliminating the frequency reuse problem encountered in other technologies.<br /> [[Image:cdma11.jpg|thumb|600 px|centre|CDMA]]&lt;br&gt;<br /> <br /> A comparative study between the above three access technologies with respect to time and frequency is as shown below.<br /> [[Image:cdma12.jpg|thumb|600 px|centre|Comparison of cellular access schemes]]<br /> <br /> == Code Division Multiple Access ==<br /> The CDMA technology can be implemented by spreading the spectrum which can be done in the following two ways<br /> * Direct Sequence Spread Sprectrum - DSSS CDMA<br /> * Frequency Hopping - FH CDMA<br /> === Direct Sequence Spread Sprectrum - DSSS CDMA === <br /> In this method, the direct sequence(input data) which is spread over a limited bandwidth is multiplied with a code or spreading sequence (a pseudorandom sequence also known as PN sequence) which will spread the input data over the entire bandwidth of the communication channel. The power density is also reduced and is spread over the frequency spectrum and hence is known as spread spectrum method. The modulation part of DSSS is as shown below.<br /> [[Image:cdma13.jpg|thumb|600px|center|CDMA Modulation]]<br /> The modulated signal is transmitted over the channel and all users can receive it but only the user which knows the correct code can decode the message. This is depicted in the figure below.<br /> [[Image:cdma14.jpg|thumb|600px|center|CDMA Demodulation]]<br /> * CDMA's spread spectrum technique overlaps every transmission on the same carrier frequency by assigning a unique code to each conversation.<br /> * The signal is spread at two levels first using a Walsh Code and then using a PN Code. The number of bits in either of the two codes is known as the &quot;chip rate,&quot; and each bit in the spreading signal is called a &quot;chip&quot;. One bit from each conversation (baseband signal)is multiplied with the walsh code and then the PN code by the spreading techniques, giving the receiving side an enormous amount of data it can average just to determine the value of one bit.<br /> * Base station is the one that assigns spreading code to each call when a mobile requests for a call (unique Walsh code for each conversation and a same PN code for each call in a cell sector). In the analysis henceforth we discuss the dynamic allocation of these spread codes in accordance with the required QoS.<br /> <br /> === Frequency Reuse === <br /> The number of radio channel frequencies is limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> === Soft Handoff === <br /> Handoff means switching a cellular phone transmission from one cell to another as a mobile user moves into a new cellular area. It is so called because the radio link with the previous sector(s) is not broken before a link is established with a new sector; this type of handoff is described as &quot;make before break&quot;. In CDMA, due to this soft handoff, there is no interruption of call even at the border of a cell site which means more number of customers can be accommodated, automatically increasing the capacity of the cell site.<br /> <br /> === Multipath Fading === <br /> In a mobile environment, a mobile station will receive one direct signal from the base station and multiple signals which are reflected from obstructions like buildings and towers. Each signal would have travelled a different length and would be displaced in time. Due to this, when they are combined at the mobile handset, it will cause interference resulting in poor signal quality. This is known as ''fading''. This problem is handled in a very good way in CDMA. Here, the phase of the multiple signals is modified such that only positive interference(addition) takes place and the overall signal strength increases. A receiver that implements the above principle is known as a RAKE receiver as shown in the figure below.<br /> [[Image:cdma15.jpg|thumb|center|600px|RAKE receiver]]<br /> === Near Far Problem === <br /> The problem is best described by taking an example: Consider a receiver and two transmitters (one close to the receiver; the other far away). If both transmitters transmit simultaneously and at equal powers, then due to the inverse square law, the receiver will receive more power from the nearer transmitter. This makes the farther transmitter voice more difficult to understand. Since one transmission's signal is the other's noise the signal-to-noise ratio (SNR) for the farther transmitter is much lower. If the nearer transmitter transmits a signal that is orders of magnitude higher than the farther transmitter, then the SNR for the farther transmitter may be below detectability and the farther transmitter may just as well not transmit. This effectively jams the communication channel. In CDMA systems, this is commonly solved by dynamic output power adjustment of the transmitters. That is, the closer transmitters use less power so that the SNR for all transmitters at the receiver is roughly the same. This sometimes can have a noticeable impact on battery life, which can be dramatically different depending on distance from the base station.<br /> [[Image:cdma16.jpg|thumb|600px|center|Dynamic output power adjustment for CDMA transmitters]]<br /> <br /> ===Power Control=== <br /> As the propagation losses between BS and MS's are different according to individual communication distances, the received levels at the base station are different from each other when all mobile stations transmit their signals at the same power. Moreover, the received level fluctuates quickly due to fading. In order to maintain the strength of received signal level at BS, power control technique must be employed in CDMA systems.&lt;br&gt;.<br /> [[Image:cdma17.jpg]]&lt;br&gt;<br /> Power control can be implemented in two ways : open loop power control and closed loop power control&lt;br&gt;<br /> [[Image:cdma18.jpg]]<br /> <br /> '''Effect of Power Control''': Power control is capable of compensating the fading fluctuation. Received power from all MS are controlled to be equal.　Near-Far problem is mitigated by the power control.<br /> [[Image:cdma19.jpg]]<br /> <br /> <br /> ==Quality of Service(QoS)==<br /> CDMA is being accepted as a third generation (3G) system and a specific feature of 3G systems is that they offer a radio interface adapted for all kinds of services and combination of services (such as data, voice, video etc). The big challenge is multiplexing these services which do not have the same demands in terms of quality of service(QoS) which can be represented as BER(bit error rate), processing delay, frame error rate etc. Different QoS will require different channel encoding and interleaving strategies. The demand of BER can be satisfied when the coding bits have at least a code dependent ratio Eb/I(ratio of bit energy to interference). <br /> <br /> ===Need for Rate Matching===<br /> In a system using Multiple Access CDMA technology, the greater the Eb/I ratio the greater is the QoS. Transport channels having different QoS requirement do not have the same need in terms of Eb/I ratio. If all the channels are allocated a fixed Eb/I ratio which corresponds with the maximum required by a transport channel then other channels will have &quot;too&quot; good a Quality of Service, needlessly causing interference and resource blocking. There are several influences that might change system performance(BER) and hence Eb/I ratio,in accordance with the required QoS of which the most effective is variation of Bit Rate by a step of '''Rate Matching'''. The standard framework for the management of QoS in CDMA systems is shown below. The following framework highlights the various steps involved in providing variable QoS. The received data from the transport block is classified into different processes based on their QoS. Data is split onto various transport channels to which a CRC code is attached for error correction. Further, all these transport channels are multiplexed on one line by concatenation, interleaved, segmented and then rate matched. The rate matching step is performed using the rate matching ratio and puncturing ratio which is received from the sending entity (an exchange of handshaking signals occurs).&lt;br&gt;<br /> [[Image:cdma_2_7.jpg|thumb|700px|center|QoS Management in CDMA - Standard Framework]]<br /> <br /> The rate matching step in above figure is essentially implemented by repetition or puncturing, SIEMENS has proposed an algorithm to ETSI, to obtain a non-integer punture/repetition ratio referenced SM/G2/UMTS-L1/Tdoc428/98 and it is given as follows. This algorithm is used as a standard approach for Rate Matching. <br /> [[Image:cdma21.jpg|thumb|700px|center|Rate matching algorithm by SEIMENS]]<br /> <br /> ===QoS Management Algorithms===<br /> Quality of Service can be managed according to the varying type of traffic i.e. data, voice, video in the following four ways.<br /> # Rate Matching Algorithm<br /> # Code Hopping Algorithm<br /> # Dynamic Resource Scheduling(DRS) Algorithm<br /> # Optimal Power Control Algorithm<br /> [[Image:cdma_22.jpg|thumb|600 px|center|QoS Management in CDMA - Analysis restricted till 1999]]<br /> <br /> ===Rate Matching Algorithm===<br /> The patent [http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1385290&amp;F=0 EP1385290] titled &quot;Method for balancing Eb/I ratio in a service multiplexing CDMA system and a telecommunication system using this method&quot; targets this concept of Rate matching and introduces an algorithm for calculating effective data output bits by a process of repetition or puncturing of the input bits governed by a '''rate matching ratio''' and '''puncturing ratio''' received from the sending entity (can be a BS or MS). As the number of services increases the number of potential combinations will also increase. There arises a need for simple arithmetic procedures to calculate the transport sizes which is done using the following three rules.<br /> # The first rule concerns Channel encoding wherin the transport block is converted into the coded block by a possible relation of the form Y=X/(coding rate)+Ntail<br /> # The second rule concerns segmentation of the coded block into the size of the segment produced by segmentation per multiplexing frame<br /> # The third rule is about obtaining the size of the oputput block Y from the Input block X according to a rate matching step explained below.&lt;br&gt;<br /> The Parameters Ei(Energy per bit),Pi(Max puncture Rate) and Xi(Input data rate) are the characteristic constants of a transport channel both at the Mobile Station(MS) and the Base Station(BS). Initially Ei,Pi and Xi are determined at the Base Station and a maximum possible payload is calculated. This is known as the intermediate size and and a vector of expected is transmitted to the Mobile Station(MS) along with the parameters Ei and Pi. Using the values of Pi,Ei and Xi the mobile will also calculate its output frame size Yi. Then final step is matching this value of Yi with the received vector of Intermediate values Yi and decide the final frame size. The bits are repeated or punctured according to the required Final Frame Size.&lt;br&gt;<br /> <br /> <br /> ===Code Hopping Algorithm===<br /> According to one of the methods of dynamic power control (Code Hopping) used in W-CDMA technology, the Rate Information (RI) field in the uplink control channel in W-CDMA frame can be used to notify the base station about the variable bit rates (VBR) it wants to send, then the base station assigns a new spreading factor for each data rate and hence the optimal power calculation is done according to the spreading factor as follows.&lt;br&gt; Spreading factor(Gi) is defined as the ratio of bandwidth of the system to the data rate of the radio frame.<br /> Mathematically,&lt;br&gt;<br /> '''Gi = W / Ri''',where W=system bandwidth which is a constant for a system and Ri= data rate of radio frame.&lt;br&gt;<br /> A power index (gi) is calculated from this Spreading Factor(Gi) using the following expression&lt;br&gt;<br /> '''gi= (vi / (vi+Gi))''', where vi is minimum QoS for the ith session which is a constant.&lt;br&gt; <br /> This power index will ascertain the optimal power to be alloted to each service channel(each data rate for different services).&lt;br&gt; <br /> '''Pi = (gi*No*W )/ (Hi*(1-(Sgj)'''&lt;br&gt;<br /> where No is AWGN(Additive White Guassian Noise)a constant,&lt;br&gt; <br /> Hi is path loss which is dependent on the distance and is a constant for a path,&lt;br&gt; <br /> and Sgj is sum of the power index of all the sessions which is constant for all sessions of the radio frame.<br /> <br /> From the above analysis, we observe that when the mobile is sent the optimal power at which it should transmit. It can backtrack and calculate the power index and spreading factor and hence the Data rate is changed accordingly. This step can be considered to be an equivalent to the Rate Matching Algorithm explained above. The method and algorithm to schedule optimal power is detailed in the IEEE paper 765366 [[Media:IEEEGurbuz.pdf|Dynamic Resource Scheduling for Variable QoS Traffic in W-CDMA - Ozgur Gurbuz, Henry Owen]]. <br /> <br /> Thus, we conclude that by adjusting the optimal power we are actually trying to implement a rate matching step.<br /> <br /> ===Dynamic Resource Scheduling(DRS) Algorithm===<br /> The Mobile Station(MS) performs Matching of Traffic Descriptors such as Peak Cell Rate(PRC),Sustainable Cell Rate(SCR) and obtains the connection parameters like average cell rate, SIR, Delay from them. These parameters are sent to the Base Station(BS) where they are queued in a FIFO. The BS determines a spreading factor which allocates the Orthogonal Varible Spread code(OVSF) using '''Gi = W / Ri''',where W=system bandwidth which is a constant for a system and Ri= data rate of radio frame.&lt;br&gt; The base station calculates a value of power index '''gi= (vi / (vi+Gi))'''and hence Power levels and transmits them to the MS. This information is conveyed to the MS using TPC(Transmission Power Control) bits and a closed loop power control method as explained in section 5.6 above is performed to obtain the final value of power at which transmission should be done.The method and algorithm to schedule optimal power using Dynamic Resource Scheduling is detailed in the IEEE paper 765366 [[Media:IEEEGurbuz.pdf|Dynamic Resource Scheduling for Variable QoS Traffic in W-CDMA - Ozgur Gurbuz, Henry Owen]].<br /> <br /> ===Optimal Power Control Algorithm===<br /> The Base Station receives a Pilot Signal from the Mobile station and calculates BER based on Distance,Transmission rate and No of Users in the Cell. Ptk is the transmitted signal power which is expressed by the power control function g ( rt , k ), a function of the distance from the mobile to<br /> base station,<br /> '''Ptk= g(rt,k)Po''' <br /> where Po is the maximum transmission power. The optimum power functions are transmitted to the Mobile station which calculates the optimal power and starts transmitting at that value. Thus meeting the required QoS parameters.The method and algorithm for optimal power control is detailed in the IEEE paper 503476 [[Media:IEEEYao.pdf|Optimal power control law for Multi-media - Multi-rate CDMA systems<br /> - Shee Yao and Evaggelos Geraniotis<br /> ]].<br /> <br /> ==Research Activity (Non Patent) in the Period (1991-2003)==<br /> NOTE: The analysis presented below is with respect to the IEEE Papers published between 1991-2003 which focus on the aspect of Quality of Service and its Management using various paramters like Rate matching, Power control, Variable Spreading Factor etc.<br /> <br /> [[Image:Publication_Year.JPG|center|thumb|500 px|Number of publications VS Year of publication]]<br /> The above analysis suggests a increase in the Research activity in the area of QoS Management in the year 1999.<br /> <br /> [[Image:Publishers.JPG|center|thumb|500 px|Publisher VS number of publications during(1991-2003)]]<br /> <br /> It is to be noted that the non patent research is attributed mostly to universities in USA and Asia Pacific. The mention of '''IEEE member''' in the above graph indicates the absence of information about the parent department of the Researcher.<br /> <br /> [[Image:CDMA_-_3D.JPG|center|thumb|500 px|Graph showing number of publications by the publishers during 1991-2003]]<br /> <br /> <br /> <br /> ==Conclusion==<br /> Substantial amount of research has been done in the field of QoS in CDMA communication system in the year 1998-99 and this has led to the invention of multitude of methodologies ranging from power control to Rate matching and Dynamic Resource scheduling, all with the sole aim of improving QoS.</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Dolcera_Offerings&diff=1896 2006-07-02T18:33:50Z

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I used your presentation for my company's Board (of Directors).<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Business plans&quot;&gt;<br /> <br /> == Business plans ==<br /> Dolcera works in partnership with research and development groups within companies to help them understand the business opportunities for their research. We develop full-strength business plans with:<br /> * Commercialization possibilities for research<br /> * Competitive landscape<br /> * SWOT Analysis: Strengths, Weaknesses, Opportunities, Threats<br /> <br /> [[Image:swot_sample.jpg|thumb|250px|center|SWOT Analysis]]<br /> ==== Case study: Business plans ====<br /> {{CaseStudy<br /> | topic = Business plans<br /> | client = A global software company<br /> | goal = Create business case for a research project with several patent applications<br /> | duration = 6 weeks<br /> | result = Complete business plan including market research, financial plan, competitive analysis, product positioning, product and need characteristics<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Strong technology and business expertise to help researchers shorter innovation cycle<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = Dolcera is an integral part of our research commercialization strategy.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executive dashboard&quot;&gt;<br /> <br /> == Executive dashboard ==<br /> The Dolcera executive IP dashboard provides an integrated view of all the key performance indicators for your organization's intellectual property, including:<br /> * Patent filings<br /> * Patent licensing opportunities<br /> * Patent threats<br /> * Competitive position<br /> * Key IP performance indicators<br /> <br /> The interactive executive IP dashboard allows users to perform their own what-if analysis. Behind the scenes, the Dolcera team performs extensive research and market+competitive analysis to drive the executive dashboard and keep it up-to-date.<br /> <br /> &lt;gflash&gt;600 600 http://dolcera.com/ipmapdemo/rfid_model.swf&lt;/gflash&gt;<br /> <br /> ==== Case study: Executive dashboard ====<br /> {{CaseStudy<br /> | topic = Executive dashboard<br /> | client = A US medical device major<br /> | goal = Provide a central point of entry for all corporate IP performance indicators<br /> | duration = Ongoing<br /> | result = All patent information in one spot, and shared by all stakeholders within the organization.<br /> | customer_savings = Greater overall visibility improves response time considerably<br /> | dolcera_advantage = Correlating market movements with IP information and technology trends<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/alopecia_model.swf Consumer products dashboard], [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID Dashboard]<br /> | quote = The dashboard helps our team think strategically.<br /> }}<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Brand dashboard&quot;&gt;<br /> == Brand dashboard ==<br /> The brand manager dashboard is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard identifies the impact of global and local events on client's and competitor's brands. It brings together data from a variety of data sources. It also includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> &lt;gflash&gt;600 600 http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf&lt;/gflash&gt;<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Collaboration services&quot;&gt;<br /> <br /> == Collaboration services ==<br /> Dolcera provides a range of collaboration services for large organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup<br /> * Taxonomy design and updates<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> [[Image:taxonomy.jpg|thumb|300px|center|Dolcera taxonomy tool]]<br /> <br /> ==== Case study: Collaboration services ====<br /> {{CaseStudy<br /> | topic = Collaboration services<br /> | client = Large pharmaceutical company<br /> | goal = Provide a central Human Resources forms and document system for the corporate intranet.<br /> | duration = 2 months<br /> | result = We prepared the taxonomy and classification system for all documents and classified the documents initially. We also trained clients to update the documents on an ongoing basis.<br /> | customer_savings = Approximately $300,000 for the project<br /> | dolcera_advantage = Best-in-class technology and processes, ably supported by our technical team in India <br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IPMap]<br /> | quote = Our goal is to be a smarter organization, and Dolcera helped us achieve it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Intellectual asset management services&quot;&gt;<br /> == Intellectual asset management services==<br /> Dolcera takes medium- to large-sized patent portfolios and:<br /> # Creates a taxonomy to organize the patents<br /> # Organizes the patents inside the taxonomy <br /> # Identify and juxtapose the key competitive patent and non-patent documents<br /> # Identify products and 'virtual products' related to different sets of patents<br /> # Highlight the key strengths, weaknesses, opportunities and threats<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Technology trends research&quot;&gt;<br /> == Technology trends research ==<br /> Technology changes rapidly and it is often difficult to keep track of all the trends swirling on the Internet, all the ideas bubbling in academia, and the range of innovations you and your competitors are working on. Dolcera provides a sophisticated service to track technology trends, juxtaposing academic research, market data and patent filings information worldwide. <br /> <br /> [[Image:future_trends.jpg|thumb|400px|center|RFID technology trends]]<br /> <br /> ==== Case study: Technology trends research ====<br /> {{CaseStudy<br /> | topic = Technology trends research<br /> | client = Major technology company<br /> | goal = Provide an overview of technology directions of an important technology topic.<br /> | duration = 2 months<br /> | result = We identified the key technology trends, the patent information worldwide and provided predictions for the 'next big thing'<br /> | customer_savings = Potentially millions, with timely positioning of new offerings<br /> | dolcera_advantage = Constant monitoring of technology trends<br /> | sample_links = [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = We are swamped with information and are unable to digest it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> <br /> == Dolcera offerings maps ==<br /> <br /> {| class=&quot;wikitable&quot; style=&quot;font-size:120%&quot; border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; <br /> |- style=&quot;background:lightgrey&quot;<br /> ! 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[[#Technology trends research | Technology trends research]]<br /> | Monitor technology, IP and market trends || Medium and large companies || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf Technology trends report] <br /> |}<br /> <br /> <br /> == Questions Dolcera answers ==<br /> We help you answer questions such as:<br /> {| border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; align=&quot;center&quot; valign=&quot;top&quot;<br /> |-<br /> | <br /> * '''What’s hot'''<br /> ** What technology/approaches are the most promising?<br /> ** What technology/approaches have already been tried?<br /> ** What can I license?<br /> ** Is any empirical data available?<br /> * '''Where should I focus my R&amp;D investment'''<br /> ** Where’s the ‘white space’ for me to play in?<br /> * '''Any hints for research'''<br /> ** Are there any combinations I could develop?<br /> | <br /> * '''What should I do in this geography'''<br /> ** What are my competitors up to in this geography?<br /> ** What are my strengths/ weaknesses here?<br /> * '''What’s my competition up to'''<br /> ** What’s my top competitor investing in?<br /> ** Are there any loopholes in their strategy?<br /> ** Will a competitor emerge from nowhere and surprise me?<br /> ** What are the crowded areas?<br /> * '''How do I play defense'''<br /> ** What should my blocking/reactive strategies be?<br /> |}<br /> <br /> == Dolcera Expertise ==<br /> The Dolcera team has expertise in:<br /> * Technology analysis in the areas of chemistry, biotechnology, computer software, electronics, communication and mechanical engineering.<br /> * Market research - primary and secondary - across multiple industries <br /> * Information integration for large sets of structured and unstructured data<br /> * Collaboration tools and technology including wikis, blogs and Web 2.0</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Quality_of_Service_on_CDMA_platforms&diff=1885 2006-07-02T17:36:34Z

<p>67.180.226.207: </p> <hr /> <div>== Cellular Communication ==<br /> A cellular mobile communications system uses a large number of low-power wireless transmitters to create cells — the basic geographic service area of a wireless communications system. Variable power levels allow cells to be sized according to the subscriber density and demand within a particular region. As mobile users travel from cell to cell, their conversations are handed off between cells to maintain seamless service. Channels (frequencies) used in one cell can be reused in another cell some distance away. Cells can be added to accommodate growth, creating new cells in unserved areas or overlaying cells in existing areas. [http://www.IEC.org Source]<br /> <br /> There are three main entities in cellular communication<br /> * Mobile Station (MS): A mobile station consists of 2 entities - equipment and SIM card<br /> * Base Transceiver station(BTS): A base transceiver station consists of 2 entities - a base transceiver (transmitter and receiver) station and a base station controller. The BTS is the antenna tower site.<br /> * Main Switching centre(MSC): The main switching centre is the heart of the network - the central switching office which controls all the base stations and provides connection with landline phones. It performs three main tasks. It:<br /> # connects calls from sender to receiver,<br /> # collects details of the calls made and received, and<br /> # supervises operation of the rest of the network components.<br /> <br /> == Cellular System Architecture ==<br /> Cellular systems are increasing in demand as more users are added to their systems. The amount of frequency spectrum available for mobile cellular use was limited, and efficient use of the required frequencies was needed for mobile cellular coverage. In modern cellular telephony, rural and urban regions are divided into areas according to specific provisioning guidelines. Provisioning for each region is planned according to an engineering plan that includes cells, clusters, frequency reuse, and handovers.<br /> <br /> ==== Cells ==== <br /> A cell is the basic geographic unit of a cellular system. Cells are base stations transmitting over small geographic areas that are represented as hexagons.<br /> <br /> ==== Clusters ==== <br /> A cluster is a group of cells. No channels are reused within a cluster. Normally a cluster has seven cells in it as shown below.<br /> <br /> ==== Frequency Reuse ====<br /> The number of radio channel frequencies is limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> ==== Cell Splitting ==== <br /> As a service area becomes full of users, this approach is used to split a single area into smaller ones. In this way, urban centers can be split into as many areas as necessary to provide acceptable service levels in heavy-traffic regions, while larger, less expensive cells can be used to cover remote rural regions.<br /> <br /> ==== Handoff ====<br /> <br /> The final obstacle in the development of the cellular network involved the problem created when a mobile subscriber traveled from one cell to another during a call. As adjacent areas do not use the same radio channels, a call must either be dropped or transferred from one radio channel to another when a user crosses the line between adjacent cells. Because dropping the call is unacceptable, the process of handoff was created. Handoff occurs when the mobile telephone network automatically transfers a call from radio channel to radio channel as a mobile crosses adjacent cells.<br /> <br /> ==Evolution of Cellular Systems==<br /> [[Image:cdma1.jpg|500 px|center]]<br /> == Multiple Access Methods ==<br /> There are predominantly three types of multiple access methods.<br /> === Frequency Division Multiple Access ===<br /> In this system, each user is allotted a different set of frequencies to operate upon. The uplink(mobile to base station) frequency is different from downlink frequency(base station to mobile).<br /> [[Image:cdma6.jpg|thumb|700px|center|[http://www.ai.u-hyogo.ac.jp/~thai-proj/presen/20051222-Ishikawa.ppt FDMA]]]<br /> === Time Division Multiple Access ===<br /> In this system, each user is allocated a different time slot. Forward link frequency and reverse link frequency is the same. A synchronous switch is responsible for the time switching.<br /> [[Image:cdma10.jpg|thumb|600px|center|TDMA]]<br /> <br /> === Code Division Multiple Access ===<br /> There is no restriction on time and frequency in this scheme. All the users can transmit at all times and at all frequencies. Because users are isolated by code, they can share the same carrier frequency, eliminating the frequency reuse problem encountered in other technologies.<br /> [[Image:cdma11.jpg|thumb|600 px|centre|CDMA]]&lt;br&gt;<br /> <br /> A comparative study between the above three access technologies with respect to time and frequency is as shown below.<br /> [[Image:cdma12.jpg|thumb|600 px|centre|Comparison of cellular access schemes]]<br /> <br /> == Code Division Multiple Access ==<br /> The CDMA technology can be implemented by spreading the spectrum which can be done in the following two ways<br /> * Direct Sequence Spread Sprectrum - DSSS CDMA<br /> * Frequency Hopping - FH CDMA<br /> === Direct Sequence Spread Sprectrum - DSSS CDMA === <br /> In this method, the direct sequence(input data) which is spread over a limited bandwidth is multiplied with a code or spreading sequence (a pseudorandom sequence also known as PN sequence) which will spread the input data over the entire bandwidth of the communication channel. The power density is also reduced and is spread over the frequency spectrum and hence is known as spread spectrum method. The modulation part of DSSS is as shown below.<br /> [[Image:cdma13.jpg|thumb|600px|center|CDMA Modulation]]<br /> The modulated signal is transmitted over the channel and all users can receive it but only the user which knows the correct code can decode the message. This is depicted in the figure below.<br /> [[Image:cdma14.jpg|thumb|600px|center|CDMA Demodulation]]<br /> * CDMA's spread spectrum technique overlaps every transmission on the same carrier frequency by assigning a unique code to each conversation.<br /> * The signal is spread at two levels first using a Walsh Code and then using a PN Code. The number of bits in either of the two codes is known as the &quot;chip rate,&quot; and each bit in the spreading signal is called a &quot;chip&quot;. One bit from each conversation (baseband signal)is multiplied with the walsh code and then the PN code by the spreading techniques, giving the receiving side an enormous amount of data it can average just to determine the value of one bit.<br /> * Base station is the one that assigns spreading code to each call when a mobile requests for a call (unique Walsh code for each conversation and a same PN code for each call in a cell sector). In the analysis henceforth we discuss the dynamic allocation of these spread codes in accordance with the required QoS.<br /> <br /> === Frequency Reuse === <br /> The number of radio channel frequencies is limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> === Soft Handoff === <br /> Handoff means switching a cellular phone transmission from one cell to another as a mobile user moves into a new cellular area. It is so called because the radio link with the previous sector(s) is not broken before a link is established with a new sector; this type of handoff is described as &quot;make before break&quot;. In CDMA, due to this soft handoff, there is no interruption of call even at the border of a cell site which means more number of customers can be accommodated, automatically increasing the capacity of the cell site.<br /> <br /> === Multipath Fading === <br /> In a mobile environment, a mobile station will receive one direct signal from the base station and multiple signals which are reflected from obstructions like buildings and towers. Each signal would have travelled a different length and would be displaced in time. Due to this, when they are combined at the mobile handset, it will cause interference resulting in poor signal quality. This is known as ''fading''. This problem is handled in a very good way in CDMA. Here, the phase of the multiple signals is modified such that only positive interference(addition) takes place and the overall signal strength increases. A receiver that implements the above principle is known as a RAKE receiver as shown in the figure below.<br /> [[Image:cdma15.jpg|thumb|center|600px|RAKE receiver]]<br /> === Near Far Problem === <br /> The problem is best described by taking an example: Consider a receiver and two transmitters (one close to the receiver; the other far away). If both transmitters transmit simultaneously and at equal powers, then due to the inverse square law, the receiver will receive more power from the nearer transmitter. This makes the farther transmitter voice more difficult to understand. Since one transmission's signal is the other's noise the signal-to-noise ratio (SNR) for the farther transmitter is much lower. If the nearer transmitter transmits a signal that is orders of magnitude higher than the farther transmitter, then the SNR for the farther transmitter may be below detectability and the farther transmitter may just as well not transmit. This effectively jams the communication channel. In CDMA systems, this is commonly solved by dynamic output power adjustment of the transmitters. That is, the closer transmitters use less power so that the SNR for all transmitters at the receiver is roughly the same. This sometimes can have a noticeable impact on battery life, which can be dramatically different depending on distance from the base station.<br /> [[Image:cdma16.jpg|thumb|600px|center|Dynamic output power adjustment for CDMA transmitters]]<br /> <br /> ===Power Control=== <br /> As the propagation losses between BS and MS's are different according to individual communication distances, the received levels at the base station are different from each other when all mobile stations transmit their signals at the same power. Moreover, the received level fluctuates quickly due to fading. In order to maintain the strength of received signal level at BS, power control technique must be employed in CDMA systems.&lt;br&gt;.<br /> [[Image:cdma17.jpg]]&lt;br&gt;<br /> Power control can be implemented in two ways : open loop power control and closed loop power control&lt;br&gt;<br /> [[Image:cdma18.jpg]]<br /> <br /> '''Effect of Power Control''': Power control is capable of compensating the fading fluctuation. Received power from all MS are controlled to be equal. Near-Far problem is mitigated by the power control.<br /> [[Image:cdma19.jpg]]<br /> <br /> ==Quality of Service(QoS)==<br /> CDMA is being accepted as a third generation (3G) system and a specific feature of 3G systems is that they offer a radio interface adapted for all kinds of services and combination of services (such as data, voice, video etc). The big challenge is multiplexing these services which do not have the same demands in terms of quality of service(QoS) which can be represented as BER(bit error rate), processing delay, frame error rate etc. Different QoS will require different channel encoding and interleaving strategies. The demand of BER can be satisfied when the coding bits have at least a code dependent ratio Eb/I(ratio of bit energy to interference). There are several influences that might change system performance(BER) and hence Eb/I ratio, of which the most effective is variation of Bit Rate by a step of '''Rate Matching'''. The standard framework for the management of QoS in CDMA systems is shown below. The transport block is divided into different processes and all the channels of like QoS are included in one process. The standard steps of multiplexing, encoding, and interleaving are followed by an important procedure of rate matching, wherein the data rate is varied in accordance with the Eb/I ratio(QoS parameter). Apart from this pathway, there are other pathways which focus on the power control aspect and a relation ship to rate matching can be backtracked through this approach.<br /> [[Image:cdma25.jpg|thumb|600px|center|QoS Management in CDMA - Pathway]]<br /> <br /> The process of Implementation of rate Matching is done using Puncturing or Repetition. If the number of bits are more than the calculated rate of transmission then the bits of transmission block are punctured otherwise they are repeated till the calculated size is reached. Siemens has proposed an algorithm to ETSI, to obtain a non-integer punture/repetition ratio referenced SM/G2/UMTS-L1/Tdoc428/98 and it is given as follows. This algorithm is used as a standard approach for Rate Matching. <br /> [[Image:cdma21.jpg|thumb|700px|center|Rate matching algorithm by Siemens]]<br /> ===Rate Matching and QoS===<br /> The patent [http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1385290&amp;F=0 EP1385290] titled &quot;Method for balancing Eb/I ratio in a service multiplexing CDMA system and a telecommunication system using this method&quot; targets this concept of Rate matching and introduces an algorithm for calculating effective data output bits by a process of repetition or puncturing of the input bits governed by a '''rate matching ratio''' and '''puncturing ratio''' received from the sending entity (can be a BS or MS). The Parameters Ei(Energy per bit),Pi(Max puncture Rate) and Xi(Input data rate) are the characteristic constants of a transport channel both at the Mobile Station(MS) and the Base Station(BS). Initially Ei,Pi and Xi are determined at the Base Station and a maximum possible payload is calculated. This is known as the intermediate size and and a vector of expected is transmitted to the Mobile Station(MS) along with the parameters Ei and Pi. Using the values of Pi,Ei and Xi the mobile will also calculate its output frame size Yi. Then final step is matching this value of Yi with the received vector of Intermediate values Yi and decide the final frame size. The bits are repeated or punctured according to the required Final Frame Size.&lt;br&gt;<br /> The following framework highlights the various steps involved in providing variable QoS. The received data from the transport block is classified into different processes based on their QoS. Data is split onto various transport channels to which a CRC code is attached for error correction. Further, all these transport channels are multiplexed on one line by concatenation, interleaved, segmented and then rate matched. The rate matching step is performed using the rate matching ratio and puncturing ratio which is received from the sending entity (an exchange of handshaking signals occurs).<br /> <br /> <br /> <br /> The rate matching step in above figure is essentially implemented by repetition or puncturing, Siemens has proposed an algorithm to ETSI, to obtain a non-integer punture/repetition ratio referenced SM/G2/UMTS-L1/Tdoc428/98 and it is given as follows. This algorithm is used as a standard approach for Rate Matching. <br /> [[Image:cdma21.jpg|thumb|700px|center|Rate matching algorithm by Siemens]]<br /> <br /> The above algorithm avoids puncturing consecutive bits when operating in the puncturing mode. In the repetition mode, the repetition bits follow the bits which they repeat. [[Interleaving]] is an essential step in a communication systems. In the current scenario of repetition,when interleaving is executed after rate matching it would space the repeated bits apart. While Puncturing, if the interleaver precedes the rate matching it may puncture consecutive bits of the channel encoder which were dispersed by interleaving. Hence it is always preffered to have the rate matching step as close as possible to the Channel Encoder<br /> <br /> ===Power Control, Rate Matching and QoS using Code Hopping===<br /> According to one of the methods of dynamic power control (Code Hopping) used in W-CDMA technology, the Rate Information (RI) field in the uplink control channel in W-CDMA frame can be used to notify the base station about the variable bit rates (VBR) it wants to send, then the base station assigns a new spreading factor for each data rate and hence the optimal power calculation is done according to the spreading factor as follows.&lt;br&gt; Spreading factor(Gi) is defined as the ratio of bandwidth of the system to the data rate of the radio frame.<br /> Mathematically,&lt;br&gt;<br /> '''Gi = W / Ri''',where W=system bandwidth which is a constant for a system and Ri= data rate of radio frame.&lt;br&gt;<br /> A power index (gi) is calculated from this Spreading Factor(Gi) using the following expression&lt;br&gt;<br /> '''gi= (vi / (vi+Gi))''', where vi is minimum QoS for the ith session which is a constant.&lt;br&gt; <br /> This power index will ascertain the optimal power to be alloted to each service channel(each data rate for different services).&lt;br&gt; <br /> '''Pi = (gi*No*W )/ (Hi*(1-(Sgj)'''&lt;br&gt;<br /> where No is AWGN(Additive White Guassian Noise)a constant,&lt;br&gt; <br /> Hi is path loss which is dependent on the distance and is a constant for a path,&lt;br&gt; <br /> and Sgj is sum of the power index of all the sessions which is constant for all sessions of the radio frame.<br /> <br /> From the above analysis, we observe that the bit rate is inversely proportional to the spreading factor which will inversely effect the power index and hence the optimal power. Therefore, the Bit Rate and Optimal power go hand in hand, and have the same effect on Eb/I and QoS.<br /> <br /> The method and algorithm to schedule optimal power is detailed in the IEEE paper 765366 [[Media:IEEEGurbuz.pdf|Dynamic Resource Scheduling for Variable QoS Traffic in W-CDMA - Ozgur Gurbuz, Henry Owen]]. <br /> <br /> Thus, we conclude that by adjusting the optimal power we are actually trying to implement a rate matching step.<br /> <br /> ===Power control and QoS using Dynamic Resource Scheduling(DRS) Pathway===<br /> The Mobile Station(MS) performs Matching of Traffic Descriptors such as Peak Cell Rate(PRC),Sustainable Cell Rate(SCR) and obtains the connection parameters like average cell rate, SIR, Delay from them. These parameters are sent to the Base Station(BS) where they are queued in a FIFO. The BS determines a spreading factor which allocates the Orthogonal Varible Spread code(OVSF) using '''Gi = W / Ri''',where W=system bandwidth which is a constant for a system and Ri= data rate of radio frame.&lt;br&gt; The base station calculates a value of power index '''gi= (vi / (vi+Gi))'''and hence Power levels and transmits them to the MS. This information is conveyed to the MS using TPC(Transmission Power Control) bits and a closed loop power control method as explained in section 5.6 above is performed to obtain the final value of power at which transmission should be done.The method and algorithm to schedule optimal power using Dynamic Resource Scheduling is detailed in the IEEE paper 765366 [[Media:IEEEGurbuz.pdf|Dynamic Resource Scheduling for Variable QoS Traffic in W-CDMA - Ozgur Gurbuz, Henry Owen]].<br /> <br /> ===QoS Management using Optimal Power Control Pathway===<br /> The Base Station receives a Pilot Signal from the Mobile station and calculates BER based on Distance,Transmission rate and No of Users in the Cell. Ptk is the transmitted signal power which is expressed by the power control function g ( rt , k ), a function of the distance from the mobile to<br /> base station,<br /> '''Ptk= g(rt,k)Po''' <br /> where Po is the maximum transmission power. The optimum power functions are transmitted to the Mobile station which calculates the optimal power and starts transmitting at that value. Thus meeting the required QoS parameters.The method and algorithm for optimal power control is detailed in the IEEE paper 503476 [[Media:IEEEYao.pdf|Optimal power control law for Multi-media - Multi-rate CDMA systems<br /> - Shee Yao and Evaggelos Geraniotis<br /> ]].<br /> <br /> ==Conclusion==<br /> Substantial amount of research has been done in the field of QoS in CDMA communication system in the year 1998-99 and this has led to the invention of multitude of methodologies ranging from power control to Rate matching and Dynamic Resource scheduling, all with the sole aim of improving QoS.</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Dolcera_Offerings&diff=1882 2006-07-02T11:14:20Z

<p>67.180.226.207: </p> <hr /> <div>== Dolcera for your organization: Technology, IP and Market Research ==<br /> Dolcera's mission is to provide information integration and outsourced research services for decision support. Our services are targeted towards multiple types of '''knowledge workers''' within organizations including:<br /> # [[#Researchers|Researchers, engineers and technologists]]<br /> # [[#Patent Counsel|Patent counsel and attorneys]]<br /> # [[#Knowledge managers|Knowledge managers]]<br /> # [[#Marketers|Marketers and brand managers]]<br /> # [[#Executives|Senior executives and strategists]]<br /> &lt;div id=&quot;Researchers&quot;&gt;<br /> === Dolcera for Researchers ===<br /> Dolcera works with researchers, engineers and technologists, and provides them with very high-quality technology and market information through our '''[[#Technology reports | technology reports]]'''. Our technical team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Patent Counsel&quot;&gt;<br /> === Dolcera for Patent Counsel and Attorneys ===<br /> Dolcera provides the intellectual property (IP) teams with a variety of services including:<br /> * Prior art, invalidation and infringement searches ([[#IPMaps |Dolcera IPMaps]])<br /> * Technical writing and patent drafting<br /> * [[#Technology reports | Technology reports]]<br /> * [[#Intellectual asset management services | IP asset management services]]<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Knowledge managers&quot;&gt;<br /> === Dolcera for Knowledge Managers ===<br /> Knowledge managers are faced with a rapidly changing environment that includes a plethora of new tools (blogs, wikis, the semantic web etc.) and many challenges to go with them (e.g. taxonomy organization). Dolcera provides a range of '''[[#Collaboration services |collaboration services]]''' for managers of knowledge-driven organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup and management<br /> * Taxonomy design and updates for large taxonomies<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Marketers&quot;&gt;<br /> === Dolcera for Brand Managers ===<br /> The '''[[#Brand dashboard |brand manager dashboard]]''' is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard:<br /> # Identifies the impact of global and local events on client's and competitor's brands,<br /> # Brings together data from a variety of data sources, and<br /> # Includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executives&quot;&gt;<br /> === Dolcera for Strategists and Executives ===<br /> Executives and strategists use the integrated '''[[#Executive dashboard|executive dashboards]]''' to obtain a comprehensive overview of market, research and IP trends. Other services from Dolcera include:<br /> # [[#Business plan|Business plan development]]<br /> # [[#Timelines|Timelines]]<br /> # [[#Technology trends research|Technology trends research]]<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Technology reports&quot;&gt;<br /> <br /> == Technology reports ==<br /> Dolcera team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> The unique aspects of Dolcera's technology reports are:<br /> * High quality of technology and market analysis,<br /> * Interactive development in partnership with client, and<br /> * Continuous updates <br /> <br /> [[Image:report_sample.jpg|thumb|500px|center|[http://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss Alopecia report]]]<br /> <br /> ==== Case study: Technology reports ====<br /> {{CaseStudy<br /> | topic = Technology reports<br /> | client = A large medical device company<br /> | goal = Create a technology report on one of the newest types of cardiac devices. Integrate data from a variety of data sources.<br /> | duration = Intial preparation - 4 weeks<br /> | result = The Dolcera report was shared between the research, marketing and legal groups within the client corporation. Dolcera also provides monthly updates for this report.<br /> | customer_savings = Approximately 1/8th of the cost <br /> | dolcera_advantage = Multi-disciplinary data integration, rapid results, low costs<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System Hybrid Electric Vehicle report]<br /> | quote = We can collaborate much more easily now.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;IPMaps&quot;&gt;<br /> <br /> == IPMaps ==<br /> Dolcera IPMaps present the comprehensive view of intellectual property in a particular area. Prepared by highly-trained technical analysts, Dolcera IPMaps are:<br /> * Comprehensive<br /> * Interactive<br /> * Visually clear-cut<br /> * Database-driven<br /> <br /> [[Image:Satellite_Antenna_IPMap.jpg|thumb|500px|center|[http://www.dolcera.com/ipmapdemo/satellite_antenna/impamp.html Satellite Antenna IPMap]]]<br /> ==== Case study: IPMaps ====<br /> {{CaseStudy<br /> | topic = IPMaps<br /> | client = A Fortune 500 software company<br /> | goal = Provide an overview of the company's patent portfolio in a key technology area.<br /> | duration = 2 weeks<br /> | result = The Dolcera IPMap integrated patent and competitive information from a variety of sources in one 'snapshot' IPMap that was used by the client for validating the market space and their own research strength.<br /> | customer_savings = Approximately 1/5th of the cost <br /> | dolcera_advantage = Data integration, technology expertise, speed, low costs<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/rfid/ipmap.html RFID IPMap], [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Hair loss IPMap], [http://www.dolcera.com/ipmapdemo/multimodal_apps/ipmap.html Multimodal applications IPMap]<br /> | quote = You showed us how small this market is. We would not have entered this market if we had this information in advance.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Timelines&quot;&gt;<br /> == Timelines ==<br /> Certain fields of research progress at bewildering speeds. It is often impossible for researchers, technology experts and executives alike to keep track of the developments. Dolcera timelines are exactly what their name implies: interactive visual maps that show the development of a field over the course of time. Our timelines are used for a variety of purposes including:<br /> * Understanding the development of a field of science/technology<br /> * Determining the contributions of individuals/companies to <br /> * Juxtaposing market and technology developments<br /> <br /> [[Image:timeline_sample_2.jpg|thumb|500px|center|Sample timeline]]<br /> ==== Case study: Timelines ====<br /> {{CaseStudy<br /> | topic = Timelines<br /> | client = A major N. American smartphone manufacturer<br /> | goal = Determine inventorship of some of the most important cellular telephony standards by analyzing patent, standard and market data.<br /> | duration = 4 weeks<br /> | result = Dolcera timelines, based on research through several gigabytes of standards meetings minutes, specifications and patents, allowed the client to negotiate with their competitors.<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Powerful search tools, data integration from disparate sources, succinct presentation<br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Sample timeline]<br /> | quote = I did not even have to lift a finger to understand the information... I used your presentation for my company's Board (of Directors).<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Business plans&quot;&gt;<br /> <br /> == Business plans ==<br /> Dolcera works in partnership with research and development groups within companies to help them understand the business opportunities for their research. We develop full-strength business plans with:<br /> * Commercialization possibilities for research<br /> * Competitive landscape<br /> * SWOT Analysis: Strengths, Weaknesses, Opportunities, Threats<br /> <br /> [[Image:swot_sample.jpg|thumb|250px|center|SWOT Analysis]]<br /> ==== Case study: Business plans ====<br /> {{CaseStudy<br /> | topic = Business plans<br /> | client = A global software company<br /> | goal = Create business case for a research project with several patent applications<br /> | duration = 6 weeks<br /> | result = Complete business plan including market research, financial plan, competitive analysis, product positioning, product and need characteristics<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Strong technology and business expertise to help researchers shorter innovation cycle<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = Dolcera is an integral part of our research commercialization strategy.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executive dashboard&quot;&gt;<br /> <br /> == Executive dashboard ==<br /> The Dolcera executive IP dashboard provides an integrated view of all the key performance indicators for your organization's intellectual property, including:<br /> * Patent filings<br /> * Patent licensing opportunities<br /> * Patent threats<br /> * Competitive position<br /> * Key IP performance indicators<br /> <br /> The interactive executive IP dashboard allows users to perform their own what-if analysis. Behind the scenes, the Dolcera team performs extensive research and market+competitive analysis to drive the executive dashboard and keep it up-to-date.<br /> <br /> &lt;gflash&gt;600 600 http://dolcera.com/ipmapdemo/rfid_model.swf&lt;/gflash&gt;<br /> <br /> ==== Case study: Executive dashboard ====<br /> {{CaseStudy<br /> | topic = Executive dashboard<br /> | client = A US medical device major<br /> | goal = Provide a central point of entry for all corporate IP performance indicators<br /> | duration = Ongoing<br /> | result = All patent information in one spot, and shared by all stakeholders within the organization.<br /> | customer_savings = Greater overall visibility improves response time considerably<br /> | dolcera_advantage = Correlating market movements with IP information and technology trends<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/alopecia_model.swf Consumer products dashboard], [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID Dashboard]<br /> | quote = The dashboard helps our team think strategically.<br /> }}<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Brand dashboard&quot;&gt;<br /> == Brand dashboard ==<br /> The brand manager dashboard is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard identifies the impact of global and local events on client's and competitor's brands. It brings together data from a variety of data sources. It also includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> &lt;gflash&gt;600 600 http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf&lt;/gflash&gt;<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Collaboration services&quot;&gt;<br /> <br /> == Collaboration services ==<br /> Dolcera provides a range of collaboration services for large organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup<br /> * Taxonomy design and updates<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> [[Image:taxonomy.jpg|thumb|300px|center|Dolcera taxonomy tool]]<br /> <br /> ==== Case study: Collaboration services ====<br /> {{CaseStudy<br /> | topic = Collaboration services<br /> | client = Large pharmaceutical company<br /> | goal = Provide a central Human Resources forms and document system for the corporate intranet.<br /> | duration = 2 months<br /> | result = We prepared the taxonomy and classification system for all documents and classified the documents initially. We also trained clients to update the documents on an ongoing basis.<br /> | customer_savings = Approximately $300,000 for the project<br /> | dolcera_advantage = Best-in-class technology and processes, ably supported by our technical team in India <br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IPMap]<br /> | quote = Our goal is to be a smarter organization, and Dolcera helped us achieve it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Intellectual asset management services&quot;&gt;<br /> == Intellectual asset management services==<br /> Dolcera takes medium- to large-sized patent portfolios and:<br /> # Creates a taxonomy to organize the patents<br /> # Organizes the patents inside the taxonomy <br /> # Identify and juxtapose the key competitive patent and non-patent documents<br /> # Identify products and 'virtual products' related to different sets of patents<br /> # Highlight the key strengths, weaknesses, opportunities and threats<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Technology trends research&quot;&gt;<br /> == Technology trends research ==<br /> Technology changes rapidly and it is often difficult to keep track of all the trends swirling on the Internet, all the ideas bubbling in academia, and the range of innovations you and your competitors are working on. Dolcera provides a sophisticated service to track technology trends, juxtaposing academic research, market data and patent filings information worldwide. <br /> <br /> [[Image:future_trends.jpg|thumb|400px|center|RFID technology trends]]<br /> <br /> ==== Case study: Technology trends research ====<br /> {{CaseStudy<br /> | topic = Technology trends research<br /> | client = Major technology company<br /> | goal = Provide an overview of technology directions of an important technology topic.<br /> | duration = 2 months<br /> | result = We identified the key technology trends, the patent information worldwide and provided predictions for the 'next big thing'<br /> | customer_savings = Potentially millions, with timely positioning of new offerings<br /> | dolcera_advantage = Constant monitoring of technology trends<br /> | sample_links = [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = We are swamped with information and are unable to digest it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> <br /> == Dolcera offerings maps ==<br /> <br /> {| class=&quot;wikitable&quot; style=&quot;font-size:120%&quot; border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; <br /> |- style=&quot;background:lightgrey&quot;<br /> ! Offering !! Goal !! Client !! Role !! Demo<br /> |-<br /> ! [[#Technology reports| Technology reports]] <br /> | 360-degree view of technology and market data || Technology company || Researcher || [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV report] <br /> |-<br /> ! [[#IPMaps | IPMaps]] <br /> | Comprehensive view of a particular research area || Law firms, corporations || Researcher || [http://www.dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Satellite Antenna IPMap] <br /> |-<br /> ! [[#Timelines | Timelines]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Business plans | Business plans]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Executive dashboard| Executive dashboard]] <br /> | Up-to-date snapshot of market+competitive data || Large corporation || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID dashboard] <br /> |-<br /> ! [[#Brand dashboard | Brand dashboard]] <br /> | Integrated market information for a brand || Consumer products company || Brand Manager || [http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf Brand dashboard] <br /> |-<br /> ! [[#Collaboration services | Collaboration services]]<br /> | Multi-way interaction platform for research, marketing and manufacturing groups || Medium and large companies || Knowledge worker ||[http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Interactive reports] <br /> |-<br /> ! [[#Intellectual asset management services | Intellectual asset management services]]<br /> | Comprehensive overview of all your and your competition's IP || Medium and large companies || Patent counsel || [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IP asset management] <br /> |-<br /> ! [[#Technology trends research | Technology trends research]]<br /> | Monitor technology, IP and market trends || Medium and large companies || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf Technology trends report] <br /> |}<br /> <br /> <br /> == Questions Dolcera answers ==<br /> We help you answer questions such as:<br /> {| border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; align=&quot;center&quot; valign=&quot;top&quot;<br /> |-<br /> | <br /> * '''What’s hot'''<br /> ** What technology/approaches are the most promising?<br /> ** What technology/approaches have already been tried?<br /> ** What can I license?<br /> ** Is any empirical data available?<br /> * '''Where should I focus my R&amp;D investment'''<br /> ** Where’s the ‘white space’ for me to play in?<br /> * '''Any hints for research'''<br /> ** Are there any combinations I could develop?<br /> | <br /> * '''What should I do in this geography'''<br /> ** What are my competitors up to in this geography?<br /> ** What are my strengths/ weaknesses here?<br /> * '''What’s my competition up to'''<br /> ** What’s my top competitor investing in?<br /> ** Are there any loopholes in their strategy?<br /> ** Will a competitor emerge from nowhere and surprise me?<br /> ** What are the crowded areas?<br /> * '''How do I play defense'''<br /> ** What should my blocking/reactive strategies be?<br /> |}<br /> <br /> == Dolcera Expertise ==<br /> The Dolcera team has expertise in:<br /> * Technology analysis in the areas of chemistry, biotechnology, computer software, electronics, communication and mechanical engineering.<br /> * Market research - primary and secondary - across multiple industries <br /> * Information integration for large sets of structured and unstructured data<br /> * Collaboration tools and technology including wikis, blogs and Web 2.0</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Dolcera_Offerings&diff=1848 2006-06-30T10:39:22Z

<p>67.180.226.207: /* Dolcera for Knowledge Managers */</p> <hr /> <div>__NOTOC__<br /> == Dolcera for your organization: Technology, IP and Market Research ==<br /> Dolcera's mission is to provides information integration and outsourced research services for decision support. Our services are targeted towards multiple types of '''knowledge workers''' within organizations including:<br /> # Researchers, engineers and technologists<br /> # Patent counsel and attorneys<br /> # Knowledge managers<br /> # Marketers and brand managers<br /> # Senior executives and strategists<br /> === Dolcera for Researchers ===<br /> Dolcera works with researchers, engineers and technologists, and provides them with very high-quality technology and market information through our '''[[#Technology reports | technology reports]]'''. Our technical team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> === Dolcera for Patent Counsel and Attorneys ===<br /> Dolcera provides the intellectual property (IP) teams with a variety of services including:<br /> * Prior art, invalidation and infringement searches ([[#IPMaps |Dolcera IPMaps]])<br /> * Technical writing and patent drafting<br /> * [[#Technology reports | Technology reports]]<br /> * [[#Intellectual asset management services | IP asset management services]]<br /> <br /> === Dolcera for Knowledge Managers ===<br /> Knowledge managers are faced with a rapidly changing environment that includes a plethora of new tools (blogs, wikis, the semantic web etc.) and many challenges to go with them (e.g. taxonomy organization). Dolcera provides a range of '''[[#Collaboration services |collaboration services]]''' for managers of knowledge-driven organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup and management<br /> * Taxonomy design and updates for large taxonomies<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> === Dolcera for Brand Managers ===<br /> The '''[[#Brand dashboard |brand manager dashboard]]''' is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard:<br /> # Identifies the impact of global and local events on client's and competitor's brands,<br /> # Brings together data from a variety of data sources, and<br /> # Includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> === Dolcera for Strategists and Executives ===<br /> Executives and strategists use the integrated '''[[#Executive dashboard|executive dashboards]]''' to obtain a comprehensive overview of market, research and IP trends. Other services from Dolcera include:<br /> # [[#Business plan|Business plan development]]<br /> # [[#Timelines|Timelines]]<br /> # [[#Technology trends research|Technology trends research]]<br /> <br /> Here is a list of Dolcera services for various roles within an organization:<br /> <br /> {| class=&quot;wikitable&quot; style=&quot;font-size:120%&quot; border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; <br /> |- style=&quot;background:lightgrey&quot;<br /> ! Offering !! Goal !! Client !! Role !! Demo<br /> |-<br /> ! [[#Technology reports| Technology reports]] <br /> | 360-degree view of technology and market data || Technology company || Researcher || [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV report] <br /> |-<br /> ! [[#IPMaps | IPMaps]] <br /> | Comprehensive view of a particular research area || Law firms, corporations || Researcher || [http://www.dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Satellite Antenna IPMap] <br /> |-<br /> ! [[#Timelines | Timelines]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Business plans | Business plans]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Executive dashboard| Executive dashboard]] <br /> | Up-to-date snapshot of market+competitive data || Large corporation || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID dashboard] <br /> |-<br /> ! [[#Brand dashboard | Brand dashboard]] <br /> | Integrated market information for a brand || Consumer products company || Brand Manager || [http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf Brand dashboard] <br /> |-<br /> ! [[#Collaboration services | Collaboration services]]<br /> | Multi-way interaction platform for research, marketing and manufacturing groups || Medium and large companies || Knowledge worker ||[http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Interactive reports] <br /> |-<br /> ! [[#Intellectual asset management services | Intellectual asset management services]]<br /> | Comprehensive overview of all your and your competition's IP || Medium and large companies || Patent counsel || [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IP asset management] <br /> |-<br /> ! [[#Technology trends research | Technology trends research]]<br /> | Monitor technology, IP and market trends || Medium and large companies || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf Technology trends report] <br /> |}<br /> &lt;div id=&quot;Technology reports&quot;&gt;<br /> <br /> == Technology reports ==<br /> Dolcera team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> The unique aspects of Dolcera's technology reports are:<br /> * High quality of technology and market analysis,<br /> * Interactive development in partnership with client, and<br /> * Continuous updates <br /> <br /> [[Image:report_sample.jpg|thumb|500px|center|[http://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss Alopecia report]]]<br /> <br /> ==== Case study: Technology reports ====<br /> {{CaseStudy<br /> | topic = Technology reports<br /> | client = A large medical device company<br /> | goal = Create a technology report on one of the newest types of cardiac devices. Integrate data from a variety of data sources.<br /> | duration = Intial preparation - 4 weeks<br /> | result = The Dolcera report was shared between the research, marketing and legal groups within the client corporation. Dolcera also provides monthly updates for this report.<br /> | customer_savings = Approximately 1/8th of the cost <br /> | dolcera_advantage = Multi-disciplinary data integration, rapid results, low costs<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System Hybrid Electric Vehicle report]<br /> | quote = We can collaborate much more easily now.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;IPMaps&quot;&gt;<br /> <br /> == IPMaps ==<br /> Dolcera IPMaps present the comprehensive view of intellectual property in a particular area. Prepared by highly-trained technical analysts, Dolcera IPMaps are:<br /> * Comprehensive<br /> * Interactive<br /> * Visually clear-cut<br /> * Database-driven<br /> <br /> [[Image:Satellite_Antenna_IPMap.jpg|thumb|500px|center|[http://www.dolcera.com/ipmapdemo/satellite_antenna/impamp.html Satellite Antenna IPMap]]]<br /> ==== Case study: IPMaps ====<br /> {{CaseStudy<br /> | topic = IPMaps<br /> | client = A Fortune 500 software company<br /> | goal = Provide an overview of the company's patent portfolio in a key technology area.<br /> | duration = 2 weeks<br /> | result = The Dolcera IPMap integrated patent and competitive information from a variety of sources in one 'snapshot' IPMap that was used by the client for validating the market space and their own research strength.<br /> | customer_savings = Approximately 1/5th of the cost <br /> | dolcera_advantage = Data integration, technology expertise, speed, low costs<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/rfid/ipmap.html RFID IPMap], [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Hair loss IPMap], [http://www.dolcera.com/ipmapdemo/multimodal_apps/ipmap.html Multimodal applications IPMap]<br /> | quote = You showed us how small this market is. We would not have entered this market if we had this information in advance.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Timelines&quot;&gt;<br /> == Timelines ==<br /> Certain fields of research progress at bewildering speeds. It is often impossible for researchers, technology experts and executives alike to keep track of the developments. Dolcera timelines are exactly what their name implies: interactive visual maps that show the development of a field over the course of time. Our timelines are used for a variety of purposes including:<br /> * Understanding the development of a field of science/technology<br /> * Determining the contributions of individuals/companies to <br /> * Juxtaposing market and technology developments<br /> <br /> [[Image:timeline_sample_2.jpg|thumb|500px|center|Sample timeline]]<br /> ==== Case study: Timelines ====<br /> {{CaseStudy<br /> | topic = Timelines<br /> | client = A major N. American smartphone manufacturer<br /> | goal = Determine inventorship of some of the most important cellular telephony standards by analyzing patent, standard and market data.<br /> | duration = 4 weeks<br /> | result = Dolcera timelines, based on research through several gigabytes of standards meetings minutes, specifications and patents, allowed the client to negotiate with their competitors.<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Powerful search tools, data integration from disparate sources, succinct presentation<br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Sample timeline]<br /> | quote = I did not even have to lift a finger to understand the information... I used your presentation for my company's Board (of Directors).<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Business plans&quot;&gt;<br /> <br /> == Business plans ==<br /> Dolcera works in partnership with research and development groups within companies to help them understand the business opportunities for their research. We develop full-strength business plans with:<br /> * Commercialization possibilities for research<br /> * Competitive landscape<br /> * SWOT Analysis: Strengths, Weaknesses, Opportunities, Threats<br /> <br /> [[Image:swot_sample.jpg|thumb|250px|center|SWOT Analysis]]<br /> ==== Case study: Business plans ====<br /> {{CaseStudy<br /> | topic = Business plans<br /> | client = A global software company<br /> | goal = Create business case for a research project with several patent applications<br /> | duration = 6 weeks<br /> | result = Complete business plan including market research, financial plan, competitive analysis, product positioning, product and need characteristics<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Strong technology and business expertise to help researchers shorter innovation cycle<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = Dolcera is an integral part of our research commercialization strategy.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executive dashboard&quot;&gt;<br /> <br /> == Executive dashboard ==<br /> The Dolcera executive IP dashboard provides an integrated view of all the key performance indicators for your organization's intellectual property, including:<br /> * Patent filings<br /> * Patent licensing opportunities<br /> * Patent threats<br /> * Competitive position<br /> * Key IP performance indicators<br /> <br /> The interactive executive IP dashboard allows users to perform their own what-if analysis. Behind the scenes, the Dolcera team performs extensive research and market+competitive analysis to drive the executive dashboard and keep it up-to-date.<br /> <br /> &lt;gflash&gt;600 600 http://dolcera.com/ipmapdemo/rfid_model.swf&lt;/gflash&gt;<br /> <br /> ==== Case study: Executive dashboard ====<br /> {{CaseStudy<br /> | topic = Executive dashboard<br /> | client = A US medical device major<br /> | goal = Provide a central point of entry for all corporate IP performance indicators<br /> | duration = Ongoing<br /> | result = All patent information in one spot, and shared by all stakeholders within the organization.<br /> | customer_savings = Greater overall visibility improves response time considerably<br /> | dolcera_advantage = Correlating market movements with IP information and technology trends<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/alopecia_model.swf Consumer products dashboard], [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID Dashboard]<br /> | quote = The dashboard helps our team think strategically.<br /> }}<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Brand dashboard&quot;&gt;<br /> == Brand dashboard ==<br /> The brand manager dashboard is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard identifies the impact of global and local events on client's and competitor's brands. It brings together data from a variety of data sources. It also includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> &lt;gflash&gt;600 600 http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf&lt;/gflash&gt;<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Collaboration services&quot;&gt;<br /> <br /> == Collaboration services ==<br /> Dolcera provides a range of collaboration services for large organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup<br /> * Taxonomy design and updates<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> [[Image:taxonomy.jpg|thumb|300px|center|Dolcera taxonomy tool]]<br /> <br /> ==== Case study: Collaboration services ====<br /> {{CaseStudy<br /> | topic = Collaboration services<br /> | client = Large pharmaceutical company<br /> | goal = Provide a central Human Resources forms and document system for the corporate intranet.<br /> | duration = 2 months<br /> | result = We prepared the taxonomy and classification system for all documents and classified the documents initially. We also trained clients to update the documents on an ongoing basis.<br /> | customer_savings = Approximately $300,000 for the project<br /> | dolcera_advantage = Best-in-class technology and processes, ably supported by our technical team in India <br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IPMap]<br /> | quote = Our goal is to be a smarter organization, and Dolcera helped us achieve it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Intellectual asset management services&quot;&gt;<br /> == Intellectual asset management services==<br /> Dolcera takes medium- to large-sized patent portfolios and:<br /> # Creates a taxonomy to organize the patents<br /> # Organizes the patents inside the taxonomy <br /> # Identify and juxtapose the key competitive patent and non-patent documents<br /> # Identify products and 'virtual products' related to different sets of patents<br /> # Highlight the key strengths, weaknesses, opportunities and threats<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Technology trends research&quot;&gt;<br /> == Technology trends research ==<br /> Technology changes rapidly and it is often difficult to keep track of all the trends swirling on the Internet, all the ideas bubbling in academia, and the range of innovations you and your competitors are working on. Dolcera provides a sophisticated service to track technology trends, juxtaposing academic research, market data and patent filings information worldwide. <br /> <br /> [[Image:future_trends.jpg|thumb|400px|center|RFID technology trends]]<br /> <br /> ==== Case study: Technology trends research ====<br /> {{CaseStudy<br /> | topic = Technology trends research<br /> | client = Major technology company<br /> | goal = Provide an overview of technology directions of an important technology topic.<br /> | duration = 2 months<br /> | result = We identified the key technology trends, the patent information worldwide and provided predictions for the 'next big thing'<br /> | customer_savings = Potentially millions, with timely positioning of new offerings<br /> | dolcera_advantage = Constant monitoring of technology trends<br /> | sample_links = [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = We are swamped with information and are unable to digest it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> <br /> == Questions Dolcera answers ==<br /> We help you answer questions such as:<br /> {| border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; align=&quot;center&quot; valign=&quot;top&quot;<br /> |-<br /> | <br /> * '''What’s hot'''<br /> ** What technology/approaches are the most promising?<br /> ** What technology/approaches have already been tried?<br /> ** What can I license?<br /> ** Is any empirical data available?<br /> * '''Where should I focus my R&amp;D investment'''<br /> ** Where’s the ‘white space’ for me to play in?<br /> * '''Any hints for research'''<br /> ** Are there any combinations I could develop?<br /> | <br /> * '''What should I do in this geography'''<br /> ** What are my competitors up to in this geography?<br /> ** What are my strengths/ weaknesses here?<br /> * '''What’s my competition up to'''<br /> ** What’s my top competitor investing in?<br /> ** Are there any loopholes in their strategy?<br /> ** Will a competitor emerge from nowhere and surprise me?<br /> ** What are the crowded areas?<br /> * '''How do I play defense'''<br /> ** What should my blocking/reactive strategies be?<br /> |}<br /> <br /> == Dolcera Expertise ==<br /> The Dolcera team has expertise in:<br /> * Technology analysis in the areas of chemistry, biotechnology, computer software, electronics, communication and mechanical engineering.<br /> * Market research - primary and secondary - across multiple industries <br /> * Information integration for large sets of structured and unstructured data<br /> * Collaboration tools and technology including wikis, blogs and Web 2.0</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Dolcera_Offerings&diff=1847 2006-06-30T10:38:37Z

<p>67.180.226.207: </p> <hr /> <div>__NOTOC__<br /> == Dolcera for your organization: Technology, IP and Market Research ==<br /> Dolcera's mission is to provides information integration and outsourced research services for decision support. Our services are targeted towards multiple types of '''knowledge workers''' within organizations including:<br /> # Researchers, engineers and technologists<br /> # Patent counsel and attorneys<br /> # Knowledge managers<br /> # Marketers and brand managers<br /> # Senior executives and strategists<br /> === Dolcera for Researchers ===<br /> Dolcera works with researchers, engineers and technologists, and provides them with very high-quality technology and market information through our '''[[#Technology reports | technology reports]]'''. Our technical team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> === Dolcera for Patent Counsel and Attorneys ===<br /> Dolcera provides the intellectual property (IP) teams with a variety of services including:<br /> * Prior art, invalidation and infringement searches ([[#IPMaps |Dolcera IPMaps]])<br /> * Technical writing and patent drafting<br /> * [[#Technology reports | Technology reports]]<br /> * [[#Intellectual asset management services | IP asset management services]]<br /> <br /> === Dolcera for Knowledge Managers ===<br /> Knowledge managers are faced with a rapidly changing environment that includes a plethora of new tools (blogs, wikis, the semantic web etc.) and many challenges to go with them. Dolcera provides a range of '''[[#Collaboration services |collaboration services]]''' for managers of knowledge-driven organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup and management<br /> * Taxonomy design and updates for large taxonomies<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> === Dolcera for Brand Managers ===<br /> The '''[[#Brand dashboard |brand manager dashboard]]''' is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard:<br /> # Identifies the impact of global and local events on client's and competitor's brands,<br /> # Brings together data from a variety of data sources, and<br /> # Includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> === Dolcera for Strategists and Executives ===<br /> Executives and strategists use the integrated '''[[#Executive dashboard|executive dashboards]]''' to obtain a comprehensive overview of market, research and IP trends. Other services from Dolcera include:<br /> # [[#Business plan|Business plan development]]<br /> # [[#Timelines|Timelines]]<br /> # [[#Technology trends research|Technology trends research]]<br /> <br /> Here is a list of Dolcera services for various roles within an organization:<br /> <br /> {| class=&quot;wikitable&quot; style=&quot;font-size:120%&quot; border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; <br /> |- style=&quot;background:lightgrey&quot;<br /> ! Offering !! Goal !! Client !! Role !! Demo<br /> |-<br /> ! [[#Technology reports| Technology reports]] <br /> | 360-degree view of technology and market data || Technology company || Researcher || [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV report] <br /> |-<br /> ! [[#IPMaps | IPMaps]] <br /> | Comprehensive view of a particular research area || Law firms, corporations || Researcher || [http://www.dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Satellite Antenna IPMap] <br /> |-<br /> ! [[#Timelines | Timelines]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Business plans | Business plans]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Executive dashboard| Executive dashboard]] <br /> | Up-to-date snapshot of market+competitive data || Large corporation || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID dashboard] <br /> |-<br /> ! [[#Brand dashboard | Brand dashboard]] <br /> | Integrated market information for a brand || Consumer products company || Brand Manager || [http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf Brand dashboard] <br /> |-<br /> ! [[#Collaboration services | Collaboration services]]<br /> | Multi-way interaction platform for research, marketing and manufacturing groups || Medium and large companies || Knowledge worker ||[http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Interactive reports] <br /> |-<br /> ! [[#Intellectual asset management services | Intellectual asset management services]]<br /> | Comprehensive overview of all your and your competition's IP || Medium and large companies || Patent counsel || [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IP asset management] <br /> |-<br /> ! [[#Technology trends research | Technology trends research]]<br /> | Monitor technology, IP and market trends || Medium and large companies || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf Technology trends report] <br /> |}<br /> &lt;div id=&quot;Technology reports&quot;&gt;<br /> <br /> == Technology reports ==<br /> Dolcera team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> The unique aspects of Dolcera's technology reports are:<br /> * High quality of technology and market analysis,<br /> * Interactive development in partnership with client, and<br /> * Continuous updates <br /> <br /> [[Image:report_sample.jpg|thumb|500px|center|[http://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss Alopecia report]]]<br /> <br /> ==== Case study: Technology reports ====<br /> {{CaseStudy<br /> | topic = Technology reports<br /> | client = A large medical device company<br /> | goal = Create a technology report on one of the newest types of cardiac devices. Integrate data from a variety of data sources.<br /> | duration = Intial preparation - 4 weeks<br /> | result = The Dolcera report was shared between the research, marketing and legal groups within the client corporation. Dolcera also provides monthly updates for this report.<br /> | customer_savings = Approximately 1/8th of the cost <br /> | dolcera_advantage = Multi-disciplinary data integration, rapid results, low costs<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System Hybrid Electric Vehicle report]<br /> | quote = We can collaborate much more easily now.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;IPMaps&quot;&gt;<br /> <br /> == IPMaps ==<br /> Dolcera IPMaps present the comprehensive view of intellectual property in a particular area. Prepared by highly-trained technical analysts, Dolcera IPMaps are:<br /> * Comprehensive<br /> * Interactive<br /> * Visually clear-cut<br /> * Database-driven<br /> <br /> [[Image:Satellite_Antenna_IPMap.jpg|thumb|500px|center|[http://www.dolcera.com/ipmapdemo/satellite_antenna/impamp.html Satellite Antenna IPMap]]]<br /> ==== Case study: IPMaps ====<br /> {{CaseStudy<br /> | topic = IPMaps<br /> | client = A Fortune 500 software company<br /> | goal = Provide an overview of the company's patent portfolio in a key technology area.<br /> | duration = 2 weeks<br /> | result = The Dolcera IPMap integrated patent and competitive information from a variety of sources in one 'snapshot' IPMap that was used by the client for validating the market space and their own research strength.<br /> | customer_savings = Approximately 1/5th of the cost <br /> | dolcera_advantage = Data integration, technology expertise, speed, low costs<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/rfid/ipmap.html RFID IPMap], [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Hair loss IPMap], [http://www.dolcera.com/ipmapdemo/multimodal_apps/ipmap.html Multimodal applications IPMap]<br /> | quote = You showed us how small this market is. We would not have entered this market if we had this information in advance.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Timelines&quot;&gt;<br /> == Timelines ==<br /> Certain fields of research progress at bewildering speeds. It is often impossible for researchers, technology experts and executives alike to keep track of the developments. Dolcera timelines are exactly what their name implies: interactive visual maps that show the development of a field over the course of time. Our timelines are used for a variety of purposes including:<br /> * Understanding the development of a field of science/technology<br /> * Determining the contributions of individuals/companies to <br /> * Juxtaposing market and technology developments<br /> <br /> [[Image:timeline_sample_2.jpg|thumb|500px|center|Sample timeline]]<br /> ==== Case study: Timelines ====<br /> {{CaseStudy<br /> | topic = Timelines<br /> | client = A major N. American smartphone manufacturer<br /> | goal = Determine inventorship of some of the most important cellular telephony standards by analyzing patent, standard and market data.<br /> | duration = 4 weeks<br /> | result = Dolcera timelines, based on research through several gigabytes of standards meetings minutes, specifications and patents, allowed the client to negotiate with their competitors.<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Powerful search tools, data integration from disparate sources, succinct presentation<br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Sample timeline]<br /> | quote = I did not even have to lift a finger to understand the information... I used your presentation for my company's Board (of Directors).<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Business plans&quot;&gt;<br /> <br /> == Business plans ==<br /> Dolcera works in partnership with research and development groups within companies to help them understand the business opportunities for their research. We develop full-strength business plans with:<br /> * Commercialization possibilities for research<br /> * Competitive landscape<br /> * SWOT Analysis: Strengths, Weaknesses, Opportunities, Threats<br /> <br /> [[Image:swot_sample.jpg|thumb|250px|center|SWOT Analysis]]<br /> ==== Case study: Business plans ====<br /> {{CaseStudy<br /> | topic = Business plans<br /> | client = A global software company<br /> | goal = Create business case for a research project with several patent applications<br /> | duration = 6 weeks<br /> | result = Complete business plan including market research, financial plan, competitive analysis, product positioning, product and need characteristics<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Strong technology and business expertise to help researchers shorter innovation cycle<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = Dolcera is an integral part of our research commercialization strategy.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executive dashboard&quot;&gt;<br /> <br /> == Executive dashboard ==<br /> The Dolcera executive IP dashboard provides an integrated view of all the key performance indicators for your organization's intellectual property, including:<br /> * Patent filings<br /> * Patent licensing opportunities<br /> * Patent threats<br /> * Competitive position<br /> * Key IP performance indicators<br /> <br /> The interactive executive IP dashboard allows users to perform their own what-if analysis. Behind the scenes, the Dolcera team performs extensive research and market+competitive analysis to drive the executive dashboard and keep it up-to-date.<br /> <br /> &lt;gflash&gt;600 600 http://dolcera.com/ipmapdemo/rfid_model.swf&lt;/gflash&gt;<br /> <br /> ==== Case study: Executive dashboard ====<br /> {{CaseStudy<br /> | topic = Executive dashboard<br /> | client = A US medical device major<br /> | goal = Provide a central point of entry for all corporate IP performance indicators<br /> | duration = Ongoing<br /> | result = All patent information in one spot, and shared by all stakeholders within the organization.<br /> | customer_savings = Greater overall visibility improves response time considerably<br /> | dolcera_advantage = Correlating market movements with IP information and technology trends<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/alopecia_model.swf Consumer products dashboard], [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID Dashboard]<br /> | quote = The dashboard helps our team think strategically.<br /> }}<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Brand dashboard&quot;&gt;<br /> == Brand dashboard ==<br /> The brand manager dashboard is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard identifies the impact of global and local events on client's and competitor's brands. It brings together data from a variety of data sources. It also includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> &lt;gflash&gt;600 600 http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf&lt;/gflash&gt;<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Collaboration services&quot;&gt;<br /> <br /> == Collaboration services ==<br /> Dolcera provides a range of collaboration services for large organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup<br /> * Taxonomy design and updates<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> [[Image:taxonomy.jpg|thumb|300px|center|Dolcera taxonomy tool]]<br /> <br /> ==== Case study: Collaboration services ====<br /> {{CaseStudy<br /> | topic = Collaboration services<br /> | client = Large pharmaceutical company<br /> | goal = Provide a central Human Resources forms and document system for the corporate intranet.<br /> | duration = 2 months<br /> | result = We prepared the taxonomy and classification system for all documents and classified the documents initially. We also trained clients to update the documents on an ongoing basis.<br /> | customer_savings = Approximately $300,000 for the project<br /> | dolcera_advantage = Best-in-class technology and processes, ably supported by our technical team in India <br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IPMap]<br /> | quote = Our goal is to be a smarter organization, and Dolcera helped us achieve it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Intellectual asset management services&quot;&gt;<br /> == Intellectual asset management services==<br /> Dolcera takes medium- to large-sized patent portfolios and:<br /> # Creates a taxonomy to organize the patents<br /> # Organizes the patents inside the taxonomy <br /> # Identify and juxtapose the key competitive patent and non-patent documents<br /> # Identify products and 'virtual products' related to different sets of patents<br /> # Highlight the key strengths, weaknesses, opportunities and threats<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Technology trends research&quot;&gt;<br /> == Technology trends research ==<br /> Technology changes rapidly and it is often difficult to keep track of all the trends swirling on the Internet, all the ideas bubbling in academia, and the range of innovations you and your competitors are working on. Dolcera provides a sophisticated service to track technology trends, juxtaposing academic research, market data and patent filings information worldwide. <br /> <br /> [[Image:future_trends.jpg|thumb|400px|center|RFID technology trends]]<br /> <br /> ==== Case study: Technology trends research ====<br /> {{CaseStudy<br /> | topic = Technology trends research<br /> | client = Major technology company<br /> | goal = Provide an overview of technology directions of an important technology topic.<br /> | duration = 2 months<br /> | result = We identified the key technology trends, the patent information worldwide and provided predictions for the 'next big thing'<br /> | customer_savings = Potentially millions, with timely positioning of new offerings<br /> | dolcera_advantage = Constant monitoring of technology trends<br /> | sample_links = [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = We are swamped with information and are unable to digest it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> <br /> == Questions Dolcera answers ==<br /> We help you answer questions such as:<br /> {| border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; align=&quot;center&quot; valign=&quot;top&quot;<br /> |-<br /> | <br /> * '''What’s hot'''<br /> ** What technology/approaches are the most promising?<br /> ** What technology/approaches have already been tried?<br /> ** What can I license?<br /> ** Is any empirical data available?<br /> * '''Where should I focus my R&amp;D investment'''<br /> ** Where’s the ‘white space’ for me to play in?<br /> * '''Any hints for research'''<br /> ** Are there any combinations I could develop?<br /> | <br /> * '''What should I do in this geography'''<br /> ** What are my competitors up to in this geography?<br /> ** What are my strengths/ weaknesses here?<br /> * '''What’s my competition up to'''<br /> ** What’s my top competitor investing in?<br /> ** Are there any loopholes in their strategy?<br /> ** Will a competitor emerge from nowhere and surprise me?<br /> ** What are the crowded areas?<br /> * '''How do I play defense'''<br /> ** What should my blocking/reactive strategies be?<br /> |}<br /> <br /> == Dolcera Expertise ==<br /> The Dolcera team has expertise in:<br /> * Technology analysis in the areas of chemistry, biotechnology, computer software, electronics, communication and mechanical engineering.<br /> * Market research - primary and secondary - across multiple industries <br /> * Information integration for large sets of structured and unstructured data<br /> * Collaboration tools and technology including wikis, blogs and Web 2.0</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Dolcera_Offerings&diff=1846 2006-06-30T09:34:06Z

<p>67.180.226.207: </p> <hr /> <div>Dolcera's mission is to provides information integration and outsourced research services for decision support. Our services are targeted towards multiple types of '''knowledge workers''' within organizations including:<br /> * senior executives and strategists<br /> * researchers, engineers and technologists<br /> * marketers and brand managers<br /> * attorneys<br /> <br /> The Dolcera team has expertise in:<br /> * Technology analysis in the areas of chemistry, biotechnology, computer software, electronics, communication and mechanical engineering.<br /> * Market research - primary and secondary - across multiple industries <br /> * Information integration for large sets of structured and unstructured data<br /> * Collaboration tools and technology including wikis, blogs and Web 2.0<br /> <br /> Here is a list of Dolcera services for various roles within an organization:<br /> <br /> {| class=&quot;wikitable&quot; style=&quot;font-size:120%&quot; border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; <br /> |- style=&quot;background:lightgrey&quot;<br /> ! Offering !! Goal !! Client !! Role !! Demo<br /> |-<br /> ! [[#Technology reports| Technology reports]] <br /> | 360-degree view of technology and market data || Technology company || Researcher || [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV report] <br /> |-<br /> ! [[#IPMaps | IPMaps]] <br /> | Comprehensive view of a particular research area || Law firms, corporations || Researcher || [http://www.dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Satellite Antenna IPMap] <br /> |-<br /> ! [[#Timelines | Timelines]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Business plans | Business plans]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Executive dashboard| Executive dashboard]] <br /> | Up-to-date snapshot of market+competitive data || Large corporation || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID dashboard] <br /> |-<br /> ! [[#Brand dashboard | Brand dashboard]] <br /> | Integrated market information for a brand || Consumer products company || Brand Manager || [http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf Brand dashboard] <br /> |-<br /> ! [[#Collaboration services | Collaboration services]]<br /> | Multi-way interaction platform for research, marketing and manufacturing groups || Medium and large companies || Knowledge worker ||[http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Interactive reports] <br /> |-<br /> ! [[#Intellectual asset management services | Intellectual asset management services]]<br /> | Comprehensive overview of all your and your competition's IP || Medium and large companies || Patent counsel || [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IP asset management] <br /> |-<br /> ! [[#Technology trends research | Technology trends research]]<br /> | Monitor technology, IP and market trends || Medium and large companies || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf Technology trends report] <br /> |}<br /> __NOTOC__<br /> &lt;div id=&quot;Technology reports&quot;&gt;<br /> <br /> == Technology reports ==<br /> Dolcera team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> The unique aspects of Dolcera's technology reports are:<br /> * High quality of technology and market analysis,<br /> * Interactive development in partnership with client, and<br /> * Continuous updates <br /> <br /> [[Image:report_sample.jpg|thumb|500px|center|[http://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss Alopecia report]]]<br /> <br /> ==== Case study: Technology reports ====<br /> {{CaseStudy<br /> | topic = Technology reports<br /> | client = A large medical device company<br /> | goal = Create a technology report on one of the newest types of cardiac devices. Integrate data from a variety of data sources.<br /> | duration = Intial preparation - 4 weeks<br /> | result = The Dolcera report was shared between the research, marketing and legal groups within the client corporation. Dolcera also provides monthly updates for this report.<br /> | customer_savings = Approximately 1/8th of the cost <br /> | dolcera_advantage = Multi-disciplinary data integration, rapid results, low costs<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System Hybrid Electric Vehicle report]<br /> | quote = We can collaborate much more easily now.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;IPMaps&quot;&gt;<br /> <br /> == IPMaps ==<br /> Dolcera IPMaps present the comprehensive view of intellectual property in a particular area. Prepared by highly-trained technical analysts, Dolcera IPMaps are:<br /> * Comprehensive<br /> * Interactive<br /> * Visually clear-cut<br /> * Database-driven<br /> <br /> [[Image:Satellite_Antenna_IPMap.jpg|thumb|500px|center|[http://www.dolcera.com/ipmapdemo/satellite_antenna/impamp.html Satellite Antenna IPMap]]]<br /> ==== Case study: IPMaps ====<br /> {{CaseStudy<br /> | topic = IPMaps<br /> | client = A Fortune 500 software company<br /> | goal = Provide an overview of the company's patent portfolio in a key technology area.<br /> | duration = 2 weeks<br /> | result = The Dolcera IPMap integrated patent and competitive information from a variety of sources in one 'snapshot' IPMap that was used by the client for validating the market space and their own research strength.<br /> | customer_savings = Approximately 1/5th of the cost <br /> | dolcera_advantage = Data integration, technology expertise, speed, low costs<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/rfid/ipmap.html RFID IPMap], [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Hair loss IPMap], [http://www.dolcera.com/ipmapdemo/multimodal_apps/ipmap.html Multimodal applications IPMap]<br /> | quote = You showed us how small this market is. We would not have entered this market if we had this information in advance.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Timelines&quot;&gt;<br /> == Timelines ==<br /> Certain fields of research progress at bewildering speeds. It is often impossible for researchers, technology experts and executives alike to keep track of the developments. Dolcera timelines are exactly what their name implies: interactive visual maps that show the development of a field over the course of time. Our timelines are used for a variety of purposes including:<br /> * Understanding the development of a field of science/technology<br /> * Determining the contributions of individuals/companies to <br /> * Juxtaposing market and technology developments<br /> <br /> [[Image:timeline_sample_2.jpg|thumb|500px|center|Sample timeline]]<br /> ==== Case study: Timelines ====<br /> {{CaseStudy<br /> | topic = Timelines<br /> | client = A major N. American smartphone manufacturer<br /> | goal = Determine inventorship of some of the most important cellular telephony standards by analyzing patent, standard and market data.<br /> | duration = 4 weeks<br /> | result = Dolcera timelines, based on research through several gigabytes of standards meetings minutes, specifications and patents, allowed the client to negotiate with their competitors.<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Powerful search tools, data integration from disparate sources, succinct presentation<br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Sample timeline]<br /> | quote = I did not even have to lift a finger to understand the information... I used your presentation for my company's Board (of Directors).<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Business plans&quot;&gt;<br /> <br /> == Business plans ==<br /> Dolcera works in partnership with research and development groups within companies to help them understand the business opportunities for their research. We develop full-strength business plans with:<br /> * Commercialization possibilities for research<br /> * Competitive landscape<br /> * SWOT Analysis: Strengths, Weaknesses, Opportunities, Threats<br /> <br /> [[Image:swot_sample.jpg|thumb|250px|center|SWOT Analysis]]<br /> ==== Case study: Business plans ====<br /> {{CaseStudy<br /> | topic = Business plans<br /> | client = A global software company<br /> | goal = Create business case for a research project with several patent applications<br /> | duration = 6 weeks<br /> | result = Complete business plan including market research, financial plan, competitive analysis, product positioning, product and need characteristics<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Strong technology and business expertise to help researchers shorter innovation cycle<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = Dolcera is an integral part of our research commercialization strategy.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executive dashboard&quot;&gt;<br /> <br /> == Executive dashboard ==<br /> The Dolcera executive IP dashboard provides an integrated view of all the key performance indicators for your organization's intellectual property, including:<br /> * Patent filings<br /> * Patent licensing opportunities<br /> * Patent threats<br /> * Competitive position<br /> * Key IP performance indicators<br /> <br /> The interactive executive IP dashboard allows users to perform their own what-if analysis. Behind the scenes, the Dolcera team performs extensive research and market+competitive analysis to drive the executive dashboard and keep it up-to-date.<br /> <br /> &lt;gflash&gt;600 600 http://dolcera.com/ipmapdemo/rfid_model.swf&lt;/gflash&gt;<br /> <br /> ==== Case study: Executive dashboard ====<br /> {{CaseStudy<br /> | topic = Executive dashboard<br /> | client = A US medical device major<br /> | goal = Provide a central point of entry for all corporate IP performance indicators<br /> | duration = Ongoing<br /> | result = All patent information in one spot, and shared by all stakeholders within the organization.<br /> | customer_savings = Greater overall visibility improves response time considerably<br /> | dolcera_advantage = Correlating market movements with IP information and technology trends<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/alopecia_model.swf Consumer products dashboard], [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID Dashboard]<br /> | quote = The dashboard helps our team think strategically.<br /> }}<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Brand dashboard&quot;&gt;<br /> == Brand dashboard ==<br /> The brand manager dashboard is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard identifies the impact of global and local events on client's and competitor's brands. It brings together data from a variety of data sources. It also includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> &lt;gflash&gt;600 600 http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf&lt;/gflash&gt;<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Collaboration services&quot;&gt;<br /> <br /> == Collaboration services ==<br /> Dolcera provides a range of collaboration services for large organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup<br /> * Taxonomy design and updates<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> [[Image:taxonomy.jpg|thumb|300px|center|Dolcera taxonomy tool]]<br /> <br /> ==== Case study: Collaboration services ====<br /> {{CaseStudy<br /> | topic = Collaboration services<br /> | client = Large pharmaceutical company<br /> | goal = Provide a central Human Resources forms and document system for the corporate intranet.<br /> | duration = 2 months<br /> | result = We prepared the taxonomy and classification system for all documents and classified the documents initially. We also trained clients to update the documents on an ongoing basis.<br /> | customer_savings = Approximately $300,000 for the project<br /> | dolcera_advantage = Best-in-class technology and processes, ably supported by our technical team in India <br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IPMap]<br /> | quote = Our goal is to be a smarter organization, and Dolcera helped us achieve it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> <br /> <br /> == Questions Dolcera answers ==<br /> We help you answer questions such as:<br /> {| border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; align=&quot;center&quot; valign=&quot;top&quot;<br /> |-<br /> | <br /> * '''What’s hot'''<br /> ** What technology/approaches are the most promising?<br /> ** What technology/approaches have already been tried?<br /> ** What can I license?<br /> ** Is any empirical data available?<br /> * '''Where should I focus my R&amp;D investment'''<br /> ** Where’s the ‘white space’ for me to play in?<br /> * '''Any hints for research'''<br /> ** Are there any combinations I could develop?<br /> | <br /> * '''What should I do in this geography'''<br /> ** What are my competitors up to in this geography?<br /> ** What are my strengths/ weaknesses here?<br /> * '''What’s my competition up to'''<br /> ** What’s my top competitor investing in?<br /> ** Are there any loopholes in their strategy?<br /> ** Will a competitor emerge from nowhere and surprise me?<br /> ** What are the crowded areas?<br /> * '''How do I play defense'''<br /> ** What should my blocking/reactive strategies be?<br /> |}</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Dolcera_Offerings&diff=1845 2006-06-30T08:54:50Z

<p>67.180.226.207: </p> <hr /> <div>Dolcera's mission is to provides information integration and outsourced research services for decision support. Our services are targeted towards multiple types of '''knowledge workers''' within organizations including:<br /> * senior executives and strategists<br /> * researchers, engineers and technologists<br /> * marketers and brand managers<br /> * attorneys<br /> <br /> The Dolcera team has expertise in:<br /> * Technology analysis in the areas of chemistry, biotechnology, computer software, electronics, communication and mechanical engineering.<br /> * Market research - primary and secondary - across multiple industries <br /> * Information integration for large sets of structured and unstructured data<br /> * Collaboration tools and technology including wikis, blogs and Web 2.0<br /> <br /> Here is a list of Dolcera services for various roles within an organization:<br /> <br /> {| class=&quot;wikitable&quot; style=&quot;font-size:120%&quot; border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; <br /> |- style=&quot;background:lightgrey&quot;<br /> ! Offering !! Goal !! Client !! Role !! Demo<br /> |-<br /> ! [[#Technology reports| Technology reports]] <br /> | 360-degree view of technology and market data || Technology company || Researcher || [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV report] <br /> |-<br /> ! [[#IPMaps | IPMaps]] <br /> | Comprehensive view of a particular research area || Law firms, corporations || Researcher || [http://www.dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Satellite Antenna IPMap] <br /> |-<br /> ! [[#Timelines | Timelines]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Business plans | Business plans]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Executive dashboard| Executive dashboard]] <br /> | Up-to-date snapshot of market+competitive data || Large corporation || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID dashboard] <br /> |-<br /> ! [[#Brand dashboard | Brand dashboard]] <br /> | Integrated market information for a brand || Consumer products company || Brand Manager || [http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf Brand dashboard] <br /> |-<br /> ! [[#Collaboration services | Collaboration services]]<br /> | Multi-way interaction platform for research, marketing and manufacturing groups || Medium and large companies || Knowledge worker ||[http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Interactive reports] <br /> |-<br /> ! [[#Intellectual asset management services | Intellectual asset management services]]<br /> | Comprehensive overview of all your and your competition's IP || Medium and large companies || Patent counsel || [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IP asset management] <br /> |}<br /> __NOTOC__<br /> &lt;div id=&quot;Technology reports&quot;&gt;<br /> <br /> == Technology reports ==<br /> Dolcera team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> The unique aspects of Dolcera's technology reports are:<br /> * High quality of technology and market analysis,<br /> * Interactive development in partnership with client, and<br /> * Continuous updates <br /> <br /> [[Image:report_sample.jpg|thumb|500px|center|[http://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss Alopecia report]]]<br /> <br /> ==== Case study: Technology reports ====<br /> {{CaseStudy<br /> | topic = Technology reports<br /> | client = A large medical device company<br /> | goal = Create a technology report on one of the newest types of cardiac devices. Integrate data from a variety of data sources.<br /> | duration = Intial preparation - 4 weeks<br /> | result = The Dolcera report was shared between the research, marketing and legal groups within the client corporation. Dolcera also provides monthly updates for this report.<br /> | customer_savings = Approximately 1/8th of the cost <br /> | dolcera_advantage = Multi-disciplinary data integration, rapid results, low costs<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System Hybrid Electric Vehicle report]<br /> | quote = We can collaborate much more easily now.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;IPMaps&quot;&gt;<br /> <br /> == IPMaps ==<br /> Dolcera IPMaps present the comprehensive view of intellectual property in a particular area. Prepared by highly-trained technical analysts, Dolcera IPMaps are:<br /> * Comprehensive<br /> * Interactive<br /> * Visually clear-cut<br /> * Database-driven<br /> <br /> [[Image:Satellite_Antenna_IPMap.jpg|thumb|500px|center|[http://www.dolcera.com/ipmapdemo/satellite_antenna/impamp.html Satellite Antenna IPMap]]]<br /> ==== Case study: IPMaps ====<br /> {{CaseStudy<br /> | topic = IPMaps<br /> | client = A Fortune 500 software company<br /> | goal = Provide an overview of the company's patent portfolio in a key technology area.<br /> | duration = 2 weeks<br /> | result = The Dolcera IPMap integrated patent and competitive information from a variety of sources in one 'snapshot' IPMap that was used by the client for validating the market space and their own research strength.<br /> | customer_savings = Approximately 1/5th of the cost <br /> | dolcera_advantage = Data integration, technology expertise, speed, low costs<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/rfid/ipmap.html RFID IPMap], [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Hair loss IPMap], [http://www.dolcera.com/ipmapdemo/multimodal_apps/ipmap.html Multimodal applications IPMap]<br /> | quote = You showed us how small this market is. We would not have entered this market if we had this information in advance.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Timelines&quot;&gt;<br /> == Timelines ==<br /> Certain fields of research progress at bewildering speeds. It is often impossible for researchers, technology experts and executives alike to keep track of the developments. Dolcera timelines are exactly what their name implies: interactive visual maps that show the development of a field over the course of time. Our timelines are used for a variety of purposes including:<br /> * Understanding the development of a field of science/technology<br /> * Determining the contributions of individuals/companies to <br /> * Juxtaposing market and technology developments<br /> <br /> [[Image:timeline_sample_2.jpg|thumb|500px|center|Sample timeline]]<br /> ==== Case study: Timelines ====<br /> {{CaseStudy<br /> | topic = Timelines<br /> | client = A major N. American smartphone manufacturer<br /> | goal = Determine inventorship of some of the most important cellular telephony standards by analyzing patent, standard and market data.<br /> | duration = 4 weeks<br /> | result = Dolcera timelines, based on research through several gigabytes of standards meetings minutes, specifications and patents, allowed the client to negotiate with their competitors.<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Powerful search tools, data integration from disparate sources, succinct presentation<br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Sample timeline]<br /> | quote = I did not even have to lift a finger to understand the information... I used your presentation for my company's Board (of Directors).<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Business plans&quot;&gt;<br /> <br /> == Business plans ==<br /> Dolcera works in partnership with research and development groups within companies to help them understand the business opportunities for their research. We develop full-strength business plans with:<br /> * Commercialization possibilities for research<br /> * Competitive landscape<br /> * SWOT Analysis: Strengths, Weaknesses, Opportunities, Threats<br /> <br /> [[Image:swot_sample.jpg|thumb|250px|center|SWOT Analysis]]<br /> ==== Case study: Business plans ====<br /> {{CaseStudy<br /> | topic = Business plans<br /> | client = A global software company<br /> | goal = Create business case for a research project with several patent applications<br /> | duration = 6 weeks<br /> | result = Complete business plan including market research, financial plan, competitive analysis, product positioning, product and need characteristics<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Strong technology and business expertise to help researchers shorter innovation cycle<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = Dolcera is an integral part of our research commercialization strategy.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executive dashboard&quot;&gt;<br /> <br /> == Executive dashboard ==<br /> The Dolcera executive IP dashboard provides an integrated view of all the key performance indicators for your organization's intellectual property, including:<br /> * Patent filings<br /> * Patent licensing opportunities<br /> * Patent threats<br /> * Competitive position<br /> * Key IP performance indicators<br /> <br /> The interactive executive IP dashboard allows users to perform their own what-if analysis. Behind the scenes, the Dolcera team performs extensive research and market+competitive analysis to drive the executive dashboard and keep it up-to-date.<br /> <br /> &lt;gflash&gt;600 600 http://dolcera.com/ipmapdemo/rfid_model.swf&lt;/gflash&gt;<br /> <br /> ==== Case study: Executive dashboard ====<br /> {{CaseStudy<br /> | topic = Executive dashboard<br /> | client = A US medical device major<br /> | goal = Provide a central point of entry for all corporate IP performance indicators<br /> | duration = Ongoing<br /> | result = All patent information in one spot, and shared by all stakeholders within the organization.<br /> | customer_savings = Greater overall visibility improves response time considerably<br /> | dolcera_advantage = Correlating market movements with IP information and technology trends<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/alopecia_model.swf Consumer products dashboard], [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID Dashboard]<br /> | quote = The dashboard helps our team think strategically.<br /> }}<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Brand dashboard&quot;&gt;<br /> == Brand dashboard ==<br /> The brand manager dashboard is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard identifies the impact of global and local events on client's and competitor's brands. It brings together data from a variety of data sources. It also includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> &lt;gflash&gt;600 600 http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf&lt;/gflash&gt;<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Collaboration services&quot;&gt;<br /> <br /> == Collaboration services ==<br /> Dolcera provides a range of collaboration services for large organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup<br /> * Taxonomy design and updates<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> [[Image:taxonomy.jpg|thumb|300px|center|Dolcera taxonomy tool]]<br /> <br /> ==== Case study: Collaboration services ====<br /> {{CaseStudy<br /> | topic = Collaboration services<br /> | client = Large pharmaceutical company<br /> | goal = Provide a central Human Resources forms and document system for the corporate intranet.<br /> | duration = 2 months<br /> | result = We prepared the taxonomy and classification system for all documents and classified the documents initially. We also trained clients to update the documents on an ongoing basis.<br /> | customer_savings = Approximately $300,000 for the project<br /> | dolcera_advantage = Best-in-class technology and processes, ably supported by our technical team in India <br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IPMap]<br /> | quote = Our goal is to be a smarter organization, and Dolcera helped us achieve it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> <br /> <br /> == Questions Dolcera answers ==<br /> We help you answer questions such as:<br /> {| border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; align=&quot;center&quot; valign=&quot;top&quot;<br /> |-<br /> | <br /> * '''What’s hot'''<br /> ** What technology/approaches are the most promising?<br /> ** What technology/approaches have already been tried?<br /> ** What can I license?<br /> ** Is any empirical data available?<br /> * '''Where should I focus my R&amp;D investment'''<br /> ** Where’s the ‘white space’ for me to play in?<br /> * '''Any hints for research'''<br /> ** Are there any combinations I could develop?<br /> | <br /> * '''What should I do in this geography'''<br /> ** What are my competitors up to in this geography?<br /> ** What are my strengths/ weaknesses here?<br /> * '''What’s my competition up to'''<br /> ** What’s my top competitor investing in?<br /> ** Are there any loopholes in their strategy?<br /> ** Will a competitor emerge from nowhere and surprise me?<br /> ** What are the crowded areas?<br /> * '''How do I play defense'''<br /> ** What should my blocking/reactive strategies be?<br /> |}</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Dolcera_Offerings&diff=1844 2006-06-30T08:53:38Z

<p>67.180.226.207: </p> <hr /> <div>Dolcera's mission is to provides information integration and outsourced research services for decision support. Our services are targeted towards multiple types of '''knowledge workers''' within organizations including:<br /> * senior executives and strategists<br /> * researchers, engineers and technologists<br /> * marketers and brand managers<br /> * attorneys<br /> <br /> The Dolcera team has expertise in:<br /> * Technology analysis in the areas of chemistry, biotechnology, computer software, electronics, communication and mechanical engineering.<br /> * Market research - primary and secondary - across multiple industries <br /> * Information integration for large sets of structured and unstructured data<br /> * Collaboration tools and technology including wikis, blogs and Web 2.0<br /> <br /> Here is a list of Dolcera services for various roles within an organization:<br /> <br /> {| class=&quot;wikitable&quot; style=&quot;font-size:120%&quot; border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; <br /> |- style=&quot;background:lightgrey&quot;<br /> ! Offering !! Goal !! Client !! Role !! Demo<br /> |-<br /> ! [[#Technology reports| Technology reports]] <br /> | 360-degree view of technology and market data || Technology company || Researcher || [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV report] <br /> |-<br /> ! [[#IPMaps | IPMaps]] <br /> | Comprehensive view of a particular research area || Law firms, corporations || Researcher || [http://www.dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Satellite Antenna IPMap] <br /> |-<br /> ! [[#Timelines | Timelines]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Business plans | Business plans]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Executive dashboard| Executive dashboard]] <br /> | Up-to-date snapshot of market+competitive data || Large corporation || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID dashboard] <br /> |-<br /> ! [[#Brand dashboard | Brand dashboard]] <br /> | Integrated market information for a brand || Consumer products company || Brand Manager || [http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf Brand dashboard] <br /> |-<br /> ! [[#Collaboration services | Collaboration services]]<br /> | Multi-way interaction platform for research, marketing and manufacturing groups || Medium and large companies || Knowledge worker ||[http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Interactive reports] <br /> |-<br /> ! [[#Intellectual asset management services | Intellectual asset management services]]<br /> | Comprehensive overview of all your and your competition's IP || Medium and large companies || Patent counsel || [[http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IP asset management] <br /> |}<br /> __NOTOC__<br /> &lt;div id=&quot;Technology reports&quot;&gt;<br /> <br /> == Technology reports ==<br /> Dolcera team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> The unique aspects of Dolcera's technology reports are:<br /> * High quality of technology and market analysis,<br /> * Interactive development in partnership with client, and<br /> * Continuous updates <br /> <br /> [[Image:report_sample.jpg|thumb|500px|center|[http://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss Alopecia report]]]<br /> <br /> ==== Case study: Technology reports ====<br /> {{CaseStudy<br /> | topic = Technology reports<br /> | client = A large medical device company<br /> | goal = Create a technology report on one of the newest types of cardiac devices. Integrate data from a variety of data sources.<br /> | duration = Intial preparation - 4 weeks<br /> | result = The Dolcera report was shared between the research, marketing and legal groups within the client corporation. Dolcera also provides monthly updates for this report.<br /> | customer_savings = Approximately 1/8th of the cost <br /> | dolcera_advantage = Multi-disciplinary data integration, rapid results, low costs<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System Hybrid Electric Vehicle report]<br /> | quote = We can collaborate much more easily now.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;IPMaps&quot;&gt;<br /> <br /> == IPMaps ==<br /> Dolcera IPMaps present the comprehensive view of intellectual property in a particular area. Prepared by highly-trained technical analysts, Dolcera IPMaps are:<br /> * Comprehensive<br /> * Interactive<br /> * Visually clear-cut<br /> * Database-driven<br /> <br /> [[Image:Satellite_Antenna_IPMap.jpg|thumb|500px|center|[http://www.dolcera.com/ipmapdemo/satellite_antenna/impamp.html Satellite Antenna IPMap]]]<br /> ==== Case study: IPMaps ====<br /> {{CaseStudy<br /> | topic = IPMaps<br /> | client = A Fortune 500 software company<br /> | goal = Provide an overview of the company's patent portfolio in a key technology area.<br /> | duration = 2 weeks<br /> | result = The Dolcera IPMap integrated patent and competitive information from a variety of sources in one 'snapshot' IPMap that was used by the client for validating the market space and their own research strength.<br /> | customer_savings = Approximately 1/5th of the cost <br /> | dolcera_advantage = Data integration, technology expertise, speed, low costs<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/rfid/ipmap.html RFID IPMap], [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Hair loss IPMap], [http://www.dolcera.com/ipmapdemo/multimodal_apps/ipmap.html Multimodal applications IPMap]<br /> | quote = You showed us how small this market is. We would not have entered this market if we had this information in advance.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Timelines&quot;&gt;<br /> == Timelines ==<br /> Certain fields of research progress at bewildering speeds. It is often impossible for researchers, technology experts and executives alike to keep track of the developments. Dolcera timelines are exactly what their name implies: interactive visual maps that show the development of a field over the course of time. Our timelines are used for a variety of purposes including:<br /> * Understanding the development of a field of science/technology<br /> * Determining the contributions of individuals/companies to <br /> * Juxtaposing market and technology developments<br /> <br /> [[Image:timeline_sample_2.jpg|thumb|500px|center|Sample timeline]]<br /> ==== Case study: Timelines ====<br /> {{CaseStudy<br /> | topic = Timelines<br /> | client = A major N. American smartphone manufacturer<br /> | goal = Determine inventorship of some of the most important cellular telephony standards by analyzing patent, standard and market data.<br /> | duration = 4 weeks<br /> | result = Dolcera timelines, based on research through several gigabytes of standards meetings minutes, specifications and patents, allowed the client to negotiate with their competitors.<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Powerful search tools, data integration from disparate sources, succinct presentation<br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Sample timeline]<br /> | quote = I did not even have to lift a finger to understand the information... I used your presentation for my company's Board (of Directors).<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Business plans&quot;&gt;<br /> <br /> == Business plans ==<br /> Dolcera works in partnership with research and development groups within companies to help them understand the business opportunities for their research. We develop full-strength business plans with:<br /> * Commercialization possibilities for research<br /> * Competitive landscape<br /> * SWOT Analysis: Strengths, Weaknesses, Opportunities, Threats<br /> <br /> [[Image:swot_sample.jpg|thumb|250px|center|SWOT Analysis]]<br /> ==== Case study: Business plans ====<br /> {{CaseStudy<br /> | topic = Business plans<br /> | client = A global software company<br /> | goal = Create business case for a research project with several patent applications<br /> | duration = 6 weeks<br /> | result = Complete business plan including market research, financial plan, competitive analysis, product positioning, product and need characteristics<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Strong technology and business expertise to help researchers shorter innovation cycle<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = Dolcera is an integral part of our research commercialization strategy.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executive dashboard&quot;&gt;<br /> <br /> == Executive dashboard ==<br /> The Dolcera executive IP dashboard provides an integrated view of all the key performance indicators for your organization's intellectual property, including:<br /> * Patent filings<br /> * Patent licensing opportunities<br /> * Patent threats<br /> * Competitive position<br /> * Key IP performance indicators<br /> <br /> The interactive executive IP dashboard allows users to perform their own what-if analysis. Behind the scenes, the Dolcera team performs extensive research and market+competitive analysis to drive the executive dashboard and keep it up-to-date.<br /> <br /> &lt;gflash&gt;600 600 http://dolcera.com/ipmapdemo/rfid_model.swf&lt;/gflash&gt;<br /> <br /> ==== Case study: Executive dashboard ====<br /> {{CaseStudy<br /> | topic = Executive dashboard<br /> | client = A US medical device major<br /> | goal = Provide a central point of entry for all corporate IP performance indicators<br /> | duration = Ongoing<br /> | result = All patent information in one spot, and shared by all stakeholders within the organization.<br /> | customer_savings = Greater overall visibility improves response time considerably<br /> | dolcera_advantage = Correlating market movements with IP information and technology trends<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/alopecia_model.swf Consumer products dashboard], [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID Dashboard]<br /> | quote = The dashboard helps our team think strategically.<br /> }}<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Brand dashboard&quot;&gt;<br /> == Brand dashboard ==<br /> The brand manager dashboard is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard identifies the impact of global and local events on client's and competitor's brands. It brings together data from a variety of data sources. It also includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> &lt;gflash&gt;600 600 http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf&lt;/gflash&gt;<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Collaboration services&quot;&gt;<br /> <br /> == Collaboration services ==<br /> Dolcera provides a range of collaboration services for large organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup<br /> * Taxonomy design and updates<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> [[Image:taxonomy.jpg|thumb|300px|center|Dolcera taxonomy tool]]<br /> <br /> ==== Case study: Collaboration services ====<br /> {{CaseStudy<br /> | topic = Collaboration services<br /> | client = Large pharmaceutical company<br /> | goal = Provide a central Human Resources forms and document system for the corporate intranet.<br /> | duration = 2 months<br /> | result = We prepared the taxonomy and classification system for all documents and classified the documents initially. We also trained clients to update the documents on an ongoing basis.<br /> | customer_savings = Approximately $300,000 for the project<br /> | dolcera_advantage = Best-in-class technology and processes, ably supported by our technical team in India <br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IPMap]<br /> | quote = Our goal is to be a smarter organization, and Dolcera helped us achieve it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> <br /> <br /> == Questions Dolcera answers ==<br /> We help you answer questions such as:<br /> {| border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; align=&quot;center&quot; valign=&quot;top&quot;<br /> |-<br /> | <br /> * '''What’s hot'''<br /> ** What technology/approaches are the most promising?<br /> ** What technology/approaches have already been tried?<br /> ** What can I license?<br /> ** Is any empirical data available?<br /> * '''Where should I focus my R&amp;D investment'''<br /> ** Where’s the ‘white space’ for me to play in?<br /> * '''Any hints for research'''<br /> ** Are there any combinations I could develop?<br /> | <br /> * '''What should I do in this geography'''<br /> ** What are my competitors up to in this geography?<br /> ** What are my strengths/ weaknesses here?<br /> * '''What’s my competition up to'''<br /> ** What’s my top competitor investing in?<br /> ** Are there any loopholes in their strategy?<br /> ** Will a competitor emerge from nowhere and surprise me?<br /> ** What are the crowded areas?<br /> * '''How do I play defense'''<br /> ** What should my blocking/reactive strategies be?<br /> |}</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Quality_of_Service_on_CDMA_platforms&diff=1836 2006-06-27T05:25:25Z

<p>67.180.226.207: /* Power Control */</p> <hr /> <div>== Cellular Communication ==<br /> A cellular mobile communications system uses a large number of low-power wireless transmitters to create cells — the basic geographic service area of a wireless communications system. Variable power levels allow cells to be sized according to the subscriber density and demand within a particular region. As mobile users travel from cell to cell, their conversations are handed off between cells to maintain seamless service. Channels (frequencies) used in one cell can be reused in another cell some distance away. Cells can be added to accommodate growth, creating new cells in unserved areas or overlaying cells in existing areas. [http://www.IEC.org Source]<br /> <br /> There are three main entities in cellular communication<br /> * Mobile Station (MS): A mobile station consists of 2 entities - equipment and SIM card<br /> * Base Transceiver station(BTS): A base transceiver station consists of 2 entities - a base transceiver (transmitter and receiver) station and a base station controller. The BTS is the antenna tower site.<br /> * Main Switching centre(MSC): The main switching centre is the heart of the network - the central switching office which controls all the base stations and provides connection with landline phones. It performs three main tasks. It:<br /> # connects calls from sender to receiver,<br /> # collects details of the calls made and received, and<br /> # supervises operation of the rest of the network components.<br /> <br /> == Cellular System Architecture ==<br /> Cellular systems are increasing in demand as more users are added to their systems. The amount of frequency spectrum available for mobile cellular use was limited, and efficient use of the required frequencies was needed for mobile cellular coverage. In modern cellular telephony, rural and urban regions are divided into areas according to specific provisioning guidelines. Provisioning for each region is planned according to an engineering plan that includes cells, clusters, frequency reuse, and handovers.<br /> <br /> ==== Cells ==== <br /> A cell is the basic geographic unit of a cellular system. Cells are base stations transmitting over small geographic areas that are represented as hexagons.<br /> <br /> ==== Clusters ==== <br /> A cluster is a group of cells. No channels are reused within a cluster. Normally a cluster has seven cells in it as shown below.<br /> <br /> ==== Frequency Reuse ====<br /> The number of radio channel frequencies is limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> ==== Cell Splitting ==== <br /> As a service area becomes full of users, this approach is used to split a single area into smaller ones. In this way, urban centers can be split into as many areas as necessary to provide acceptable service levels in heavy-traffic regions, while larger, less expensive cells can be used to cover remote rural regions.<br /> <br /> ==== Handoff ====<br /> <br /> The final obstacle in the development of the cellular network involved the problem created when a mobile subscriber traveled from one cell to another during a call. As adjacent areas do not use the same radio channels, a call must either be dropped or transferred from one radio channel to another when a user crosses the line between adjacent cells. Because dropping the call is unacceptable, the process of handoff was created. Handoff occurs when the mobile telephone network automatically transfers a call from radio channel to radio channel as a mobile crosses adjacent cells.<br /> <br /> ==Evolution of Cellular Systems==<br /> [[Image:cdma1.jpg|500 px|center]]<br /> == Multiple Access Methods ==<br /> There are predominantly three types of multiple access methods.<br /> === Frequency Division Multiple Access ===<br /> In this system, each user is allotted a different set of frequencies to operate upon. The uplink(mobile to base station) frequency is different from downlink frequency(base station to mobile).<br /> [[Image:cdma6.jpg|thumb|700px|center|[http://www.ai.u-hyogo.ac.jp/~thai-proj/presen/20051222-Ishikawa.ppt FDMA]]]<br /> === Time Division Multiple Access ===<br /> In this system, each user is allocated a different time slot. Forward link frequency and reverse link frequency is the same. A synchronous switch is responsible for the time switching.<br /> [[Image:cdma10.jpg|thumb|600px|center|TDMA]]<br /> <br /> === Code Division Multiple Access ===<br /> There is no restriction on time and frequency in this scheme. All the users can transmit at all times and at all frequencies. Because users are isolated by code, they can share the same carrier frequency, eliminating the frequency reuse problem encountered in other technologies.<br /> [[Image:cdma11.jpg|thumb|600 px|centre|CDMA]]&lt;br&gt;<br /> <br /> A comparative study between the above three access technologies with respect to time and frequency is as shown below.<br /> [[Image:cdma12.jpg|thumb|600 px|centre|Comparison of cellular access schemes]]<br /> <br /> == Code Division Multiple Access ==<br /> The CDMA technology can be implemented in two ways<br /> * Direct Sequence Spread Sprectrum - DSSS CDMA<br /> * Frequency Hopping - FH CDMA<br /> === Direct Sequence Spread Sprectrum - DSSS CDMA === <br /> In this method, the direct sequence(input data) which is spread over a limited bandwidth is multiplied with a code or spreading sequence (a pseudorandom sequence) which will spread the input data over the entire bandwidth of the communication channel. The power density is also reduced and is spread over the frequency spectrum and hence is known as spread spectrum method. The modulation part of DSSS is as shown below.<br /> [[Image:cdma13.jpg|thumb|600px|center|CDMA Modulation]]<br /> The modulated signal is transmitted over the channel and all users can receive it but only the user which knows the correct code can decode the message. This is depicted in the figure below.<br /> [[Image:cdma14.jpg|thumb|600px|center|CDMA Demodulation]]<br /> <br /> === Frequency Reuse === <br /> The number of radio channel frequencies is limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> === Soft Handoff === <br /> Handoff means switching a cellular phone transmission from one cell to another as a mobile user moves into a new cellular area. It is so called because the radio link with the previous sector(s) is not broken before a link is established with a new sector; this type of handoff is described as &quot;make before break&quot;. In CDMA, due to this soft handoff, there is no interruption of call even at the border of a cell site which means more number of customers can be accommodated, automatically increasing the capacity of the cell site.<br /> <br /> === Multipath Fading === <br /> In a mobile environment, a mobile station will receive one direct signal from the base station and multiple signals which are reflected from obstructions like buildings and towers. Each signal would have travelled a different length and would be displaced in time. Due to this, when they are combined at the mobile handset, it will cause interference resulting in poor signal quality. This is known as ''fading''. This problem is handled in a very good way in CDMA. Here, the phase of the multiple signals is modified such that only positive interference(addition) takes place and the overall signal strength increases. A receiver that implements the above principle is known as a RAKE receiver as shown in the figure below.<br /> [[Image:cdma15.jpg|thumb|center|600px|RAKE receiver]]<br /> === Near Far Problem === <br /> The problem is best described by taking an example: Consider a receiver and two transmitters (one close to the receiver; the other far away). If both transmitters transmit simultaneously and at equal powers, then due to the inverse square law, the receiver will receive more power from the nearer transmitter. This makes the farther transmitter voice more difficult to understand. Since one transmission's signal is the other's noise the signal-to-noise ratio (SNR) for the farther transmitter is much lower. If the nearer transmitter transmits a signal that is orders of magnitude higher than the farther transmitter, then the SNR for the farther transmitter may be below detectability and the farther transmitter may just as well not transmit. This effectively jams the communication channel. In CDMA systems, this is commonly solved by dynamic output power adjustment of the transmitters. That is, the closer transmitters use less power so that the SNR for all transmitters at the receiver is roughly the same. This sometimes can have a noticeable impact on battery life, which can be dramatically different depending on distance from the base station.<br /> [[Image:cdma16.jpg|thumb|600px|center|Dynamic output power adjustment for CDMA transmitters]]<br /> <br /> ===Power Control=== <br /> As the propagation losses between BS and MS's are different according to individual communication distances, the received levels at the base station are different from each other when all mobile stations transmit their signals at the same power. Moreover, the received level fluctuates quickly due to fading. In order to maintain the strength of received signal level at BS, power control technique must be employed in CDMA systems.&lt;br&gt;.<br /> [[Image:cdma17.jpg]]&lt;br&gt;<br /> Power control can be implemented in two ways : open loop power control and closed loop power control&lt;br&gt;<br /> [[Image:cdma18.jpg]]<br /> <br /> '''Effect of Power Control''': Power control is capable of compensating the fading fluctuation. Received power from all MS are controlled to be equal.　Near-Far problem is mitigated by the power control.<br /> [[Image:cdma19.jpg]]<br /> <br /> ==Quality of Service(QoS)==<br /> CDMA is being accepted as a third generation (3G) system and a specific feature of 3G systems is that they offer a radio interface adapted for all kinds of services and combination of services (such as data, voice, video etc). The big challenge is multiplexing these services which have do not have the same demands in terms of quality of service(QoS) which can be represented as BER(bit error rate), processing delay, frame error rate etc. Different QoS will require different channel encoding and interleaving strategies. The demand of BER can be satisfied when the coding bits have at least a code dependent ratio Eb/I(ratio of bit energy to interference). There are several influences that might change system performance(BER) and hence Eb/I ratio, of which the most effective is variation of Bit Rate by a step of '''Rate Matching'''.<br /> <br /> ===Rate Matching and QoS===<br /> The patent [http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1385290&amp;F=0 EP1385290] titled &quot;Method for balancing Eb/I ratio in a service multiplexing CDMA system and a telecommunication system using this method&quot; targets this concept of Rate matching and introduces an algorithm for calculating effective data output bits by a process of repetition or puncturing of the input bits governed by a '''rate matching ratio''' and '''puncturing ratio''' received from the sending entity (can be a BS or MS). The following framework highlights the various steps involved in providing variable QoS. The received data from the transport block is classified into different processes based on their QoS. Data is split onto various transport channels to which a CRC code is attached for error correction. Further, all these transport channels are multiplexed on one line by concatenation, interleaved, segmented and then rate matched. The rate matching step is performed using the rate matching ratio and puncturing ratio which is received from the sending entity (an exchange of handshaking signals occurs).<br /> <br /> [[Image:cdma20.jpg|thumb|600px|center|Rate matching and QoS]]<br /> <br /> ===Power Control, Rate Matching and QoS===<br /> According to one of the methods of dynamic power control (Code Hopping) used in W-CDMA technology, the Rate Information (RI) field in the uplink control channel in W-CDMA frame can be used to notify the base station about the variable bit rates (VBR) it wants to send, then the base station computes and assigns optimal powers according to the new spreading factor for each radio frame. Spreading factor(Gi) is defined as the ratio of bandwidth of the system to the data rate of the radio frame.<br /> Mathematically,&lt;br&gt;<br /> '''Gi = W / Ri''',where W=system bandwidth which is a constant for a system and Ri= data rate of radio frame.&lt;br&gt;<br /> A power index (gi) is calculated from this Spreading Factor(Gi) using the following expression&lt;br&gt;<br /> '''gi= (vi / (vi+Gi))''', where vi is minimum QoS for the ith session which is a constant.&lt;br&gt; <br /> This power index will ascertain the optimal power to be alloted to each service channel.&lt;br&gt; <br /> '''Pi = (gi*No*W )/ (Hi*(1-(Sgj)'''&lt;br&gt;<br /> where No is AWGN(Additive White Guassian Noise)a constant,&lt;br&gt; <br /> Hi is path loss which is dependent on the distance and is a costant for a path,&lt;br&gt; <br /> and Sgj is sum of the power index of all the sessions which is constant for all sessions of the radio frame.<br /> <br /> From the above analysis, we observe that the bit rate is inversely proportional to the spreading factor which will inversely effect the power index and hence the optimal power. Therefore, the Bit Rate and Optimal power go hand in hand, and have the same effect on Eb/I and QoS.<br /> <br /> The method and algorithm to schedule optimal power is detailed in the IEEE paper [[Media:IEEEGurbuz.pdf|Dynamic Resource Scheduling for Variable QoS Traffic in W-CDMA - Ozgur Gurbuz, Henry Owen]]. <br /> <br /> Thus, we conclude that by adjusting the optimal power we are actually trying to implement a rate matching step.<br /> <br /> ===Power control and QoS===<br /> Transmission power of mobile station is proportional to power control law, which is a function of distance from the base station, transmission rates, interference level (number of active users). In this method, the Bit Error probability of the multi-rate CDMA mobile station is calculated at the Base station using transmission rates of the mobile. The optimal power control functions are derived based on the bit error probability at the base station and these power control functions are transmitted to the mobile handset. The mobile calculates the optimum power using dynamic programming and transmits its data at this power level. It is of interest to note that the optimum power level is related to power index which will determine the spreading gain and hence the overall bit rate. Thus the optimum power level is acheived by transmitting the data at the calculated bit rate.<br /> <br /> ==Conclusion==<br /> Substantial amount of research has been done in the field of QoS in CDMA communication system in the year 1998-99 and this has led to the invention of multitude of methodologies ranging from power control to Rate matching and so on with the sole aim of improving QoS.</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Quality_of_Service_on_CDMA_platforms&diff=1797 2006-06-26T07:14:04Z

<p>67.180.226.207: /* Cellular Communication */</p> <hr /> <div>==Cellular Communication==<br /> A cellular mobile communications system uses a large number of low-power wireless transmitters to create cells—the basic geographic service area of a wireless communications system. Variable power levels allow cells to be sized according to the subscriber density and demand within a particular region. As mobile users travel from cell to cell, their conversations are handed off between cells to maintain seamless service. Channels (frequencies) used in one cell can be reused in another cell some distance away. Cells can be added to accommodate growth, creating new cells in unserved areas or overlaying cells in existing areas.<br /> [http://www.IEC.org Source]&lt;br&gt;<br /> There are three main entities in cellular communication<br /> * Mobile station (MS)- consists of 2 entities- Equipment and SIM card<br /> * Base Transceiver station(BTS) - consists of 2 entities- Base transceiver(transmitter and receiver) station and Base station controller. This is the antenna tower site.<br /> * Main Switching centre(MSC) - Heart of the network, Central switching office which controls all the base stations and provides connection with landline phones.<br /> Three main jobs:<br /> # connects calls from sender to receiver<br /> # collects details of the calls made and received<br /> # supervises operation of the rest of the network components<br /> <br /> ==Cellular System Architecture==<br /> Increases in demand - more users in their systems.Amount of frequency spectrum available for mobile cellular use was limited, efficient use of the required frequencies was needed for mobile cellular coverage. In modern cellular telephony, rural and urban regions are divided into areas according to specific provisioning guidelines. Provisioning for each region is planned according to an engineering plan that includes cells, clusters, frequency reuse, and handovers.<br /> <br /> '''Cells'''<br /> A cell is the basic geographic unit of a cellular system. Cells are base stations transmitting over small geographic areas that are represented as hexagons.<br /> <br /> '''Clusters'''<br /> A cluster is a group of cells. No channels are reused within a cluster. Normally a cluster has seven-cells in it as shown below.<br /> <br /> '''Frequency Reuse'''<br /> Number of radio channel frequencies are limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> '''Cell Splitting'''<br /> <br /> As a service area becomes full of users, this approach is used to split a single area into smaller ones. In this way, urban centers can be split into as many areas as necessary to provide acceptable service levels in heavy-traffic regions, while larger, less expensive cells can be used to cover remote rural regions<br /> <br /> '''Handoff'''<br /> <br /> The final obstacle in the development of the cellular network involved the problem created when a mobile subscriber traveled from one cell to another during a call. As adjacent areas do not use the same radio channels, a call must either be dropped or transferred from one radio channel to another when a user crosses the line between adjacent cells. Because dropping the call is unacceptable, the process of handoff was created. Handoff occurs when the mobile telephone network automatically transfers a call from radio channel to radio channel as a mobile crosses adjacent cells<br /> ==Evolution of Cellular Systems==<br /> [[Image:cdma1.jpg|500 px|center]]<br /> ==Multiple Access Methods==<br /> There are predominantly three types of multiple access methods.&lt;br&gt;<br /> '''Frequency Division Multiple Access:''' In this system each user is alloted a different set of frequency to operate upon. The uplink(mobile to base station) frequency is different from downlink frequency(base station to mobile).<br /> [[Image:cdma6.jpg]]&lt;br&gt;<br /> [Ref:www.ai.u-hyogo.ac.jp/~thai-proj/presen/20051222-Ishikawa.ppt]<br /> '''Time Division Multiple Access:'''In this system each user is allocated a different time slot.Forward link frequency and reverse link frequency is the same. A synchronous switch is responsible to do the time switching.<br /> [[Image:cdma10.jpg]]<br /> '''Code Division Multiple Access:'''There is no restriction on time and frequency in this scheme. All the users can transmit at all times and at all frequencies. Because users are isolated by code, they can share the same carrier frequency, eliminating the frequency reuse problem encountered in other technologies.&lt;br&gt;<br /> [[Image:cdma11.jpg|600 px|centre]]&lt;br&gt;<br /> A comparative study between the above three access technologies with respect to time and frequency is as shown below&lt;br&gt;.<br /> [[Image:cdma12.jpg|600 px|centre]]<br /> <br /> ==Code Division Multiple Access==<br /> The CDMA technology can be implemented in two ways<br /> * Direct Sequence Spread Sprectrum - DSSS CDMA<br /> * Frequency Hopping - FH CDMA<br /> '''Direct Sequence Spread Sprectrum - DSSS CDMA:''' In this method the direct sequence(input data) which is spread over a limited bandwidth is multiplied with a code or spreading sequence (a pseudorandom sequence) which will spread the input data over the entire bandwidth of the communication channel. The power density is also reduced and is spread over the frequency spectrum and hence is known as spread spectrum method. The modulation part of DSSS is as shown below&lt;br&gt;<br /> [[Image:cdma13.jpg]]<br /> The modulated signal is transmitted over the channel and all users can receive it but only the user which knows the correct code can only decode the message. This is depicted in the figure below.&lt;br&gt;<br /> [[Image:cdma14.jpg]]<br /> ===Features of CDMA===<br /> ====Frequency Reuse==== <br /> Number of radio channel frequencies are limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> ====Soft Handoff==== Handoff means Switching a cellular phone transmission from one cell to another as a mobile user moves into a new cellular area. It is so called because the radio link with the previous sector(s) is not broken before a link is established with a new sector; this type of handoff is described as &quot;make before break&quot;. In CDMA due to this soft handoff there is no interruption of call even at the border of cell site which means more number of customers can be accommodated automatically increasing the capacity of the cell site.<br /> <br /> ====Multipath Fading==== In a mobile environment a mobile station will receive one direct signal from the base station and multiple signals which are reflected from obstructions like building and towers. Each signal would have travelled a different length and would be displaced in time. Due to this when they are combined at the mobile it will cause interference resulting in poor signal quality. This is called as fading. This problem is handled in a very good way in CDMA. Here the phase of the multiple signals is modified such the only positive interference(addition) takes place the overall signal strength increases. A receiver that implements the above principle is known as a RAKE receiver as shown in the figure below&lt;br&gt;<br /> [[Image:cdma15.jpg]]<br /> ====Near Far Problem==== The problem is described by taking an example consider a receiver and two transmitters (one close to the receiver; the other far away). If both transmitters transmit simultaneously and at equal powers, then due to the inverse square law the receiver will receive more power from the nearer transmitter. This makes the farther transmitter voice more difficult to understand. Since one transmission's signal is the other's noise the signal-to-noise ratio (SNR) for the farther transmitter is much lower. If the nearer transmitter transmits a signal that is orders of magnitude higher than the farther transmitter then the SNR for the farther transmitter may be below detectability and the farther transmitter may just as well not transmit. This effectively jams the communication channel. In CDMA systems this is commonly solved by dynamic output power adjustment of the transmitters. That is the closer transmitters use less power so that the SNR for all transmitters at the receiver is roughly the same. This sometimes can have a noticeable impact on battery life, which can be dramatically different depending on distance from the base station.&lt;br&gt;<br /> [[Image:cdma16.jpg]]<br /> ====Power Control:==== As the propagation losses between BS and MS's are different according to individual communication distances, the received levels at the base station are different from each other when all mobile stations transmit their signals at the same power. Moreover, the received level fluctuates quickly due to fading. In order to maintain the strength of received signal level at BS, power control technique must be employed in CDMA systems.&lt;br&gt;.<br /> [[Image:cdma17.jpg]]&lt;br&gt;<br /> Power control can be implemented in two ways : open loop power control and closed loop power control&lt;br&gt;<br /> [[Image:cdma18.jpg]]<br /> <br /> '''Effect of Power Control''' Power control is capable of compensating the fading fluctuation. Received power from all MS are controlled to be equal.　Near-Far problem is mitigated by the power control.<br /> [[Image:cdma19.jpg]]<br /> ==Quality of Service(QoS)==<br /> CDMA is being accepted as a third generation system and a specific feature of 3G system is that it offers a radio interface adapted for all kinds of services and combination of services(data,voice,image etc). The big issue is of multiplexing of these services which have do not have the same demands in terms of quality of service(QoS) which can be represented as BER(bit error rate),processing delay,frame error rate etc. Different QoS will require different channel encoding and interleaving strategies. The demand of BER can be satisfied when the coding bits have atleast a code dependent ratio Eb/I(ratio of bit energy to interference). There are several influences that might change system performance(BER) and hence Eb/I ratio, of which the most effective is variation of Bit Rate by a step of '''Rate Matching'''. &lt;br&gt;&lt;br&gt;<br /> ===Rate Matching and QoS===<br /> The patent '''EP 1385290 titled Method for balancing Eb/I ratio in a service multiplexing CDMA system and a telecommunication system using this method''' targets at this concept of Rate matching and introduces an algorithm of calculating effective data output bits by a process of repetition or puncturing of the input bits governed by a '''rate matching ratio''' and '''puncturing ratio''' received from the sending entity(can be BS or MS). The following framework highlights the various steps involved in providing variable QoS.<br /> <br /> ===Power Control, Rate Matching and QoS===<br /> According to one of the methods of dynamic power control (Code Hopping) used in W-CDMA technology, the Rate Information (RI) field in the uplink control channel in W-CDMA frame can be used to notify the base station about the variable bit rates (VBR) it wants to send, then the base station computes and assigns optimal powers according to the new spreading factor for each radio frame. Spreading factor(Gi) is defined as the ratio of bandwidth of the system to the data rate of the radio frame.<br /> Mathematically,&lt;br&gt;<br /> '''Gi = W / Ri''',where W=system bandwidth which is a constant for a system and Ri= data rate of radio frame.&lt;br&gt;<br /> A power index (gi) is calculated from this Spreading Factor(Gi) using the following expression&lt;br&gt;<br /> '''gi= (gi / (gi+Gi))''', where gi is minimum QoS for the ith session which is a constant.&lt;br&gt; <br /> This power index will ascertain the optimal power to be alloted to each service channel.&lt;br&gt; <br /> '''Pi = (gi*No*W )/ (Hi*(1-(Sgj)'''&lt;br&gt;<br /> where No is AWGN(Additive White Guassian Noise)a constant,&lt;br&gt; Hi is path loss which is dependent on the distance and is a costant for a path,&lt;br&gt; and Sgj is sum of the power index of all the sessions which is constant for all sessions of the radio frame. &lt;br&gt;<br /> From the above analysis, we observe that Bit Rate is inversely proportional to Spreading factor which will inversely effect the power index and hence the optimal power. Therefore, the Bit Rate and Optimal power go hand in glove and have the same effect on Eb/I and QoS.<br /> The method and algorithm to schedule optimal power is detailed in the IEEE paper '''Dynamic Resource Scheduling for Variable QoS Traffic in W-CDMA Ozgur Gurbuz, Henry Owen'''. <br /> Thus we conclude that by adjusting the optimal power we are actually trying to implement a rate matching step.<br /> [[Media:ieee1.pdf]]<br /> <br /> ===Power control and QoS===<br /> SPEECH transmission is the main service supported by the first two generations of mobile communication systems. However, future systems should be able to handle a wide variety of different services with bit rate requirement ranging from a few kilobits/s to as much as 2 Mb/s. There are many ways to design a CDMA system to support multirate services . One way to do so is to spread all signals, independent of the bit rate, to the same bandwidth . This is done by keeping the chip rate constant. Users transmitting at low bit rate thus have a high processing gain. This allows those users to transmit at a lower power. Therefore, the conventional constant received power scheme is not appropriate in such a multirate system. A more sophisticated power control scheme is needed to achieve diverse quality of service (QoS) and rate requirement. One such scheme which explores the relationship between the data rate, the QoS, and the transmit power is presented in the IEEE paper '''Power Control and Rate Management for Wireless Multimedia CDMA Systems Chi Wan Sung, Member, IEEE, and Wing Shing Wong, Senior Member, IEEE.'''<br /> ===Dynamic Resource Scheduling and QoS===<br /> Dynamic Resource Scheduling (DRS) has been proposed as an adaptive resource management and QoS<br /> provisioning framework applicable to W-CDMA systems. Various spreading strategies like Fixed Spreading Gain (FSG), Variable Spreading Gain (VSG) and Multi Code (MC) strategies and their performance is compared in terms of power saving, resource allocation and QoS stability in the IEEE paper '''DYNAMIC RESOURCE SCHEDULING STRATEGIES FOR QOS IN W-CDMA by Ozgur Gurbuz, Henry Owen.''' VSG-DRS and MC-DRS outperform the FSG-DRS for capacity as a result of the statistical multiplexing gain created by adaptive bandwidth usage.<br /> <br /> ==Conclusion==<br /> Substantial amount of research has been done in the field of QoS in CDMA communication system in the year 1998-99 and this has led to the invention of multitude of methodologies ranging from power control to Rate matching and so on with the sole aim of improving QoS.</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Quality_of_Service_on_CDMA_platforms&diff=1796 2006-06-26T07:13:42Z

<p>67.180.226.207: /* Cellular Communication */</p> <hr /> <div>==Cellular Communication==<br /> A cellular mobile communications system uses a large number of low-power wireless transmitters to create cells—the basic geographic service area of a wireless communications system. Variable power levels allow cells to be sized according to the subscriber density and demand within a particular region. As mobile users travel from cell to cell, their conversations are handed off between cells to maintain seamless service. Channels (frequencies) used in one cell can be reused in another cell some distance away. Cells can be added to accommodate growth, creating new cells in unserved areas or overlaying cells in existing areas.<br /> [[http://www.IEC.org Source]]&lt;br&gt;<br /> There are three main entities in cellular communication<br /> * Mobile station (MS)- consists of 2 entities- Equipment and SIM card<br /> * Base Transceiver station(BTS) - consists of 2 entities- Base transceiver(transmitter and receiver) station and Base station controller. This is the antenna tower site.<br /> * Main Switching centre(MSC) - Heart of the network, Central switching office which controls all the base stations and provides connection with landline phones.<br /> Three main jobs:<br /> # connects calls from sender to receiver<br /> # collects details of the calls made and received<br /> # supervises operation of the rest of the network components<br /> <br /> ==Cellular System Architecture==<br /> Increases in demand - more users in their systems.Amount of frequency spectrum available for mobile cellular use was limited, efficient use of the required frequencies was needed for mobile cellular coverage. In modern cellular telephony, rural and urban regions are divided into areas according to specific provisioning guidelines. Provisioning for each region is planned according to an engineering plan that includes cells, clusters, frequency reuse, and handovers.<br /> <br /> '''Cells'''<br /> A cell is the basic geographic unit of a cellular system. Cells are base stations transmitting over small geographic areas that are represented as hexagons.<br /> <br /> '''Clusters'''<br /> A cluster is a group of cells. No channels are reused within a cluster. Normally a cluster has seven-cells in it as shown below.<br /> <br /> '''Frequency Reuse'''<br /> Number of radio channel frequencies are limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> '''Cell Splitting'''<br /> <br /> As a service area becomes full of users, this approach is used to split a single area into smaller ones. In this way, urban centers can be split into as many areas as necessary to provide acceptable service levels in heavy-traffic regions, while larger, less expensive cells can be used to cover remote rural regions<br /> <br /> '''Handoff'''<br /> <br /> The final obstacle in the development of the cellular network involved the problem created when a mobile subscriber traveled from one cell to another during a call. As adjacent areas do not use the same radio channels, a call must either be dropped or transferred from one radio channel to another when a user crosses the line between adjacent cells. Because dropping the call is unacceptable, the process of handoff was created. Handoff occurs when the mobile telephone network automatically transfers a call from radio channel to radio channel as a mobile crosses adjacent cells<br /> ==Evolution of Cellular Systems==<br /> [[Image:cdma1.jpg|500 px|center]]<br /> ==Multiple Access Methods==<br /> There are predominantly three types of multiple access methods.&lt;br&gt;<br /> '''Frequency Division Multiple Access:''' In this system each user is alloted a different set of frequency to operate upon. The uplink(mobile to base station) frequency is different from downlink frequency(base station to mobile).<br /> [[Image:cdma6.jpg]]&lt;br&gt;<br /> [Ref:www.ai.u-hyogo.ac.jp/~thai-proj/presen/20051222-Ishikawa.ppt]<br /> '''Time Division Multiple Access:'''In this system each user is allocated a different time slot.Forward link frequency and reverse link frequency is the same. A synchronous switch is responsible to do the time switching.<br /> [[Image:cdma10.jpg]]<br /> '''Code Division Multiple Access:'''There is no restriction on time and frequency in this scheme. All the users can transmit at all times and at all frequencies. Because users are isolated by code, they can share the same carrier frequency, eliminating the frequency reuse problem encountered in other technologies.&lt;br&gt;<br /> [[Image:cdma11.jpg|600 px|centre]]&lt;br&gt;<br /> A comparative study between the above three access technologies with respect to time and frequency is as shown below&lt;br&gt;.<br /> [[Image:cdma12.jpg|600 px|centre]]<br /> <br /> ==Code Division Multiple Access==<br /> The CDMA technology can be implemented in two ways<br /> * Direct Sequence Spread Sprectrum - DSSS CDMA<br /> * Frequency Hopping - FH CDMA<br /> '''Direct Sequence Spread Sprectrum - DSSS CDMA:''' In this method the direct sequence(input data) which is spread over a limited bandwidth is multiplied with a code or spreading sequence (a pseudorandom sequence) which will spread the input data over the entire bandwidth of the communication channel. The power density is also reduced and is spread over the frequency spectrum and hence is known as spread spectrum method. The modulation part of DSSS is as shown below&lt;br&gt;<br /> [[Image:cdma13.jpg]]<br /> The modulated signal is transmitted over the channel and all users can receive it but only the user which knows the correct code can only decode the message. This is depicted in the figure below.&lt;br&gt;<br /> [[Image:cdma14.jpg]]<br /> ===Features of CDMA===<br /> ====Frequency Reuse==== <br /> Number of radio channel frequencies are limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> ====Soft Handoff==== Handoff means Switching a cellular phone transmission from one cell to another as a mobile user moves into a new cellular area. It is so called because the radio link with the previous sector(s) is not broken before a link is established with a new sector; this type of handoff is described as &quot;make before break&quot;. In CDMA due to this soft handoff there is no interruption of call even at the border of cell site which means more number of customers can be accommodated automatically increasing the capacity of the cell site.<br /> <br /> ====Multipath Fading==== In a mobile environment a mobile station will receive one direct signal from the base station and multiple signals which are reflected from obstructions like building and towers. Each signal would have travelled a different length and would be displaced in time. Due to this when they are combined at the mobile it will cause interference resulting in poor signal quality. This is called as fading. This problem is handled in a very good way in CDMA. Here the phase of the multiple signals is modified such the only positive interference(addition) takes place the overall signal strength increases. A receiver that implements the above principle is known as a RAKE receiver as shown in the figure below&lt;br&gt;<br /> [[Image:cdma15.jpg]]<br /> ====Near Far Problem==== The problem is described by taking an example consider a receiver and two transmitters (one close to the receiver; the other far away). If both transmitters transmit simultaneously and at equal powers, then due to the inverse square law the receiver will receive more power from the nearer transmitter. This makes the farther transmitter voice more difficult to understand. Since one transmission's signal is the other's noise the signal-to-noise ratio (SNR) for the farther transmitter is much lower. If the nearer transmitter transmits a signal that is orders of magnitude higher than the farther transmitter then the SNR for the farther transmitter may be below detectability and the farther transmitter may just as well not transmit. This effectively jams the communication channel. In CDMA systems this is commonly solved by dynamic output power adjustment of the transmitters. That is the closer transmitters use less power so that the SNR for all transmitters at the receiver is roughly the same. This sometimes can have a noticeable impact on battery life, which can be dramatically different depending on distance from the base station.&lt;br&gt;<br /> [[Image:cdma16.jpg]]<br /> ====Power Control:==== As the propagation losses between BS and MS's are different according to individual communication distances, the received levels at the base station are different from each other when all mobile stations transmit their signals at the same power. Moreover, the received level fluctuates quickly due to fading. In order to maintain the strength of received signal level at BS, power control technique must be employed in CDMA systems.&lt;br&gt;.<br /> [[Image:cdma17.jpg]]&lt;br&gt;<br /> Power control can be implemented in two ways : open loop power control and closed loop power control&lt;br&gt;<br /> [[Image:cdma18.jpg]]<br /> <br /> '''Effect of Power Control''' Power control is capable of compensating the fading fluctuation. Received power from all MS are controlled to be equal.　Near-Far problem is mitigated by the power control.<br /> [[Image:cdma19.jpg]]<br /> ==Quality of Service(QoS)==<br /> CDMA is being accepted as a third generation system and a specific feature of 3G system is that it offers a radio interface adapted for all kinds of services and combination of services(data,voice,image etc). The big issue is of multiplexing of these services which have do not have the same demands in terms of quality of service(QoS) which can be represented as BER(bit error rate),processing delay,frame error rate etc. Different QoS will require different channel encoding and interleaving strategies. The demand of BER can be satisfied when the coding bits have atleast a code dependent ratio Eb/I(ratio of bit energy to interference). There are several influences that might change system performance(BER) and hence Eb/I ratio, of which the most effective is variation of Bit Rate by a step of '''Rate Matching'''. &lt;br&gt;&lt;br&gt;<br /> ===Rate Matching and QoS===<br /> The patent '''EP 1385290 titled Method for balancing Eb/I ratio in a service multiplexing CDMA system and a telecommunication system using this method''' targets at this concept of Rate matching and introduces an algorithm of calculating effective data output bits by a process of repetition or puncturing of the input bits governed by a '''rate matching ratio''' and '''puncturing ratio''' received from the sending entity(can be BS or MS). The following framework highlights the various steps involved in providing variable QoS.<br /> <br /> ===Power Control, Rate Matching and QoS===<br /> According to one of the methods of dynamic power control (Code Hopping) used in W-CDMA technology, the Rate Information (RI) field in the uplink control channel in W-CDMA frame can be used to notify the base station about the variable bit rates (VBR) it wants to send, then the base station computes and assigns optimal powers according to the new spreading factor for each radio frame. Spreading factor(Gi) is defined as the ratio of bandwidth of the system to the data rate of the radio frame.<br /> Mathematically,&lt;br&gt;<br /> '''Gi = W / Ri''',where W=system bandwidth which is a constant for a system and Ri= data rate of radio frame.&lt;br&gt;<br /> A power index (gi) is calculated from this Spreading Factor(Gi) using the following expression&lt;br&gt;<br /> '''gi= (gi / (gi+Gi))''', where gi is minimum QoS for the ith session which is a constant.&lt;br&gt; <br /> This power index will ascertain the optimal power to be alloted to each service channel.&lt;br&gt; <br /> '''Pi = (gi*No*W )/ (Hi*(1-(Sgj)'''&lt;br&gt;<br /> where No is AWGN(Additive White Guassian Noise)a constant,&lt;br&gt; Hi is path loss which is dependent on the distance and is a costant for a path,&lt;br&gt; and Sgj is sum of the power index of all the sessions which is constant for all sessions of the radio frame. &lt;br&gt;<br /> From the above analysis, we observe that Bit Rate is inversely proportional to Spreading factor which will inversely effect the power index and hence the optimal power. Therefore, the Bit Rate and Optimal power go hand in glove and have the same effect on Eb/I and QoS.<br /> The method and algorithm to schedule optimal power is detailed in the IEEE paper '''Dynamic Resource Scheduling for Variable QoS Traffic in W-CDMA Ozgur Gurbuz, Henry Owen'''. <br /> Thus we conclude that by adjusting the optimal power we are actually trying to implement a rate matching step.<br /> [[Media:ieee1.pdf]]<br /> <br /> ===Power control and QoS===<br /> SPEECH transmission is the main service supported by the first two generations of mobile communication systems. However, future systems should be able to handle a wide variety of different services with bit rate requirement ranging from a few kilobits/s to as much as 2 Mb/s. There are many ways to design a CDMA system to support multirate services . One way to do so is to spread all signals, independent of the bit rate, to the same bandwidth . This is done by keeping the chip rate constant. Users transmitting at low bit rate thus have a high processing gain. This allows those users to transmit at a lower power. Therefore, the conventional constant received power scheme is not appropriate in such a multirate system. A more sophisticated power control scheme is needed to achieve diverse quality of service (QoS) and rate requirement. One such scheme which explores the relationship between the data rate, the QoS, and the transmit power is presented in the IEEE paper '''Power Control and Rate Management for Wireless Multimedia CDMA Systems Chi Wan Sung, Member, IEEE, and Wing Shing Wong, Senior Member, IEEE.'''<br /> ===Dynamic Resource Scheduling and QoS===<br /> Dynamic Resource Scheduling (DRS) has been proposed as an adaptive resource management and QoS<br /> provisioning framework applicable to W-CDMA systems. Various spreading strategies like Fixed Spreading Gain (FSG), Variable Spreading Gain (VSG) and Multi Code (MC) strategies and their performance is compared in terms of power saving, resource allocation and QoS stability in the IEEE paper '''DYNAMIC RESOURCE SCHEDULING STRATEGIES FOR QOS IN W-CDMA by Ozgur Gurbuz, Henry Owen.''' VSG-DRS and MC-DRS outperform the FSG-DRS for capacity as a result of the statistical multiplexing gain created by adaptive bandwidth usage.<br /> <br /> ==Conclusion==<br /> Substantial amount of research has been done in the field of QoS in CDMA communication system in the year 1998-99 and this has led to the invention of multitude of methodologies ranging from power control to Rate matching and so on with the sole aim of improving QoS.</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Quality_of_Service_on_CDMA_platforms&diff=1795 2006-06-26T07:13:17Z

<p>67.180.226.207: </p> <hr /> <div>==Cellular Communication==<br /> A cellular mobile communications system uses a large number of low-power wireless transmitters to create cells—the basic geographic service area of a wireless communications system. Variable power levels allow cells to be sized according to the subscriber density and demand within a particular region. As mobile users travel from cell to cell, their conversations are handed off between cells to maintain seamless service. Channels (frequencies) used in one cell can be reused in another cell some distance away. Cells can be added to accommodate growth, creating new cells in unserved areas or overlaying cells in existing areas.<br /> [[source:www.IEC.org]]&lt;br&gt;<br /> There are three main entities in cellular communication<br /> * Mobile station (MS)- consists of 2 entities- Equipment and SIM card<br /> * Base Transceiver station(BTS) - consists of 2 entities- Base transceiver(transmitter and receiver) station and Base station controller. This is the antenna tower site.<br /> * Main Switching centre(MSC) - Heart of the network, Central switching office which controls all the base stations and provides connection with landline phones.<br /> Three main jobs:<br /> # connects calls from sender to receiver<br /> # collects details of the calls made and received<br /> # supervises operation of the rest of the network components<br /> <br /> ==Cellular System Architecture==<br /> Increases in demand - more users in their systems.Amount of frequency spectrum available for mobile cellular use was limited, efficient use of the required frequencies was needed for mobile cellular coverage. In modern cellular telephony, rural and urban regions are divided into areas according to specific provisioning guidelines. Provisioning for each region is planned according to an engineering plan that includes cells, clusters, frequency reuse, and handovers.<br /> <br /> '''Cells'''<br /> A cell is the basic geographic unit of a cellular system. Cells are base stations transmitting over small geographic areas that are represented as hexagons.<br /> <br /> '''Clusters'''<br /> A cluster is a group of cells. No channels are reused within a cluster. Normally a cluster has seven-cells in it as shown below.<br /> <br /> '''Frequency Reuse'''<br /> Number of radio channel frequencies are limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> '''Cell Splitting'''<br /> <br /> As a service area becomes full of users, this approach is used to split a single area into smaller ones. In this way, urban centers can be split into as many areas as necessary to provide acceptable service levels in heavy-traffic regions, while larger, less expensive cells can be used to cover remote rural regions<br /> <br /> '''Handoff'''<br /> <br /> The final obstacle in the development of the cellular network involved the problem created when a mobile subscriber traveled from one cell to another during a call. As adjacent areas do not use the same radio channels, a call must either be dropped or transferred from one radio channel to another when a user crosses the line between adjacent cells. Because dropping the call is unacceptable, the process of handoff was created. Handoff occurs when the mobile telephone network automatically transfers a call from radio channel to radio channel as a mobile crosses adjacent cells<br /> ==Evolution of Cellular Systems==<br /> [[Image:cdma1.jpg|500 px|center]]<br /> ==Multiple Access Methods==<br /> There are predominantly three types of multiple access methods.&lt;br&gt;<br /> '''Frequency Division Multiple Access:''' In this system each user is alloted a different set of frequency to operate upon. The uplink(mobile to base station) frequency is different from downlink frequency(base station to mobile).<br /> [[Image:cdma6.jpg]]&lt;br&gt;<br /> [Ref:www.ai.u-hyogo.ac.jp/~thai-proj/presen/20051222-Ishikawa.ppt]<br /> '''Time Division Multiple Access:'''In this system each user is allocated a different time slot.Forward link frequency and reverse link frequency is the same. A synchronous switch is responsible to do the time switching.<br /> [[Image:cdma10.jpg]]<br /> '''Code Division Multiple Access:'''There is no restriction on time and frequency in this scheme. All the users can transmit at all times and at all frequencies. Because users are isolated by code, they can share the same carrier frequency, eliminating the frequency reuse problem encountered in other technologies.&lt;br&gt;<br /> [[Image:cdma11.jpg|600 px|centre]]&lt;br&gt;<br /> A comparative study between the above three access technologies with respect to time and frequency is as shown below&lt;br&gt;.<br /> [[Image:cdma12.jpg|600 px|centre]]<br /> <br /> ==Code Division Multiple Access==<br /> The CDMA technology can be implemented in two ways<br /> * Direct Sequence Spread Sprectrum - DSSS CDMA<br /> * Frequency Hopping - FH CDMA<br /> '''Direct Sequence Spread Sprectrum - DSSS CDMA:''' In this method the direct sequence(input data) which is spread over a limited bandwidth is multiplied with a code or spreading sequence (a pseudorandom sequence) which will spread the input data over the entire bandwidth of the communication channel. The power density is also reduced and is spread over the frequency spectrum and hence is known as spread spectrum method. The modulation part of DSSS is as shown below&lt;br&gt;<br /> [[Image:cdma13.jpg]]<br /> The modulated signal is transmitted over the channel and all users can receive it but only the user which knows the correct code can only decode the message. This is depicted in the figure below.&lt;br&gt;<br /> [[Image:cdma14.jpg]]<br /> ===Features of CDMA===<br /> ====Frequency Reuse==== <br /> Number of radio channel frequencies are limited. The concept of frequency reuse is based on assigning to each cell a group of radio channels used within a small geographic area. Cells are assigned a group of channels that is completely different from neighboring cells. The coverage area of cells is called the footprint. This footprint is limited by a boundary so that the same group of channels can be used in different cells that are far enough away from each other so that their frequencies do not interfere.<br /> <br /> ====Soft Handoff==== Handoff means Switching a cellular phone transmission from one cell to another as a mobile user moves into a new cellular area. It is so called because the radio link with the previous sector(s) is not broken before a link is established with a new sector; this type of handoff is described as &quot;make before break&quot;. In CDMA due to this soft handoff there is no interruption of call even at the border of cell site which means more number of customers can be accommodated automatically increasing the capacity of the cell site.<br /> <br /> ====Multipath Fading==== In a mobile environment a mobile station will receive one direct signal from the base station and multiple signals which are reflected from obstructions like building and towers. Each signal would have travelled a different length and would be displaced in time. Due to this when they are combined at the mobile it will cause interference resulting in poor signal quality. This is called as fading. This problem is handled in a very good way in CDMA. Here the phase of the multiple signals is modified such the only positive interference(addition) takes place the overall signal strength increases. A receiver that implements the above principle is known as a RAKE receiver as shown in the figure below&lt;br&gt;<br /> [[Image:cdma15.jpg]]<br /> ====Near Far Problem==== The problem is described by taking an example consider a receiver and two transmitters (one close to the receiver; the other far away). If both transmitters transmit simultaneously and at equal powers, then due to the inverse square law the receiver will receive more power from the nearer transmitter. This makes the farther transmitter voice more difficult to understand. Since one transmission's signal is the other's noise the signal-to-noise ratio (SNR) for the farther transmitter is much lower. If the nearer transmitter transmits a signal that is orders of magnitude higher than the farther transmitter then the SNR for the farther transmitter may be below detectability and the farther transmitter may just as well not transmit. This effectively jams the communication channel. In CDMA systems this is commonly solved by dynamic output power adjustment of the transmitters. That is the closer transmitters use less power so that the SNR for all transmitters at the receiver is roughly the same. This sometimes can have a noticeable impact on battery life, which can be dramatically different depending on distance from the base station.&lt;br&gt;<br /> [[Image:cdma16.jpg]]<br /> ====Power Control:==== As the propagation losses between BS and MS's are different according to individual communication distances, the received levels at the base station are different from each other when all mobile stations transmit their signals at the same power. Moreover, the received level fluctuates quickly due to fading. In order to maintain the strength of received signal level at BS, power control technique must be employed in CDMA systems.&lt;br&gt;.<br /> [[Image:cdma17.jpg]]&lt;br&gt;<br /> Power control can be implemented in two ways : open loop power control and closed loop power control&lt;br&gt;<br /> [[Image:cdma18.jpg]]<br /> <br /> '''Effect of Power Control''' Power control is capable of compensating the fading fluctuation. Received power from all MS are controlled to be equal.　Near-Far problem is mitigated by the power control.<br /> [[Image:cdma19.jpg]]<br /> ==Quality of Service(QoS)==<br /> CDMA is being accepted as a third generation system and a specific feature of 3G system is that it offers a radio interface adapted for all kinds of services and combination of services(data,voice,image etc). The big issue is of multiplexing of these services which have do not have the same demands in terms of quality of service(QoS) which can be represented as BER(bit error rate),processing delay,frame error rate etc. Different QoS will require different channel encoding and interleaving strategies. The demand of BER can be satisfied when the coding bits have atleast a code dependent ratio Eb/I(ratio of bit energy to interference). There are several influences that might change system performance(BER) and hence Eb/I ratio, of which the most effective is variation of Bit Rate by a step of '''Rate Matching'''. &lt;br&gt;&lt;br&gt;<br /> ===Rate Matching and QoS===<br /> The patent '''EP 1385290 titled Method for balancing Eb/I ratio in a service multiplexing CDMA system and a telecommunication system using this method''' targets at this concept of Rate matching and introduces an algorithm of calculating effective data output bits by a process of repetition or puncturing of the input bits governed by a '''rate matching ratio''' and '''puncturing ratio''' received from the sending entity(can be BS or MS). The following framework highlights the various steps involved in providing variable QoS.<br /> <br /> ===Power Control, Rate Matching and QoS===<br /> According to one of the methods of dynamic power control (Code Hopping) used in W-CDMA technology, the Rate Information (RI) field in the uplink control channel in W-CDMA frame can be used to notify the base station about the variable bit rates (VBR) it wants to send, then the base station computes and assigns optimal powers according to the new spreading factor for each radio frame. Spreading factor(Gi) is defined as the ratio of bandwidth of the system to the data rate of the radio frame.<br /> Mathematically,&lt;br&gt;<br /> '''Gi = W / Ri''',where W=system bandwidth which is a constant for a system and Ri= data rate of radio frame.&lt;br&gt;<br /> A power index (gi) is calculated from this Spreading Factor(Gi) using the following expression&lt;br&gt;<br /> '''gi= (gi / (gi+Gi))''', where gi is minimum QoS for the ith session which is a constant.&lt;br&gt; <br /> This power index will ascertain the optimal power to be alloted to each service channel.&lt;br&gt; <br /> '''Pi = (gi*No*W )/ (Hi*(1-(Sgj)'''&lt;br&gt;<br /> where No is AWGN(Additive White Guassian Noise)a constant,&lt;br&gt; Hi is path loss which is dependent on the distance and is a costant for a path,&lt;br&gt; and Sgj is sum of the power index of all the sessions which is constant for all sessions of the radio frame. &lt;br&gt;<br /> From the above analysis, we observe that Bit Rate is inversely proportional to Spreading factor which will inversely effect the power index and hence the optimal power. Therefore, the Bit Rate and Optimal power go hand in glove and have the same effect on Eb/I and QoS.<br /> The method and algorithm to schedule optimal power is detailed in the IEEE paper '''Dynamic Resource Scheduling for Variable QoS Traffic in W-CDMA Ozgur Gurbuz, Henry Owen'''. <br /> Thus we conclude that by adjusting the optimal power we are actually trying to implement a rate matching step.<br /> [[Media:ieee1.pdf]]<br /> <br /> ===Power control and QoS===<br /> SPEECH transmission is the main service supported by the first two generations of mobile communication systems. However, future systems should be able to handle a wide variety of different services with bit rate requirement ranging from a few kilobits/s to as much as 2 Mb/s. There are many ways to design a CDMA system to support multirate services . One way to do so is to spread all signals, independent of the bit rate, to the same bandwidth . This is done by keeping the chip rate constant. Users transmitting at low bit rate thus have a high processing gain. This allows those users to transmit at a lower power. Therefore, the conventional constant received power scheme is not appropriate in such a multirate system. A more sophisticated power control scheme is needed to achieve diverse quality of service (QoS) and rate requirement. One such scheme which explores the relationship between the data rate, the QoS, and the transmit power is presented in the IEEE paper '''Power Control and Rate Management for Wireless Multimedia CDMA Systems Chi Wan Sung, Member, IEEE, and Wing Shing Wong, Senior Member, IEEE.'''<br /> ===Dynamic Resource Scheduling and QoS===<br /> Dynamic Resource Scheduling (DRS) has been proposed as an adaptive resource management and QoS<br /> provisioning framework applicable to W-CDMA systems. Various spreading strategies like Fixed Spreading Gain (FSG), Variable Spreading Gain (VSG) and Multi Code (MC) strategies and their performance is compared in terms of power saving, resource allocation and QoS stability in the IEEE paper '''DYNAMIC RESOURCE SCHEDULING STRATEGIES FOR QOS IN W-CDMA by Ozgur Gurbuz, Henry Owen.''' VSG-DRS and MC-DRS outperform the FSG-DRS for capacity as a result of the statistical multiplexing gain created by adaptive bandwidth usage.<br /> <br /> ==Conclusion==<br /> Substantial amount of research has been done in the field of QoS in CDMA communication system in the year 1998-99 and this has led to the invention of multitude of methodologies ranging from power control to Rate matching and so on with the sole aim of improving QoS.</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Main_Page&diff=1794 2006-06-26T07:08:39Z

<p>67.180.226.207: /* Dolcera Reports */</p> <hr /> <div>= Dolcera Reports =<br /> <br /> * [[Hybrid Electric Vehicle Battery System]]<br /> * [[Alopecia - Hair Loss]]<br /> * [[Supply Chain RFID Applications]]<br /> * [[Quality of Service on CDMA platforms]]<br /> <br /> = Dolcera Offerings =<br /> * [[Dolcera Offerings]]</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Template:CaseStudy&diff=1783 2006-06-25T15:00:06Z

<p>67.180.226.207: </p> <hr /> <div>{| style=&quot;border:1px solid #AAA; background:#E9E9E9;width:75%&quot; align=&quot;center&quot;<br /> |-<br /> |'''Client:''' || {{{client}}}<br /> |- <br /> |'''Goal:''' || {{{goal}}}<br /> |-<br /> |'''Duration:''' || {{{duration}}}<br /> |-<br /> |'''Result:''' || {{{result}}}<br /> |-<br /> |'''Savings:''' || {{{customer_savings}}}<br /> |- <br /> |'''Example:''' || {{{sample_links}}}<br /> |-<br /> |'''Dolcera advantage:''' || '''{{{dolcera_advantage}}}'''<br /> |-<br /> |'''Client quote:''' || ''&quot;{{{quote}}}&quot;''<br /> |}</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Dolcera_Offerings&diff=1782 2006-06-25T14:59:08Z

<p>67.180.226.207: </p> <hr /> <div>Dolcera's mission is to provides information integration and outsourced research services for decision support. Our services are targeted towards multiple types of '''knowledge workers''' within organizations including:<br /> * senior executives and strategists<br /> * researchers, engineers and technologists<br /> * marketers and brand managers<br /> * attorneys<br /> <br /> The Dolcera team has expertise in:<br /> * Technology analysis in the areas of chemistry, biotechnology, computer software, electronics, communication and mechanical engineering.<br /> * Market research - primary and secondary - across multiple industries <br /> * Information integration for large sets of structured and unstructured data<br /> * Collaboration tools and technology including wikis, blogs and Web 2.0<br /> <br /> Here is a list of Dolcera services for various roles within an organization:<br /> <br /> {| class=&quot;wikitable&quot; style=&quot;font-size:120%&quot; border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; <br /> |- style=&quot;background:lightgrey&quot;<br /> ! Offering !! Goal !! Client !! Role !! Demo<br /> |-<br /> ! [[#Technology reports| Technology reports]] <br /> | 360-degree view of technology and market data || Technology company || Researcher || [http://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV report] <br /> |-<br /> ! [[#IPMaps | IPMaps]] <br /> | Comprehensive view of a particular research area || Law firms, corporations || Researcher || [http://www.dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Satellite Antenna IPMap] <br /> |-<br /> ! [[#Timelines | Timelines]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Business plans | Business plans]] <br /> | Integrated timeline of technologies, standards and patents || Corporations || Executive || [http://www.dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Timeline view] <br /> |-<br /> ! [[#Executive dashboard| Executive dashboard]] <br /> | Up-to-date snapshot of market+competitive data || Large corporation || Executive || [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID dashboard] <br /> |-<br /> ! [[#Brand dashboard | Brand dashboard]] <br /> | Integrated market information for a brand || Consumer products company || Brand Manager || [http://www.dolcera.com/ipmapdemo/brand%20manager%20dashboard.swf Brand dashboard] <br /> |-<br /> ! [[#Collaboration services | Collaboration services]]<br /> | Multi-way interaction platform for research, marketing and manufacturing groups || Medium and large companies || Knowledge worker ||[http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html Interactive reports] <br /> |}<br /> __NOTOC__<br /> &lt;div id=&quot;Technology reports&quot;&gt;<br /> <br /> == Technology reports ==<br /> Dolcera team prepares technology reports on important areas of research and development. These reports comprehensively cover:<br /> * Technology and research developments,<br /> * Market factors, and<br /> * Intellectual property aspects<br /> <br /> The unique aspects of Dolcera's technology reports are:<br /> * High quality of technology and market analysis,<br /> * Interactive development in partnership with client, and<br /> * Continuous updates <br /> <br /> [[Image:report_sample.jpg|thumb|500px|center|[http://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss Alopecia report]]]<br /> <br /> ==== Case study: Technology reports ====<br /> {{CaseStudy<br /> | topic = Technology reports<br /> | client = A large medical device company<br /> | goal = Create a technology report on one of the newest types of cardiac devices. Integrate data from a variety of data sources.<br /> | duration = Intial preparation - 4 weeks<br /> | result = The Dolcera report was shared between the research, marketing and legal groups within the client corporation. Dolcera also provides monthly updates for this report.<br /> | customer_savings = Approximately 1/8th of the cost <br /> | dolcera_advantage = Multi-disciplinary data integration, rapid results, low costs<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System Hybrid Electric Vehicle report]<br /> | quote = We can collaborate easily.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;IPMaps&quot;&gt;<br /> <br /> == IPMaps ==<br /> Dolcera IPMaps present the comprehensive view of intellectual property in a particular area. Prepared by highly-trained technical analysts, Dolcera IPMaps are:<br /> * Comprehensive<br /> * Interactive<br /> * Visually clear-cut<br /> * Database-driven<br /> <br /> [[Image:Satellite_Antenna_IPMap.jpg|thumb|500px|center|[http://www.dolcera.com/ipmapdemo/satellite_antenna/impamp.html Satellite Antenna IPMap]]]<br /> ==== Case study: IPMaps ====<br /> {{CaseStudy<br /> | topic = IPMaps<br /> | client = A Fortune 500 software company<br /> | goal = Provide an overview of the company's patent portfolio in a key technology area.<br /> | duration = 2 weeks<br /> | result = The Dolcera IPMap integrated patent and competitive information from a variety of sources in one 'snapshot' IPMap that was used by the client for validating the market space and their own research strength.<br /> | customer_savings = Approximately 1/5th of the cost <br /> | dolcera_advantage = Data integration, technology expertise, speed, low costs<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/rfid/ipmap.html RFID IPMap], [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Hair loss IPMap], [http://www.dolcera.com/ipmapdemo/multimodal_apps/ipmap.html Multimodal applications IPMap]<br /> | quote = You showed us how small this market is. We would not have entered this market if we had this information in advance.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Timelines&quot;&gt;<br /> == Timelines ==<br /> Certain fields of research progress at bewildering speeds. It is often impossible for researchers, technology experts and executives alike to keep track of the developments. Dolcera timelines are exactly what their name implies: interactive visual maps that show the development of a field over the course of time. Our timelines are used for a variety of purposes including:<br /> * Understanding the development of a field of science/technology<br /> * Determining the contributions of individuals/companies to <br /> * Juxtaposing market and technology developments<br /> <br /> [[Image:timeline_sample.jpg|thumb|500px|center|Sample timeline]]<br /> ==== Case study: Timelines ====<br /> {{CaseStudy<br /> | topic = Timelines<br /> | client = A major N. American smartphone manufacturer<br /> | goal = Determine inventorship of some of the most important cellular telephony standards by analyzing patent, standard and market data.<br /> | duration = 4 weeks<br /> | result = Dolcera timelines, based on research through several gigabytes of standards meetings minutes, specifications and patents, allowed the client to negotiate with their competitors.<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Powerful search tools, data integration from disparate sources, succinct presentation<br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/taxonomy_timeline.htm Sample timeline]<br /> | quote = I did not even have to lift a finger to understand the information... I used your presentation for my company's Board (of Directors).<br /> }}<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Business plans&quot;&gt;<br /> == Business plans ==<br /> Dolcera works in partnership with research and development groups within companies to help them understand the business opportunities for their research. We develop full-strength business plans with:<br /> * Commercialization possibilities for research<br /> * Competitive landscape<br /> * SWOT Analysis: Strengths, Weaknesses, Opportunities, Threats<br /> <br /> [[Image:swot_sample.jpg|thumb|250px|center|SWOT Analysis]]<br /> ==== Case study: Business plans ====<br /> {{CaseStudy<br /> | topic = Business plans<br /> | client = A global software company<br /> | goal = Create business case for a research project with several patent applications<br /> | duration = 6 weeks<br /> | result = Complete business plan including market research, financial plan, competitive analysis, product positioning, product and need characteristics<br /> | customer_savings = Approximately 1/10th of the cost<br /> | dolcera_advantage = Strong technology and business expertise to help researchers shorter innovation cycle<br /> | sample_links = [http://dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System HEV Report]<br /> | quote = Dolcera is an integral part of our research commercialization strategy.<br /> }}<br /> &lt;/div&gt;<br /> <br /> &lt;div id=&quot;Executive dashboard&quot;&gt;<br /> <br /> == Executive dashboard ==<br /> The Dolcera executive IP dashboard provides an integrated view of all the key performance indicators for your organization's intellectual property, including:<br /> * Patent filings<br /> * Patent licensing opportunities<br /> * Patent threats<br /> * Competitive position<br /> * Key IP performance indicators<br /> <br /> The interactive executive IP dashboard allows users to perform their own what-if analysis. Behind the scenes, the Dolcera team performs extensive research and market+competitive analysis to drive the executive dashboard and keep it up-to-date.<br /> <br /> &lt;gflash&gt;600 600 http://dolcera.com/ipmapdemo/rfid_model.swf&lt;/gflash&gt;<br /> <br /> ==== Case study: Executive dashboard ====<br /> {{CaseStudy<br /> | topic = Executive dashboard<br /> | client = A US medical device major<br /> | goal = Provide a central point of entry for all corporate IP performance indicators<br /> | duration = Ongoing<br /> | result = All patent information in one spot, and shared by all stakeholders within the organization.<br /> | customer_savings = Greater overall visibility improves response time considerably<br /> | dolcera_advantage = Correlating market movements with IP information and technology trends<br /> | sample_links = [http://www.dolcera.com/ipmapdemo/alopecia_model.swf Consumer products dashboard], [http://www.dolcera.com/ipmapdemo/rfid_model.swf RFID Dashboard]<br /> | quote = The dashboard helps our team think strategically.<br /> }}<br /> &lt;/div&gt;<br /> &lt;div id=&quot;Brand dashboard&quot;&gt;<br /> == Brand dashboard ==<br /> The brand manager dashboard is a new Dolcera offering targeted towards marketing teams within consumer products, pharmaceutical and automotive companies that organize their product strategies around strong brands and monitor them relentlessly.<br /> <br /> The dashboard identifies the impact of global and local events on client's and competitor's brands. It brings together data from a variety of data sources. It also includes data collected through sampling blogs, social networking sites and other non-traditional media sources.<br /> <br /> &lt;gflash&gt; 600 600 http://www.dolcera.com/ipmapdemo/brand manager dashboard.swf&lt;/gflash&gt;<br /> <br /> &lt;/div&gt;<br /> &lt;div id=&quot;Collaboration services&quot;&gt;<br /> == Collaboration services ==<br /> Dolcera provides a range of collaboration services for large organizations. The collaboration services include:<br /> * Wiki and other collaboration tools setup<br /> * Taxonomy design and updates<br /> * Collaboration/knowledge processes design<br /> * Ongoing updates with latest tools<br /> <br /> [[Image:taxonomy.jpg|thumb|300px|center|Dolcera taxonomy tool]]<br /> <br /> ==== Case study: Collaboration services ====<br /> {{CaseStudy<br /> | topic = Collaboration services<br /> | client = Large pharmaceutical company<br /> | goal = Provide a central Human Resources forms and document system for the corporate intranet.<br /> | duration = 2 months<br /> | result = We prepared the taxonomy and classification system for all documents and classified the documents initially. We also trained clients to update the documents on an ongoing basis.<br /> | customer_savings = Approximately $300,000 for the project<br /> | dolcera_advantage = Best-in-class technology and processes, ably supported by our technical team in India <br /> | sample_links = [http://dolcera.com/ipmapdemo/satellite_antenna/ipmap.html IPMap]<br /> | quote = Our goal is to be a smarter organization, and Dolcera helped us achieve it.<br /> }}<br /> <br /> &lt;/div&gt;<br /> <br /> <br /> == Questions Dolcera answers ==<br /> We help you answer questions such as:<br /> {| border=&quot;1&quot; cellpadding=&quot;5&quot; cellspacing=&quot;0&quot; align=&quot;center&quot; valign=&quot;top&quot;<br /> |-<br /> | <br /> * '''What’s hot'''<br /> ** What technology/approaches are the most promising?<br /> ** What technology/approaches have already been tried?<br /> ** What can I license?<br /> ** Is any empirical data available?<br /> * '''Where should I focus my R&amp;D investment'''<br /> ** Where’s the ‘white space’ for me to play in?<br /> * '''Any hints for research'''<br /> ** Are there any combinations I could develop?<br /> | <br /> * '''What should I do in this geography'''<br /> ** What are my competitors up to in this geography?<br /> ** What are my strengths/ weaknesses here?<br /> * '''What’s my competition up to'''<br /> ** What’s my top competitor investing in?<br /> ** Are there any loopholes in their strategy?<br /> ** Will a competitor emerge from nowhere and surprise me?<br /> ** What are the crowded areas?<br /> * '''How do I play defense'''<br /> ** What should my blocking/reactive strategies be?<br /> |}</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Main_Page&diff=1781 2006-06-25T14:58:54Z

<p>67.180.226.207: /* Dolcera Offerings */</p> <hr /> <div>= Dolcera Reports =<br /> <br /> * [[Hybrid Electric Vehicle Battery System]]<br /> * [[Alopecia - Hair Loss]]<br /> * [[Supply Chain RFID Applications]]<br /> <br /> = Dolcera Offerings =<br /> * [[Dolcera Offerings]]</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Main_Page&diff=1780 2006-06-25T14:58:26Z

<p>67.180.226.207: </p> <hr /> <div>= Dolcera Reports =<br /> <br /> * [[Hybrid Electric Vehicle Battery System]]<br /> * [[Alopecia - Hair Loss]]<br /> * [[Supply Chain RFID Applications]]<br /> <br /> = Dolcera Offerings =</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss&diff=1779 2006-05-21T01:54:51Z

<p>67.180.226.207: /* Structure-Activity Relationships (SARs) of Finasteride */</p> <hr /> <div>{{TOCrightEx}}<br /> == Rationale ==<br /> * &quot;Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year.&quot; March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55]<br /> <br /> * &quot;An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries.&quot; February 16, 2006 – [http://stophair.setupmyblog.com/]<br /> <br /> * &quot;There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting.&quot; June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&amp;STORY=/www/story/06-07-2005/0003821470&amp;EDATE=]<br /> <br /> == Alopecia IPMap == <br /> [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Dolcera IPMap for Alopecia]<br /> <br /> == Introduction ==<br /> <br /> === Hair Basics ===<br /> * Hair is a complex and delicate part of the body.<br /> * Keeping it healthy and beautiful is a challenge.<br /> * Hair grows everywhere on the body with the exception of the lips, eyelids, the palms of the hands and soles of the feet.<br /> * Hair is basically a form of skin. <br /> * Hair is made up of a protein called keratin.<br /> * Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin. <br /> * Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htm]<br /> * Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.html]<br /> [[Image:Hairbasics.jpg|thumb|center|500px|Structure of Hair root and Hair bulb]]<br /> <br /> === What causes Hair loss? === <br /> * Decreased growth of the hair <br /> * Increased shedding of the hair <br /> * Breakage of hairs <br /> * Conversion of thick terminal hairs to thin vellus hairs <br /> [[Image:Facts.jpg|thumb|right|400px|Survey results from Japan]]<br /> Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed '''“Male Pattern Baldness&quot;''' or '''&quot;Androgenetic Alopecia&quot;'''.<br /> <br /> === Androgenetic Alopecia ===<br /> * Gradual Onset.<br /> * Transition from large, thick, pigmented terminal hairs to thinner, shorter, indeterminate hairs and finally to short, wispy, nonpigmented vellus hairs in the involved areas.<br /> * Characterised by a receding hairline and/or hair loss on the top of the head.<br /> <br /> '''Main Causes'''<br /> * Genetic predisposition<br /> * Hormonal effect of androgen <br /> * Reduction of blood circulation around hair follicle<br /> * Deactivation of hair matrix cells<br /> <br /> '''Some facts from Japan''' <br /> <br /> * Market size: ¥ 30 Billion<br /> * Number of products: more than 100<br /> <br /> (JICST-EPlus - Japanese Science &amp; Technology)<br /> <br /> == Goals ==<br /> <br /> The goal of this report is to:<br /> * Summarize IP activity over the years<br /> * Identify major players<br /> * Conduct patent analysis<br /> a) Composition<br /> b) Nature<br /> c) Action<br /> <br /> '''And then'''<br /> <br /> * Analyze patents pertaining to high sebum activity<br /> <br /> == Approach ==<br /> <br /> * A broad search was conducted on hair loss patents.<br /> * Patent information was sourced through SIP.<br /> * A set of patents was selected for analysis.<br /> <br /> Composition of treatment for causes are identified and categorized as follows:<br /> <br /> * Anti-androgen<br /> * Minoxidil<br /> * Double action (Anti-androgen + Mindoxidil)<br /> * Hair matrix cells activator<br /> * Sebum production inhibitor<br /> <br /> == IP activity over years ==<br /> The graph indicates:<br /> * Number of patents filed every 5 years (except for first 7 years).<br /> * First solution proposed in 1973<br /> * Filing trend indicates steep rise in activity recently.<br /> [[Image:Year1.jpg|thumb|center|400px|IP Activity over years]]<br /> <br /> == Major Players ==<br /> [[Image:players.jpg|thumb|left|400px|Assignees with more than 20 patents ]]<br /> [[Image:players1.jpg|thumb|center|400px|Assignees with fewer than 20 patents ]]<br /> <br /> * '''Active Assignees'''<br /> Assignees currently active with more than 5 patents to their credit during 2000-2005. <br /> * Warner with 9 patents,<br /> * Bristol with 6 and<br /> * Abbott with 5.<br /> <br /> [[Image:Active.jpg|thumb|center|500px|Active Assignees]]<br /> <br /> == Anti-androgens == <br /> * Anti-androgens are used in hormone therapy.<br /> * Anti-androgens are designed to affect the hormones made in the adrenal glands. They don't stop the hormones from being made, but they stop them from having an effect leading to hair loss.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Testosterone is reduced to its active metabolite, Dihydrotestosterone (DHT) by the enzyme 5 alpha reductase.<br /> * DHT attaches to androgen receptor sites at the hair follicle. <br /> * DHT causes gradual miniaturization of the follicle, which eventually results in hair loss.<br /> <br /> '''How do anti-androgens treat hair loss?'''<br /> * Anti-androgens compete with DHT to bind to the androgen receptor.<br /> * Upon binding of anti-androgen in place of DHT, follicle miniaturization is lowered and hair loss prevented.<br /> <br /> === Functions of Anti-androgen === <br /> [http://www.revivogen.com/revivogen/work.html Anti-androgen]<br /> <br /> [[Image:Andogen1.jpg|thumb|center|500px|Functions of Anti-androgen]]<br /> <br /> === IP Map for Anti-androgen ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;8&quot;, style=&quot;#008080&quot;<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> BLOTECH (2004)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Palmetto berry extract (fatty acids &amp; sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans)<br /> |bgcolor=LightCyan|Fatty acids – Inhibit testosterone<br /> Sterols - Mechanism of action unknown.<br /> <br /> Quercetin results in cell growth cycle.<br /> <br /> Beta-sitosterol reduce inflammation on scalp<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 4-cycloalkoxy benzonitrile derivatives and salts<br /> |bgcolor=LightCyan|Acts as androgen receptor modulators and blocks formation of DHT.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives.<br /> |bgcolor=LightCyan|The compounds inhibit, or decrease, activation of androgen receptor by androgens.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> APHIOS Corp (2003)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives.<br /> |bgcolor=LightCyan|Modulates androgenic activity by inhibiting 5.alpha.-reductase activity.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> Fundacion Pablo Cassara (2003)<br /> |bgcolor=LightCyan|Nucleotide<br /> |bgcolor=LightCyan|Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond)<br /> |bgcolor=LightCyan|Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> PFIZER INC (2001)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate <br /> |bgcolor=LightCyan|Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> N/A (1995)<br /> |bgcolor=LightCyan|Peptides/nucleic acid<br /> |bgcolor=LightCyan|Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein)<br /> |bgcolor=LightCyan|Inhibit synthesis of bradykinin receptors or compounds by binding to B2 receptor<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> KAO Corp (1987)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Walnut extract (leaves/pericarps) with an organic solvent<br /> |bgcolor=LightCyan|Blocks formation of DHT<br /> |}<br /> <br /> == Minoxidil ==<br /> * Minoxidil is a &quot;potassium channel opener&quot; that leads to vasodilation.<br /> * The drug is available in two forms. Oral minoxidil is used to treat high blood pressure and the topical solution form is used to treat hair loss and baldness.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * A thick network of tiny veins and arteries lines the outer wall of the follicle. Blood pumps through the bulb and hair via this network.<br /> * DHT accumulates in the hair follicles and roots, constricting the blood supply of oxygen and nutrients to the hair roots; which is also seen to possibly contribute towards hair loss.<br /> <br /> '''How does Minoxidal treat hair loss?'''<br /> * Minoxidal is applied to the scalp topically, where it dilates blood vessels in the scalp and sustains the hair follicles for longer period of time.<br /> * Scientists and researchers are not exactly sure of how Minoxidil leads to this effect.<br /> * Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.<br /> <br /> === Functions of Monoxidil === [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 Minoxidil]<br /> <br /> [[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil]]<br /> <br /> === IP Map for Minoxidil ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> WARNER LAMBERT(2002)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Benzopyran compounds<br /> |bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> LG HOUSEHOLD &amp; HEALTH CARE(2001)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Sophora flavescens extract (alkaloids &amp; flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)<br /> |bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels<br /> |}<br /> <br /> == Double action (Anti-androgen + Minoxidil) ==<br /> * Combination of Minoxidil + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.<br /> <br /> <br /> '''What is the problem with using only Anti-androgen therapy?'''<br /> * Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.<br /> * Anti-androgen only prevent binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.<br /> <br /> '''What is the problem with using only Minoxidal therapy?'''<br /> * Minoxidil-based products are generally not effective in stopping hair loss as minoxidil does not block the harmful effects of DHT in the scalp and hair follicles. <br /> * Minoxidil simply dilates blood vessels in the scalp. However, the harmful DHT is still being produced in the body and still getting into the scalp and hair follicles and causing eventual hair loss.<br /> <br /> '''How is the combination of Anti-androgens and Minoxidil effective?'''<br /> * Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.<br /> * Minoxidil causes vasodilation and therefore improves supply of oxygen and nutrients to the hair follicle and roots.<br /> * Combination therapy therefore proves to be much more effective than individual therapy.<br /> <br /> === Functions of (Anti-androgen + Minoxidil) === [http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]<br /> [[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Minoxidil)]]<br /> <br /> === IP Map for (Anti-androgen + Minoxidil) ===<br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405] <br /> N/A(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhance and sunscreen<br /> |bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577] <br /> L'OREAL(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP<br /> |bgcolor=LightCyan|Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762] <br /> COLOMER GROUP(1999)<br /> |bgcolor=LightCyan|Natural extract<br /> |bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)<br /> |bgcolor=LightCyan|Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp<br /> |}<br /> <br /> <br /> == Hair matrix cell activator ==<br /> Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.<br /> * Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.<br /> * Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.<br /> * Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.<br /> <br /> <br /> '''How does hair cell matrix activator treat hair loss?'''<br /> * Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.<br /> * This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.<br /> * Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.<br /> <br /> === Functions of Hair matrix cell activator === [http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]<br /> [[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]<br /> <br /> === IP Map for Hair matrix cell activator ===<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> SHISEIDO(1999) <br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt<br /> |bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> L'OREAL(1998) <br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions<br /> |bgcolor=LightCyan|Reducing the expression of MMPs (Metalloproteases) in the scalp - slow down or inhibit the degradation of the perifollicular matrix (extracellular matrix surround the hair follicle) <br /> |}<br /> <br /> == Sebum Production Inhibitor ==<br /> Sebum Production Inhibitor is a substance that prevents the synthesis of sebum, mixture of lipid substances.<br /> <br /> '''What causes hair loss?'''<br /> * Sebum is a fatty acid substance secreted from sebaceous glands associated with hair follicles.<br /> * Hair can get heavy sebum build-up and mixes with cholesterol to form a hardened plug around the bottom part of the hair bulb.<br /> * Hardened plugs prevent cell respirations and eventually lead to hair loss.<br /> * Bacteria will also attach to the hardened plug and this can also cause further cause problems with hair growth.<br /> <br /> '''How does Sebum production inhibitor treat hair loss?'''<br /> * The inhibitor prevents synthesis of sebum and slows down accumulation and mixing of sebum with cholesterol leading to hardened plugs. <br /> * Reduction of sebum results in unclogged hair follicles/bulbs and allows oxygen and nutrients from reaching the hair follicle.<br /> * Reduction in sebum also prevents vasoconstriction.<br /> * Sum result of these effects of Sebum production inhibitor is prevention of hair loss.<br /> <br /> <br /> * The inhibitor blocks the excessive sebum production produces greasy effect on hair and scalp and also responsible for thinning and loosing of hair.<br /> <br /> === Functions of Sebum Production Inhibitor ===<br /> [[http://en.wikipedia.org/wiki/Image:HairFollicle.jpg Sebum Production Inhibitor]]<br /> [[Image:Sebum1.jpg|thumb|center|500px|Functions of Sebum Production Inhibitor]]<br /> <br /> === IPMap for Sebum Production Inhibitor ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699] <br /> Unilever(2005)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Polyamine (putrescine, spermine or spermidine) analogs and/or derivatives; DFMO; N-acetyl cysteines; neutralized salts of a non-hydroxy C2-C40 dicarboxylic acids, preferably malonate salts; and mixtures thereof. <br /> |bgcolor=LightCyan|Decreasing sebum production and/or pore size <br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362] <br /> KAO COPR.(2004)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Avocado oil (Butyl esters of fatty acids) <br /> |bgcolor=LightCyan|Reduce sebum of the hair and scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587] <br /> Unilever(1982)<br /> |bgcolor=LightCyan|organic compound<br /> |bgcolor=LightCyan |Biotin antagonist or a salt thereof <br /> |bgcolor=LightCyan|Decrease activity of the enzyme acetyl-SCoA-carboxylase and hence reduce lipid synthesis in sebaceous glands so that less sebum is produced <br /> |}<br /> <br /> == Composition nature matrix ==<br /> <br /> === IPMap: Composition nature matrix ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;11&quot;, style=&quot;#008080&quot;<br /> !width=&quot;50&quot; bgcolor=DodgerBlue|'''Year'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Organic Compound'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extracts''' <br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Peptides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nucleotides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extract + Organic comp'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|2005 <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |- <br /> |bgcolor=LightCyan|2004 <br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|BLOTECH (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |- <br /> |bgcolor=LightCyan|2003<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|APHIOS (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|FUNDIACION (1)<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2002<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2001<br /> |bgcolor=LightCyan |PFIZER (1)<br /> |bgcolor=LightCyan|LG HEALTH-CARE (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2000<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1) / N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1999<br /> |bgcolor=LightCyan|SHISEDIO (1)<br /> |bgcolor=LightCyan|COLOMER (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1998<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1995<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |-<br /> |bgcolor=LightCyan|1987<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1982<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |}<br /> <br /> == Focus of patents ==<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;17&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Focus of patents'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Stimulating hair growth using benzopyrans<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Compositions to prevent or reduce hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Method of decreasing sebum production and pore size<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699 ]<br /> |bgcolor=LightCyan|16<br /> |- <br /> |bgcolor=LightCyan|Method for reducing sebum on the hair and skin<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |bgcolor=LightCyan|17<br /> |}<br /> <br /> === Focus of patents by technology ===<br /> [[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]<br /> <br /> == Distribution of patents ==<br /> <br /> === By patent types ===<br /> [[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]<br /> <br /> <br /> === By key ingredients ===<br /> [[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]<br /> <br /> === By target disease ===<br /> [[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]<br /> <br /> <br /> === Key ingredients vs. Target disease ===<br /> [[Image:key&amp;target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]<br /> <br /> <br /> === Target species ===<br /> [[Image:Species.jpg|thumb|center|700px|Target species]]<br /> <br /> <br /> === Mode of administration ===<br /> [[Image:Mode.jpg|thumb|center|700px|Mode of administration]]<br /> <br /> <br /> === Product type vs. Product form ===<br /> [[Image:prod.jpg|thumb|center|700px|Product type vs. Product form]]<br /> <br /> == Distribution based on different aspects ==<br /> <br /> === List of patents ===<br /> {| border=&quot;1&quot; cellpadding=&quot;9&quot;, style=&quot;#008080&quot;<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|1<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|10<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |- <br /> |bgcolor=LightCyan|2<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|11<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |- <br /> |bgcolor=LightCyan|3<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> |bgcolor=LightCyan|12<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |- <br /> |bgcolor=LightCyan|4<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427] <br /> |bgcolor=LightCyan|13<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |- <br /> |bgcolor=LightCyan|5<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282] <br /> |bgcolor=LightCyan|14<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |- <br /> |bgcolor=LightCyan|6<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467] <br /> |bgcolor=LightCyan|15<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |- <br /> |bgcolor=LightCyan|7<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|16<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699]<br /> |- <br /> |bgcolor=LightCyan|8<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|17<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |- <br /> |bgcolor=LightCyan|9<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010] <br /> |bgcolor=LightCyan|18<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |}<br /> <br /> === Patents by target diseases ===<br /> {| border=&quot;1&quot; cellpadding=&quot;16&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Target disease/ disorder'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness)<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, male pattern baldness and female pattern baldness<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|Inappropriate activation of the androgen receptor, acne, oily skin, alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Androgen-associated hair loss and androgen-skin related disorders. <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Androgenetic or androgenic alopecia or androgeno-genetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Diseases caused by testosterone (male-pattern alopecia)<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Alopecia, androgenic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Androgenetic, androgenic or androgenogenetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Curing other scalp related problems<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |bgcolor=LightCyan|16<br /> |}<br /> <br /> === Patents by application ===<br /> [[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]<br /> <br /> === Signaling Pathway and linkages ===<br /> [[Image:Slide1.GIF|thumb|center|700px|Alopecia pathways]]<br /> <br /> == Players of Wnt inhibition Pathway == [[Image:wnt.jpg|thumb|right|600px|Wnt inhibition]]<br /> {| border=&quot;1&quot; cellpadding=&quot;15&quot;, style=&quot;#008080&quot;<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Key compound'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Players of inhibition'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6989385.PN.&amp;OS=PN/6989385&amp;RS=PN/6989385 US6989385]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|CDK,GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6974819.PN.&amp;OS=PN/6974819&amp;RS=PN/6974819 US6974819]<br /> |bgcolor=LightCyan|Pyrimidine derivative<br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6743791.PN.&amp;OS=PN/6743791&amp;RS=PN/6743791 US6743791]<br /> |bgcolor=LightCyan|Heterocyclic compounds<br /> |bgcolor=LightCyan|AKT3, GSK-3, ERK2<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277773%22.PGNR.&amp;OS=DN/20050277773&amp;RS=DN/20050277773 US20050277773]<br /> |bgcolor=LightCyan|Pyrrolo[3,2-d]pyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040072836%22.PGNR.&amp;OS=DN/20040072836&amp;RS=DN/20040072836 US20040072836]<br /> |bgcolor=LightCyan|Aza-oxindole derivatives <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1477489&amp;F=0 EP1477489]<br /> |bgcolor=LightCyan|Pyrrolopyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO0056710&amp;F=0 WO0056710]<br /> |bgcolor=LightCyan|3-(Anilinomethylene) oxindoles <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO03011287&amp;F=0 WO2003011287]<br /> |bgcolor=LightCyan|Pyrazolon derivatives <br /> |bgcolor=LightCyan|GSK3, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6924141.PN.&amp;OS=PN/6924141&amp;RS=PN/6924141 US6924141]<br /> |bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7 <br /> |bgcolor=LightCyan|β-catenin, GSK3, Wnt<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6706685.PN.&amp;OS=PN/6706685&amp;RS=PN/6706685 US6706685]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6683048.PN.&amp;OS=PN/6683048&amp;RS=PN/6683048 US6683048]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|α-catenin, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6677116.PN.&amp;OS=PN/6677116&amp;RS=PN/6677116 US6677116]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6303576.PN.&amp;OS=PN/6303576&amp;RS=PN/6303576 US6303576]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |}<br /> [[Image:coloury.jpg]]- '''Target sites and Details'''<br /> <br /> == Pyrazole compounds ==<br /> <br /> * '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.<br /> * Pyrazoles are produced synthetically through the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation <br /> [[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]<br /> * Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.<br /> * Structurally related compounds are pyrazoline and pyrazolidine.<br /> [[Image:pyrazole2.jpg|thumb|center|500px|Structurally related compounds]]<br /> <br /> === GSK3 inhibition by pyrazole compounds ===<br /> [[Image:bold3.jpg]]<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?TERM1=6989385+&amp;Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=0&amp;f=S&amp;l=50 US6989385]<br /> [[Image:US6989385.jpg]]<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247] <br /> [[Image:US6664247.jpg]]<br /> !width=&quot;100&quot;|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256] <br /> [[Image:WO2005012256.jpg]]<br /> |- <br /> |bgcolor=lightcyan|R1=T-Ring D, wherein <br /> T is a valence bond and <br /> Ring D = 5-6 membered aryl or heteroaryl ring; <br /> <br /> R2 = hydrogen or C1-4 aliphatic and <br /> R2'= hydrogen; <br /> <br /> R3 = -R, -OR, or -N(R4)2, wherein <br /> R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and <br /> L is -O-, -S-, or -NH-; and <br /> Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R&lt;4&gt;), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring<br /> <br /> |bgcolor=lightcyan|X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; <br /> <br /> R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; <br /> <br /> R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and <br /> <br /> R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).<br /> <br /> |bgcolor=lightcyan|X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;<br /> A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy).<br /> |}<br /> <br /> === Inhibition by amine derivatives ===<br /> <br /> '''Patent Number''': US6989385<br /> '''Applicant''': ''Vertex Pharmaceuticals Incorporated''<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol1.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-p- yrimidin-4-yl]-amine <br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyl- sulfanyl]-pyrimidin-4-yl}-amine <br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-me- thyl-2H-pyrazol-3-yl)-amine <br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * {2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-y- l}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(- 5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfa- nyl)-pyrimidin-4-yl]-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mo- rpholin-4-yl-pyrimidin-4-yl}-amine <br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimi- din-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyri- midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * 5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-ylmethylsulf- anyl)-pyrimidin-4-yl]-amine <br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)-phenyl]-py- rimidin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methy- l-2H-pyrazol-3-yl)-amine <br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methylphenylamino)-6-phenyl-pyrimidi- n-4-yl]-amine <br /> * [2-(4-cyanomethylphenylamino)-6-phenyl-pyrimidin-4-yl]-(5-cyclopropyl-2H-p- yrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(pyridin-3-ylmethylamino)-pyri- midin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-methyl-2H-py- razol-3-yl)-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3,4,5-trimethoxyphenyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(4-sulfamoylphenylamino)-6-(3,4,5-trimethoxy- phenyl)-pyrimidin-4-yl]-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyraz- ol-3-yl]-amine <br /> * [2-(Benzimidazol-2-ylamino-)6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * (5-tert-Butyl-2H-pyrazol-3-yl)-[2-(3-chlorophenyl)amino-6-(3-nitrophenyl)-- pyrimidin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-phenyl-2H-py- razol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-a- mine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-[5-(Furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * [2-(4-Chlorophenylamino)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * (5,6-Dimethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Chlorophenyl)amino-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * (6-Methoxymethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-- amine <br /> * (6-Methyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyr- azol-3-yl]-amine <br /> * (6-methyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-phenyl-2H-pyrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenoxymethyl-pyrimidin-4-yl)- -amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-amine <br /> * [6-Methyl-2-(4-methyl-phenylsulfanylmethyl)-pyrimidin-4-yl]-(5-phenyl-2H-p- yrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-[6-Methyl-2-(4-methyl-phenylsulfanylmethy- l)-pyrimidin-4-yl]-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * (6-Ethyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)- -amine <br /> * (6-Ethyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Ethyl-2-(4-fluorophenoxymethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [6-Ethyl-2-(1-methyl-1-phenyl-ethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-p- yrazol-3-yl]-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(2-phenylsulfanylmethyl-5,6,7,8-tetrahydro-quin- azolin-4-yl)-amine <br /> * [2-(4-Methylphenylsulfanylmethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidi- n-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(1-Methyl-1-phenyl-ethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-y- l]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6,7,8-tetrahydro-quinazolin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * [7-Benzyl-2-(2,6-dichlorobenzyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-- 4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Benzyl-2-(4-chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimi- din-4-yl]-(5-methyl-2H-pyrazol-3-yl)-<br /> * [2-(4-Chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> ----<br /> '''Patent Number''': US7008948 <br /> '''Applicant''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure'''<br /> <br /> [[Image:pyrazol2.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(1H-i- ndazol-3-yl)-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[3,4-d]pyrimidin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(7-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5,7-- difluoro-1H-indazol-3-yl)-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetra- hydroquinazolin-4-yl]-amine <br /> * (5-Trifluoromethyl-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-- tetrahydroquinazolin-4-yl]-amine <br /> * (5,7-difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetra- hydro-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (6-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyr- imidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydro-5H-cycl- oheptapyrimidin-4-yl]-amine<br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[4,3-d]pyrimidin-4-yl]-amine<br /> * (1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydroquinazol- in-4-yl]-amine <br /> * (7-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine<br /> * (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> * 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> ----<br /> '''Patent Number''': US6977262<br /> '''Assignee''': Mitsubishi Pharma Corporation<br /> '''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol3.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate<br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-methyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Methyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * t-Butyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Isopropyl 4-(2-fluorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Benzyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * 4-(2-Chlorophenyl)-5-dimethylaminocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4-(2-Chlorophenyl)-5-hydrazinocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo[3,4 -b]pyridine <br /> * 4-(2-Fluorophenyl)-4,7-dihydro-6-methyl-5-isopropylthiocarbonyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4,7-Dihydro-6-methyl-5-nitro-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b] pyridine <br /> * Ethyl 4,7-dihydro-4-phenyl-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridine-5-carbox ylate <br /> * Ethyl 4-(2-fluorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate maleate <br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridi ne-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate <br /> * Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate<br /> ----<br /> '''Patent Number''': US6664247<br /> '''Assignee''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors'''<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol4.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine<br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine<br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine<br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine<br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine<br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine<br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine<br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine<br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.<br /> ----<br /> '''Patent Number''': US2004224944<br /> '''Assignee''': VERTEX PHARMACEUTICALS INC<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol5.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine <br /> * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine<br /> <br /> === Other derivates for alopecia ===<br /> [[Image:other derivates.jpeg]]<br /> <br /> == Inhibition of 5- - reductase by Finasteride ==<br /> [[Image:5-alpha-reductase inhibition.jpeg]]<br /> <br /> === Structure-Activity Relationships(SARs) ===<br /> [[Image:SAR_map.gif]]<br /> <br /> == Questions Dolcera Answers ==<br /> <br /> '''What’s hot?'''<br /> * What compositions/ approaches are the most promising?<br /> * What can I license?<br /> * Can you map blockbuster products to their patents?<br /> <br /> '''Can you save me some time?'''<br /> * What combinations/ compounds have already been tried?<br /> * Is any empirical data available?<br /> * Can you tell me the side effects?<br /> <br /> '''Where should I focus my R&amp;D investment?'''<br /> * What are the most promising approaches?<br /> * Where’s the ‘white space’ for me to play in?<br /> <br /> '''Any hints for research?'''<br /> * Are there any combinations I could develop?<br /> <br /> '''What should I do in this geography?'''<br /> * What are my competitors up to in this geography?<br /> * What are my strengths/ weaknesses here?<br /> <br /> '''What’s my competition up to?'''<br /> <br /> * What’s my top competitor investing in?<br /> * Are there any loopholes in their patents?<br /> * When are their patents expiring?<br /> * Will a competitor emerge from nowhere and surprise me?<br /> * What are the crowded areas?<br /> <br /> '''How do I play defense?'''<br /> * What should my blocking/reactive strategies be?<br /> <br /> <br /> == New Combinations based on IP study? ==<br /> <br /> Yes, new Combinations can be made with '''natural products''' based on IP study<br /> * Walnut extract containing [[Image:5ar.jpg]] inhibitor (as anti-androgen) and Flavnones (for vasodilation).<br /> * Sophora Flavnones (for vasodilation) in combination with Saw Palmetto berry (as anti-androgen).<br /> <br /> '''Note:''' The above combinations are based on limited study and are only possible examples<br /> <br /> == IP studies provides ==<br /> <br /> === Technology trends ===<br /> * Use of saw palmetto berry for treating alopecia was first patented in 1996.<br /> * Since then, 144 patents (including family patents) have been filed till 2006.<br /> * Most patents use saw palmetto berry in combination with other products.<br /> [[Image:Technology1.jpg|thumb|center|700px|Technology trends]]<br /> <br /> === New opportunities ===<br /> Yes, the IP studies provide new opportunities in the following area.<br /> * Sophora Flavescens contain flavnoids.<br /> * Natural extract Sophora Flavescens cited in LG patent of 2001.<br /> * Research shows fewer than 7 patents based on Sophora Flavescens for hair loss or alopecia.<br /> <br /> * What's this?<br /> <br /> == Conclusions ==<br /> * Hair loss medication is a very active area of research and intellectual property development.<br /> * One of the most promising areas of development is the area of Anti-androgens.<br /> * The top companies are Merck, L’Oreal and Smithkline.<br /> <br /> == Useful links ==<br /> * [http://www.biocarta.com/pathfiles/h_ghPathway.asp Pathways example]<br /> * [http://www.cellsignal.com/category.asp?catalog_name=CellSignal&amp;category_name=MAPK+Signaling Signaling Pathways]<br /> <br /> == Summary ==</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss&diff=1778 2006-05-21T01:54:17Z

<p>67.180.226.207: /* GSK3 inhibition by pryazole pyrimidine amine derivatives */</p> <hr /> <div>{{TOCrightEx}}<br /> == Rationale ==<br /> * &quot;Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year.&quot; March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55]<br /> <br /> * &quot;An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries.&quot; February 16, 2006 – [http://stophair.setupmyblog.com/]<br /> <br /> * &quot;There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting.&quot; June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&amp;STORY=/www/story/06-07-2005/0003821470&amp;EDATE=]<br /> <br /> == Alopecia IPMap == <br /> [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Dolcera IPMap for Alopecia]<br /> <br /> == Introduction ==<br /> <br /> === Hair Basics ===<br /> * Hair is a complex and delicate part of the body.<br /> * Keeping it healthy and beautiful is a challenge.<br /> * Hair grows everywhere on the body with the exception of the lips, eyelids, the palms of the hands and soles of the feet.<br /> * Hair is basically a form of skin. <br /> * Hair is made up of a protein called keratin.<br /> * Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin. <br /> * Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htm]<br /> * Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.html]<br /> [[Image:Hairbasics.jpg|thumb|center|500px|Structure of Hair root and Hair bulb]]<br /> <br /> === What causes Hair loss? === <br /> * Decreased growth of the hair <br /> * Increased shedding of the hair <br /> * Breakage of hairs <br /> * Conversion of thick terminal hairs to thin vellus hairs <br /> [[Image:Facts.jpg|thumb|right|400px|Survey results from Japan]]<br /> Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed '''“Male Pattern Baldness&quot;''' or '''&quot;Androgenetic Alopecia&quot;'''.<br /> <br /> === Androgenetic Alopecia ===<br /> * Gradual Onset.<br /> * Transition from large, thick, pigmented terminal hairs to thinner, shorter, indeterminate hairs and finally to short, wispy, nonpigmented vellus hairs in the involved areas.<br /> * Characterised by a receding hairline and/or hair loss on the top of the head.<br /> <br /> '''Main Causes'''<br /> * Genetic predisposition<br /> * Hormonal effect of androgen <br /> * Reduction of blood circulation around hair follicle<br /> * Deactivation of hair matrix cells<br /> <br /> '''Some facts from Japan''' <br /> <br /> * Market size: ¥ 30 Billion<br /> * Number of products: more than 100<br /> <br /> (JICST-EPlus - Japanese Science &amp; Technology)<br /> <br /> == Goals ==<br /> <br /> The goal of this report is to:<br /> * Summarize IP activity over the years<br /> * Identify major players<br /> * Conduct patent analysis<br /> a) Composition<br /> b) Nature<br /> c) Action<br /> <br /> '''And then'''<br /> <br /> * Analyze patents pertaining to high sebum activity<br /> <br /> == Approach ==<br /> <br /> * A broad search was conducted on hair loss patents.<br /> * Patent information was sourced through SIP.<br /> * A set of patents was selected for analysis.<br /> <br /> Composition of treatment for causes are identified and categorized as follows:<br /> <br /> * Anti-androgen<br /> * Minoxidil<br /> * Double action (Anti-androgen + Mindoxidil)<br /> * Hair matrix cells activator<br /> * Sebum production inhibitor<br /> <br /> == IP activity over years ==<br /> The graph indicates:<br /> * Number of patents filed every 5 years (except for first 7 years).<br /> * First solution proposed in 1973<br /> * Filing trend indicates steep rise in activity recently.<br /> [[Image:Year1.jpg|thumb|center|400px|IP Activity over years]]<br /> <br /> == Major Players ==<br /> [[Image:players.jpg|thumb|left|400px|Assignees with more than 20 patents ]]<br /> [[Image:players1.jpg|thumb|center|400px|Assignees with fewer than 20 patents ]]<br /> <br /> * '''Active Assignees'''<br /> Assignees currently active with more than 5 patents to their credit during 2000-2005. <br /> * Warner with 9 patents,<br /> * Bristol with 6 and<br /> * Abbott with 5.<br /> <br /> [[Image:Active.jpg|thumb|center|500px|Active Assignees]]<br /> <br /> == Anti-androgens == <br /> * Anti-androgens are used in hormone therapy.<br /> * Anti-androgens are designed to affect the hormones made in the adrenal glands. They don't stop the hormones from being made, but they stop them from having an effect leading to hair loss.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Testosterone is reduced to its active metabolite, Dihydrotestosterone (DHT) by the enzyme 5 alpha reductase.<br /> * DHT attaches to androgen receptor sites at the hair follicle. <br /> * DHT causes gradual miniaturization of the follicle, which eventually results in hair loss.<br /> <br /> '''How do anti-androgens treat hair loss?'''<br /> * Anti-androgens compete with DHT to bind to the androgen receptor.<br /> * Upon binding of anti-androgen in place of DHT, follicle miniaturization is lowered and hair loss prevented.<br /> <br /> === Functions of Anti-androgen === <br /> [http://www.revivogen.com/revivogen/work.html Anti-androgen]<br /> <br /> [[Image:Andogen1.jpg|thumb|center|500px|Functions of Anti-androgen]]<br /> <br /> === IP Map for Anti-androgen ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;8&quot;, style=&quot;#008080&quot;<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> BLOTECH (2004)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Palmetto berry extract (fatty acids &amp; sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans)<br /> |bgcolor=LightCyan|Fatty acids – Inhibit testosterone<br /> Sterols - Mechanism of action unknown.<br /> <br /> Quercetin results in cell growth cycle.<br /> <br /> Beta-sitosterol reduce inflammation on scalp<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 4-cycloalkoxy benzonitrile derivatives and salts<br /> |bgcolor=LightCyan|Acts as androgen receptor modulators and blocks formation of DHT.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives.<br /> |bgcolor=LightCyan|The compounds inhibit, or decrease, activation of androgen receptor by androgens.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> APHIOS Corp (2003)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives.<br /> |bgcolor=LightCyan|Modulates androgenic activity by inhibiting 5.alpha.-reductase activity.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> Fundacion Pablo Cassara (2003)<br /> |bgcolor=LightCyan|Nucleotide<br /> |bgcolor=LightCyan|Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond)<br /> |bgcolor=LightCyan|Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> PFIZER INC (2001)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate <br /> |bgcolor=LightCyan|Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> N/A (1995)<br /> |bgcolor=LightCyan|Peptides/nucleic acid<br /> |bgcolor=LightCyan|Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein)<br /> |bgcolor=LightCyan|Inhibit synthesis of bradykinin receptors or compounds by binding to B2 receptor<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> KAO Corp (1987)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Walnut extract (leaves/pericarps) with an organic solvent<br /> |bgcolor=LightCyan|Blocks formation of DHT<br /> |}<br /> <br /> == Minoxidil ==<br /> * Minoxidil is a &quot;potassium channel opener&quot; that leads to vasodilation.<br /> * The drug is available in two forms. Oral minoxidil is used to treat high blood pressure and the topical solution form is used to treat hair loss and baldness.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * A thick network of tiny veins and arteries lines the outer wall of the follicle. Blood pumps through the bulb and hair via this network.<br /> * DHT accumulates in the hair follicles and roots, constricting the blood supply of oxygen and nutrients to the hair roots; which is also seen to possibly contribute towards hair loss.<br /> <br /> '''How does Minoxidal treat hair loss?'''<br /> * Minoxidal is applied to the scalp topically, where it dilates blood vessels in the scalp and sustains the hair follicles for longer period of time.<br /> * Scientists and researchers are not exactly sure of how Minoxidil leads to this effect.<br /> * Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.<br /> <br /> === Functions of Monoxidil === [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 Minoxidil]<br /> <br /> [[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil]]<br /> <br /> === IP Map for Minoxidil ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> WARNER LAMBERT(2002)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Benzopyran compounds<br /> |bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> LG HOUSEHOLD &amp; HEALTH CARE(2001)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Sophora flavescens extract (alkaloids &amp; flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)<br /> |bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels<br /> |}<br /> <br /> == Double action (Anti-androgen + Minoxidil) ==<br /> * Combination of Minoxidil + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.<br /> <br /> <br /> '''What is the problem with using only Anti-androgen therapy?'''<br /> * Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.<br /> * Anti-androgen only prevent binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.<br /> <br /> '''What is the problem with using only Minoxidal therapy?'''<br /> * Minoxidil-based products are generally not effective in stopping hair loss as minoxidil does not block the harmful effects of DHT in the scalp and hair follicles. <br /> * Minoxidil simply dilates blood vessels in the scalp. However, the harmful DHT is still being produced in the body and still getting into the scalp and hair follicles and causing eventual hair loss.<br /> <br /> '''How is the combination of Anti-androgens and Minoxidil effective?'''<br /> * Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.<br /> * Minoxidil causes vasodilation and therefore improves supply of oxygen and nutrients to the hair follicle and roots.<br /> * Combination therapy therefore proves to be much more effective than individual therapy.<br /> <br /> === Functions of (Anti-androgen + Minoxidil) === [http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]<br /> [[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Minoxidil)]]<br /> <br /> === IP Map for (Anti-androgen + Minoxidil) ===<br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405] <br /> N/A(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhance and sunscreen<br /> |bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577] <br /> L'OREAL(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP<br /> |bgcolor=LightCyan|Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762] <br /> COLOMER GROUP(1999)<br /> |bgcolor=LightCyan|Natural extract<br /> |bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)<br /> |bgcolor=LightCyan|Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp<br /> |}<br /> <br /> <br /> == Hair matrix cell activator ==<br /> Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.<br /> * Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.<br /> * Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.<br /> * Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.<br /> <br /> <br /> '''How does hair cell matrix activator treat hair loss?'''<br /> * Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.<br /> * This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.<br /> * Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.<br /> <br /> === Functions of Hair matrix cell activator === [http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]<br /> [[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]<br /> <br /> === IP Map for Hair matrix cell activator ===<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> SHISEIDO(1999) <br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt<br /> |bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> L'OREAL(1998) <br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions<br /> |bgcolor=LightCyan|Reducing the expression of MMPs (Metalloproteases) in the scalp - slow down or inhibit the degradation of the perifollicular matrix (extracellular matrix surround the hair follicle) <br /> |}<br /> <br /> == Sebum Production Inhibitor ==<br /> Sebum Production Inhibitor is a substance that prevents the synthesis of sebum, mixture of lipid substances.<br /> <br /> '''What causes hair loss?'''<br /> * Sebum is a fatty acid substance secreted from sebaceous glands associated with hair follicles.<br /> * Hair can get heavy sebum build-up and mixes with cholesterol to form a hardened plug around the bottom part of the hair bulb.<br /> * Hardened plugs prevent cell respirations and eventually lead to hair loss.<br /> * Bacteria will also attach to the hardened plug and this can also cause further cause problems with hair growth.<br /> <br /> '''How does Sebum production inhibitor treat hair loss?'''<br /> * The inhibitor prevents synthesis of sebum and slows down accumulation and mixing of sebum with cholesterol leading to hardened plugs. <br /> * Reduction of sebum results in unclogged hair follicles/bulbs and allows oxygen and nutrients from reaching the hair follicle.<br /> * Reduction in sebum also prevents vasoconstriction.<br /> * Sum result of these effects of Sebum production inhibitor is prevention of hair loss.<br /> <br /> <br /> * The inhibitor blocks the excessive sebum production produces greasy effect on hair and scalp and also responsible for thinning and loosing of hair.<br /> <br /> === Functions of Sebum Production Inhibitor ===<br /> [[http://en.wikipedia.org/wiki/Image:HairFollicle.jpg Sebum Production Inhibitor]]<br /> [[Image:Sebum1.jpg|thumb|center|500px|Functions of Sebum Production Inhibitor]]<br /> <br /> === IPMap for Sebum Production Inhibitor ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699] <br /> Unilever(2005)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Polyamine (putrescine, spermine or spermidine) analogs and/or derivatives; DFMO; N-acetyl cysteines; neutralized salts of a non-hydroxy C2-C40 dicarboxylic acids, preferably malonate salts; and mixtures thereof. <br /> |bgcolor=LightCyan|Decreasing sebum production and/or pore size <br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362] <br /> KAO COPR.(2004)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Avocado oil (Butyl esters of fatty acids) <br /> |bgcolor=LightCyan|Reduce sebum of the hair and scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587] <br /> Unilever(1982)<br /> |bgcolor=LightCyan|organic compound<br /> |bgcolor=LightCyan |Biotin antagonist or a salt thereof <br /> |bgcolor=LightCyan|Decrease activity of the enzyme acetyl-SCoA-carboxylase and hence reduce lipid synthesis in sebaceous glands so that less sebum is produced <br /> |}<br /> <br /> == Composition nature matrix ==<br /> <br /> === IPMap: Composition nature matrix ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;11&quot;, style=&quot;#008080&quot;<br /> !width=&quot;50&quot; bgcolor=DodgerBlue|'''Year'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Organic Compound'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extracts''' <br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Peptides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nucleotides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extract + Organic comp'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|2005 <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |- <br /> |bgcolor=LightCyan|2004 <br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|BLOTECH (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |- <br /> |bgcolor=LightCyan|2003<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|APHIOS (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|FUNDIACION (1)<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2002<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2001<br /> |bgcolor=LightCyan |PFIZER (1)<br /> |bgcolor=LightCyan|LG HEALTH-CARE (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2000<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1) / N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1999<br /> |bgcolor=LightCyan|SHISEDIO (1)<br /> |bgcolor=LightCyan|COLOMER (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1998<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1995<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |-<br /> |bgcolor=LightCyan|1987<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1982<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |}<br /> <br /> == Focus of patents ==<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;17&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Focus of patents'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Stimulating hair growth using benzopyrans<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Compositions to prevent or reduce hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Method of decreasing sebum production and pore size<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699 ]<br /> |bgcolor=LightCyan|16<br /> |- <br /> |bgcolor=LightCyan|Method for reducing sebum on the hair and skin<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |bgcolor=LightCyan|17<br /> |}<br /> <br /> === Focus of patents by technology ===<br /> [[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]<br /> <br /> == Distribution of patents ==<br /> <br /> === By patent types ===<br /> [[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]<br /> <br /> <br /> === By key ingredients ===<br /> [[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]<br /> <br /> === By target disease ===<br /> [[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]<br /> <br /> <br /> === Key ingredients vs. Target disease ===<br /> [[Image:key&amp;target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]<br /> <br /> <br /> === Target species ===<br /> [[Image:Species.jpg|thumb|center|700px|Target species]]<br /> <br /> <br /> === Mode of administration ===<br /> [[Image:Mode.jpg|thumb|center|700px|Mode of administration]]<br /> <br /> <br /> === Product type vs. Product form ===<br /> [[Image:prod.jpg|thumb|center|700px|Product type vs. Product form]]<br /> <br /> == Distribution based on different aspects ==<br /> <br /> === List of patents ===<br /> {| border=&quot;1&quot; cellpadding=&quot;9&quot;, style=&quot;#008080&quot;<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|1<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|10<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |- <br /> |bgcolor=LightCyan|2<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|11<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |- <br /> |bgcolor=LightCyan|3<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> |bgcolor=LightCyan|12<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |- <br /> |bgcolor=LightCyan|4<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427] <br /> |bgcolor=LightCyan|13<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |- <br /> |bgcolor=LightCyan|5<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282] <br /> |bgcolor=LightCyan|14<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |- <br /> |bgcolor=LightCyan|6<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467] <br /> |bgcolor=LightCyan|15<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |- <br /> |bgcolor=LightCyan|7<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|16<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699]<br /> |- <br /> |bgcolor=LightCyan|8<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|17<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |- <br /> |bgcolor=LightCyan|9<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010] <br /> |bgcolor=LightCyan|18<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |}<br /> <br /> === Patents by target diseases ===<br /> {| border=&quot;1&quot; cellpadding=&quot;16&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Target disease/ disorder'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness)<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, male pattern baldness and female pattern baldness<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|Inappropriate activation of the androgen receptor, acne, oily skin, alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Androgen-associated hair loss and androgen-skin related disorders. <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Androgenetic or androgenic alopecia or androgeno-genetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Diseases caused by testosterone (male-pattern alopecia)<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Alopecia, androgenic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Androgenetic, androgenic or androgenogenetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Curing other scalp related problems<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |bgcolor=LightCyan|16<br /> |}<br /> <br /> === Patents by application ===<br /> [[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]<br /> <br /> === Signaling Pathway and linkages ===<br /> [[Image:Slide1.GIF|thumb|center|700px|Alopecia pathways]]<br /> <br /> == Players of Wnt inhibition Pathway == [[Image:wnt.jpg|thumb|right|600px|Wnt inhibition]]<br /> {| border=&quot;1&quot; cellpadding=&quot;15&quot;, style=&quot;#008080&quot;<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Key compound'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Players of inhibition'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6989385.PN.&amp;OS=PN/6989385&amp;RS=PN/6989385 US6989385]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|CDK,GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6974819.PN.&amp;OS=PN/6974819&amp;RS=PN/6974819 US6974819]<br /> |bgcolor=LightCyan|Pyrimidine derivative<br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6743791.PN.&amp;OS=PN/6743791&amp;RS=PN/6743791 US6743791]<br /> |bgcolor=LightCyan|Heterocyclic compounds<br /> |bgcolor=LightCyan|AKT3, GSK-3, ERK2<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277773%22.PGNR.&amp;OS=DN/20050277773&amp;RS=DN/20050277773 US20050277773]<br /> |bgcolor=LightCyan|Pyrrolo[3,2-d]pyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040072836%22.PGNR.&amp;OS=DN/20040072836&amp;RS=DN/20040072836 US20040072836]<br /> |bgcolor=LightCyan|Aza-oxindole derivatives <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1477489&amp;F=0 EP1477489]<br /> |bgcolor=LightCyan|Pyrrolopyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO0056710&amp;F=0 WO0056710]<br /> |bgcolor=LightCyan|3-(Anilinomethylene) oxindoles <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO03011287&amp;F=0 WO2003011287]<br /> |bgcolor=LightCyan|Pyrazolon derivatives <br /> |bgcolor=LightCyan|GSK3, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6924141.PN.&amp;OS=PN/6924141&amp;RS=PN/6924141 US6924141]<br /> |bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7 <br /> |bgcolor=LightCyan|β-catenin, GSK3, Wnt<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6706685.PN.&amp;OS=PN/6706685&amp;RS=PN/6706685 US6706685]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6683048.PN.&amp;OS=PN/6683048&amp;RS=PN/6683048 US6683048]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|α-catenin, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6677116.PN.&amp;OS=PN/6677116&amp;RS=PN/6677116 US6677116]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6303576.PN.&amp;OS=PN/6303576&amp;RS=PN/6303576 US6303576]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |}<br /> [[Image:coloury.jpg]]- '''Target sites and Details'''<br /> <br /> == Pyrazole compounds ==<br /> <br /> * '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.<br /> * Pyrazoles are produced synthetically through the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation <br /> [[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]<br /> * Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.<br /> * Structurally related compounds are pyrazoline and pyrazolidine.<br /> [[Image:pyrazole2.jpg|thumb|center|500px|Structurally related compounds]]<br /> <br /> === GSK3 inhibition by pyrazole compounds ===<br /> [[Image:bold3.jpg]]<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?TERM1=6989385+&amp;Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=0&amp;f=S&amp;l=50 US6989385]<br /> [[Image:US6989385.jpg]]<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247] <br /> [[Image:US6664247.jpg]]<br /> !width=&quot;100&quot;|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256] <br /> [[Image:WO2005012256.jpg]]<br /> |- <br /> |bgcolor=lightcyan|R1=T-Ring D, wherein <br /> T is a valence bond and <br /> Ring D = 5-6 membered aryl or heteroaryl ring; <br /> <br /> R2 = hydrogen or C1-4 aliphatic and <br /> R2'= hydrogen; <br /> <br /> R3 = -R, -OR, or -N(R4)2, wherein <br /> R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and <br /> L is -O-, -S-, or -NH-; and <br /> Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R&lt;4&gt;), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring<br /> <br /> |bgcolor=lightcyan|X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; <br /> <br /> R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; <br /> <br /> R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and <br /> <br /> R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).<br /> <br /> |bgcolor=lightcyan|X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;<br /> A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy).<br /> |}<br /> <br /> === Inhibition by amine derivatives ===<br /> <br /> '''Patent Number''': US6989385<br /> '''Applicant''': ''Vertex Pharmaceuticals Incorporated''<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol1.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-p- yrimidin-4-yl]-amine <br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyl- sulfanyl]-pyrimidin-4-yl}-amine <br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-me- thyl-2H-pyrazol-3-yl)-amine <br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * {2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-y- l}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(- 5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfa- nyl)-pyrimidin-4-yl]-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mo- rpholin-4-yl-pyrimidin-4-yl}-amine <br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimi- din-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyri- midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * 5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-ylmethylsulf- anyl)-pyrimidin-4-yl]-amine <br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)-phenyl]-py- rimidin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methy- l-2H-pyrazol-3-yl)-amine <br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methylphenylamino)-6-phenyl-pyrimidi- n-4-yl]-amine <br /> * [2-(4-cyanomethylphenylamino)-6-phenyl-pyrimidin-4-yl]-(5-cyclopropyl-2H-p- yrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(pyridin-3-ylmethylamino)-pyri- midin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-methyl-2H-py- razol-3-yl)-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3,4,5-trimethoxyphenyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(4-sulfamoylphenylamino)-6-(3,4,5-trimethoxy- phenyl)-pyrimidin-4-yl]-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyraz- ol-3-yl]-amine <br /> * [2-(Benzimidazol-2-ylamino-)6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * (5-tert-Butyl-2H-pyrazol-3-yl)-[2-(3-chlorophenyl)amino-6-(3-nitrophenyl)-- pyrimidin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-phenyl-2H-py- razol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-a- mine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-[5-(Furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * [2-(4-Chlorophenylamino)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * (5,6-Dimethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Chlorophenyl)amino-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * (6-Methoxymethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-- amine <br /> * (6-Methyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyr- azol-3-yl]-amine <br /> * (6-methyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-phenyl-2H-pyrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenoxymethyl-pyrimidin-4-yl)- -amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-amine <br /> * [6-Methyl-2-(4-methyl-phenylsulfanylmethyl)-pyrimidin-4-yl]-(5-phenyl-2H-p- yrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-[6-Methyl-2-(4-methyl-phenylsulfanylmethy- l)-pyrimidin-4-yl]-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * (6-Ethyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)- -amine <br /> * (6-Ethyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Ethyl-2-(4-fluorophenoxymethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [6-Ethyl-2-(1-methyl-1-phenyl-ethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-p- yrazol-3-yl]-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(2-phenylsulfanylmethyl-5,6,7,8-tetrahydro-quin- azolin-4-yl)-amine <br /> * [2-(4-Methylphenylsulfanylmethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidi- n-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(1-Methyl-1-phenyl-ethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-y- l]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6,7,8-tetrahydro-quinazolin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * [7-Benzyl-2-(2,6-dichlorobenzyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-- 4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Benzyl-2-(4-chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimi- din-4-yl]-(5-methyl-2H-pyrazol-3-yl)-<br /> * [2-(4-Chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> ----<br /> '''Patent Number''': US7008948 <br /> '''Applicant''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure'''<br /> <br /> [[Image:pyrazol2.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(1H-i- ndazol-3-yl)-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[3,4-d]pyrimidin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(7-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5,7-- difluoro-1H-indazol-3-yl)-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetra- hydroquinazolin-4-yl]-amine <br /> * (5-Trifluoromethyl-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-- tetrahydroquinazolin-4-yl]-amine <br /> * (5,7-difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetra- hydro-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (6-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyr- imidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydro-5H-cycl- oheptapyrimidin-4-yl]-amine<br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[4,3-d]pyrimidin-4-yl]-amine<br /> * (1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydroquinazol- in-4-yl]-amine <br /> * (7-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine<br /> * (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> * 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> ----<br /> '''Patent Number''': US6977262<br /> '''Assignee''': Mitsubishi Pharma Corporation<br /> '''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol3.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate<br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-methyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Methyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * t-Butyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Isopropyl 4-(2-fluorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Benzyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * 4-(2-Chlorophenyl)-5-dimethylaminocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4-(2-Chlorophenyl)-5-hydrazinocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo[3,4 -b]pyridine <br /> * 4-(2-Fluorophenyl)-4,7-dihydro-6-methyl-5-isopropylthiocarbonyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4,7-Dihydro-6-methyl-5-nitro-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b] pyridine <br /> * Ethyl 4,7-dihydro-4-phenyl-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridine-5-carbox ylate <br /> * Ethyl 4-(2-fluorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate maleate <br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridi ne-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate <br /> * Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate<br /> ----<br /> '''Patent Number''': US6664247<br /> '''Assignee''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors'''<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol4.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine<br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine<br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine<br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine<br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine<br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine<br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine<br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine<br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.<br /> ----<br /> '''Patent Number''': US2004224944<br /> '''Assignee''': VERTEX PHARMACEUTICALS INC<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol5.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine <br /> * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine<br /> <br /> === Other derivates for alopecia ===<br /> [[Image:other derivates.jpeg]]<br /> <br /> == Inhibition of 5- - reductase by Finasteride ==<br /> [[Image:5-alpha-reductase inhibition.jpeg]]<br /> <br /> === Structure-Activity Relationships (SARs) of Finasteride ===<br /> [[Image:SAR_map.gif]]<br /> <br /> == Questions Dolcera Answers ==<br /> <br /> '''What’s hot?'''<br /> * What compositions/ approaches are the most promising?<br /> * What can I license?<br /> * Can you map blockbuster products to their patents?<br /> <br /> '''Can you save me some time?'''<br /> * What combinations/ compounds have already been tried?<br /> * Is any empirical data available?<br /> * Can you tell me the side effects?<br /> <br /> '''Where should I focus my R&amp;D investment?'''<br /> * What are the most promising approaches?<br /> * Where’s the ‘white space’ for me to play in?<br /> <br /> '''Any hints for research?'''<br /> * Are there any combinations I could develop?<br /> <br /> '''What should I do in this geography?'''<br /> * What are my competitors up to in this geography?<br /> * What are my strengths/ weaknesses here?<br /> <br /> '''What’s my competition up to?'''<br /> <br /> * What’s my top competitor investing in?<br /> * Are there any loopholes in their patents?<br /> * When are their patents expiring?<br /> * Will a competitor emerge from nowhere and surprise me?<br /> * What are the crowded areas?<br /> <br /> '''How do I play defense?'''<br /> * What should my blocking/reactive strategies be?<br /> <br /> <br /> == New Combinations based on IP study? ==<br /> <br /> Yes, new Combinations can be made with '''natural products''' based on IP study<br /> * Walnut extract containing [[Image:5ar.jpg]] inhibitor (as anti-androgen) and Flavnones (for vasodilation).<br /> * Sophora Flavnones (for vasodilation) in combination with Saw Palmetto berry (as anti-androgen).<br /> <br /> '''Note:''' The above combinations are based on limited study and are only possible examples<br /> <br /> == IP studies provides ==<br /> <br /> === Technology trends ===<br /> * Use of saw palmetto berry for treating alopecia was first patented in 1996.<br /> * Since then, 144 patents (including family patents) have been filed till 2006.<br /> * Most patents use saw palmetto berry in combination with other products.<br /> [[Image:Technology1.jpg|thumb|center|700px|Technology trends]]<br /> <br /> === New opportunities ===<br /> Yes, the IP studies provide new opportunities in the following area.<br /> * Sophora Flavescens contain flavnoids.<br /> * Natural extract Sophora Flavescens cited in LG patent of 2001.<br /> * Research shows fewer than 7 patents based on Sophora Flavescens for hair loss or alopecia.<br /> <br /> * What's this?<br /> <br /> == Conclusions ==<br /> * Hair loss medication is a very active area of research and intellectual property development.<br /> * One of the most promising areas of development is the area of Anti-androgens.<br /> * The top companies are Merck, L’Oreal and Smithkline.<br /> <br /> == Useful links ==<br /> * [http://www.biocarta.com/pathfiles/h_ghPathway.asp Pathways example]<br /> * [http://www.cellsignal.com/category.asp?catalog_name=CellSignal&amp;category_name=MAPK+Signaling Signaling Pathways]<br /> <br /> == Summary ==</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Template:TOCrightEx&diff=1777 2006-05-21T01:53:03Z

<p>67.180.226.207: </p> <hr /> <div>{| cellspacing=&quot;0&quot; cellpadding=&quot;0&quot; style=&quot;clear:right; margin-bottom: .5em; float: right; padding: .5em 0 .8em 1.4em; background: none; font:normal normal normal {{{1}}} Arial;}&quot;<br /> |<br /> __TOC__<br /> |}&lt;noinclude&gt;[[Category:TOC templates|{{PAGENAME}}]]&lt;/noinclude&gt;</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss&diff=1776 2006-05-21T01:52:34Z

<p>67.180.226.207: </p> <hr /> <div>{{TOCrightEx}}<br /> == Rationale ==<br /> * &quot;Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year.&quot; March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55]<br /> <br /> * &quot;An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries.&quot; February 16, 2006 – [http://stophair.setupmyblog.com/]<br /> <br /> * &quot;There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting.&quot; June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&amp;STORY=/www/story/06-07-2005/0003821470&amp;EDATE=]<br /> <br /> == Alopecia IPMap == <br /> [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Dolcera IPMap for Alopecia]<br /> <br /> == Introduction ==<br /> <br /> === Hair Basics ===<br /> * Hair is a complex and delicate part of the body.<br /> * Keeping it healthy and beautiful is a challenge.<br /> * Hair grows everywhere on the body with the exception of the lips, eyelids, the palms of the hands and soles of the feet.<br /> * Hair is basically a form of skin. <br /> * Hair is made up of a protein called keratin.<br /> * Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin. <br /> * Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htm]<br /> * Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.html]<br /> [[Image:Hairbasics.jpg|thumb|center|500px|Structure of Hair root and Hair bulb]]<br /> <br /> === What causes Hair loss? === <br /> * Decreased growth of the hair <br /> * Increased shedding of the hair <br /> * Breakage of hairs <br /> * Conversion of thick terminal hairs to thin vellus hairs <br /> [[Image:Facts.jpg|thumb|right|400px|Survey results from Japan]]<br /> Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed '''“Male Pattern Baldness&quot;''' or '''&quot;Androgenetic Alopecia&quot;'''.<br /> <br /> === Androgenetic Alopecia ===<br /> * Gradual Onset.<br /> * Transition from large, thick, pigmented terminal hairs to thinner, shorter, indeterminate hairs and finally to short, wispy, nonpigmented vellus hairs in the involved areas.<br /> * Characterised by a receding hairline and/or hair loss on the top of the head.<br /> <br /> '''Main Causes'''<br /> * Genetic predisposition<br /> * Hormonal effect of androgen <br /> * Reduction of blood circulation around hair follicle<br /> * Deactivation of hair matrix cells<br /> <br /> '''Some facts from Japan''' <br /> <br /> * Market size: ¥ 30 Billion<br /> * Number of products: more than 100<br /> <br /> (JICST-EPlus - Japanese Science &amp; Technology)<br /> <br /> == Goals ==<br /> <br /> The goal of this report is to:<br /> * Summarize IP activity over the years<br /> * Identify major players<br /> * Conduct patent analysis<br /> a) Composition<br /> b) Nature<br /> c) Action<br /> <br /> '''And then'''<br /> <br /> * Analyze patents pertaining to high sebum activity<br /> <br /> == Approach ==<br /> <br /> * A broad search was conducted on hair loss patents.<br /> * Patent information was sourced through SIP.<br /> * A set of patents was selected for analysis.<br /> <br /> Composition of treatment for causes are identified and categorized as follows:<br /> <br /> * Anti-androgen<br /> * Minoxidil<br /> * Double action (Anti-androgen + Mindoxidil)<br /> * Hair matrix cells activator<br /> * Sebum production inhibitor<br /> <br /> == IP activity over years ==<br /> The graph indicates:<br /> * Number of patents filed every 5 years (except for first 7 years).<br /> * First solution proposed in 1973<br /> * Filing trend indicates steep rise in activity recently.<br /> [[Image:Year1.jpg|thumb|center|400px|IP Activity over years]]<br /> <br /> == Major Players ==<br /> [[Image:players.jpg|thumb|left|400px|Assignees with more than 20 patents ]]<br /> [[Image:players1.jpg|thumb|center|400px|Assignees with fewer than 20 patents ]]<br /> <br /> * '''Active Assignees'''<br /> Assignees currently active with more than 5 patents to their credit during 2000-2005. <br /> * Warner with 9 patents,<br /> * Bristol with 6 and<br /> * Abbott with 5.<br /> <br /> [[Image:Active.jpg|thumb|center|500px|Active Assignees]]<br /> <br /> == Anti-androgens == <br /> * Anti-androgens are used in hormone therapy.<br /> * Anti-androgens are designed to affect the hormones made in the adrenal glands. They don't stop the hormones from being made, but they stop them from having an effect leading to hair loss.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Testosterone is reduced to its active metabolite, Dihydrotestosterone (DHT) by the enzyme 5 alpha reductase.<br /> * DHT attaches to androgen receptor sites at the hair follicle. <br /> * DHT causes gradual miniaturization of the follicle, which eventually results in hair loss.<br /> <br /> '''How do anti-androgens treat hair loss?'''<br /> * Anti-androgens compete with DHT to bind to the androgen receptor.<br /> * Upon binding of anti-androgen in place of DHT, follicle miniaturization is lowered and hair loss prevented.<br /> <br /> === Functions of Anti-androgen === <br /> [http://www.revivogen.com/revivogen/work.html Anti-androgen]<br /> <br /> [[Image:Andogen1.jpg|thumb|center|500px|Functions of Anti-androgen]]<br /> <br /> === IP Map for Anti-androgen ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;8&quot;, style=&quot;#008080&quot;<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> BLOTECH (2004)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Palmetto berry extract (fatty acids &amp; sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans)<br /> |bgcolor=LightCyan|Fatty acids – Inhibit testosterone<br /> Sterols - Mechanism of action unknown.<br /> <br /> Quercetin results in cell growth cycle.<br /> <br /> Beta-sitosterol reduce inflammation on scalp<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 4-cycloalkoxy benzonitrile derivatives and salts<br /> |bgcolor=LightCyan|Acts as androgen receptor modulators and blocks formation of DHT.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives.<br /> |bgcolor=LightCyan|The compounds inhibit, or decrease, activation of androgen receptor by androgens.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> APHIOS Corp (2003)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives.<br /> |bgcolor=LightCyan|Modulates androgenic activity by inhibiting 5.alpha.-reductase activity.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> Fundacion Pablo Cassara (2003)<br /> |bgcolor=LightCyan|Nucleotide<br /> |bgcolor=LightCyan|Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond)<br /> |bgcolor=LightCyan|Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> PFIZER INC (2001)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate <br /> |bgcolor=LightCyan|Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> N/A (1995)<br /> |bgcolor=LightCyan|Peptides/nucleic acid<br /> |bgcolor=LightCyan|Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein)<br /> |bgcolor=LightCyan|Inhibit synthesis of bradykinin receptors or compounds by binding to B2 receptor<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> KAO Corp (1987)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Walnut extract (leaves/pericarps) with an organic solvent<br /> |bgcolor=LightCyan|Blocks formation of DHT<br /> |}<br /> <br /> == Minoxidil ==<br /> * Minoxidil is a &quot;potassium channel opener&quot; that leads to vasodilation.<br /> * The drug is available in two forms. Oral minoxidil is used to treat high blood pressure and the topical solution form is used to treat hair loss and baldness.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * A thick network of tiny veins and arteries lines the outer wall of the follicle. Blood pumps through the bulb and hair via this network.<br /> * DHT accumulates in the hair follicles and roots, constricting the blood supply of oxygen and nutrients to the hair roots; which is also seen to possibly contribute towards hair loss.<br /> <br /> '''How does Minoxidal treat hair loss?'''<br /> * Minoxidal is applied to the scalp topically, where it dilates blood vessels in the scalp and sustains the hair follicles for longer period of time.<br /> * Scientists and researchers are not exactly sure of how Minoxidil leads to this effect.<br /> * Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.<br /> <br /> === Functions of Monoxidil === [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 Minoxidil]<br /> <br /> [[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil]]<br /> <br /> === IP Map for Minoxidil ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> WARNER LAMBERT(2002)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Benzopyran compounds<br /> |bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> LG HOUSEHOLD &amp; HEALTH CARE(2001)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Sophora flavescens extract (alkaloids &amp; flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)<br /> |bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels<br /> |}<br /> <br /> == Double action (Anti-androgen + Minoxidil) ==<br /> * Combination of Minoxidil + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.<br /> <br /> <br /> '''What is the problem with using only Anti-androgen therapy?'''<br /> * Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.<br /> * Anti-androgen only prevent binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.<br /> <br /> '''What is the problem with using only Minoxidal therapy?'''<br /> * Minoxidil-based products are generally not effective in stopping hair loss as minoxidil does not block the harmful effects of DHT in the scalp and hair follicles. <br /> * Minoxidil simply dilates blood vessels in the scalp. However, the harmful DHT is still being produced in the body and still getting into the scalp and hair follicles and causing eventual hair loss.<br /> <br /> '''How is the combination of Anti-androgens and Minoxidil effective?'''<br /> * Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.<br /> * Minoxidil causes vasodilation and therefore improves supply of oxygen and nutrients to the hair follicle and roots.<br /> * Combination therapy therefore proves to be much more effective than individual therapy.<br /> <br /> === Functions of (Anti-androgen + Minoxidil) === [http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]<br /> [[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Minoxidil)]]<br /> <br /> === IP Map for (Anti-androgen + Minoxidil) ===<br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405] <br /> N/A(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhance and sunscreen<br /> |bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577] <br /> L'OREAL(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP<br /> |bgcolor=LightCyan|Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762] <br /> COLOMER GROUP(1999)<br /> |bgcolor=LightCyan|Natural extract<br /> |bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)<br /> |bgcolor=LightCyan|Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp<br /> |}<br /> <br /> <br /> == Hair matrix cell activator ==<br /> Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.<br /> * Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.<br /> * Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.<br /> * Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.<br /> <br /> <br /> '''How does hair cell matrix activator treat hair loss?'''<br /> * Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.<br /> * This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.<br /> * Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.<br /> <br /> === Functions of Hair matrix cell activator === [http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]<br /> [[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]<br /> <br /> === IP Map for Hair matrix cell activator ===<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> SHISEIDO(1999) <br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt<br /> |bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> L'OREAL(1998) <br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions<br /> |bgcolor=LightCyan|Reducing the expression of MMPs (Metalloproteases) in the scalp - slow down or inhibit the degradation of the perifollicular matrix (extracellular matrix surround the hair follicle) <br /> |}<br /> <br /> == Sebum Production Inhibitor ==<br /> Sebum Production Inhibitor is a substance that prevents the synthesis of sebum, mixture of lipid substances.<br /> <br /> '''What causes hair loss?'''<br /> * Sebum is a fatty acid substance secreted from sebaceous glands associated with hair follicles.<br /> * Hair can get heavy sebum build-up and mixes with cholesterol to form a hardened plug around the bottom part of the hair bulb.<br /> * Hardened plugs prevent cell respirations and eventually lead to hair loss.<br /> * Bacteria will also attach to the hardened plug and this can also cause further cause problems with hair growth.<br /> <br /> '''How does Sebum production inhibitor treat hair loss?'''<br /> * The inhibitor prevents synthesis of sebum and slows down accumulation and mixing of sebum with cholesterol leading to hardened plugs. <br /> * Reduction of sebum results in unclogged hair follicles/bulbs and allows oxygen and nutrients from reaching the hair follicle.<br /> * Reduction in sebum also prevents vasoconstriction.<br /> * Sum result of these effects of Sebum production inhibitor is prevention of hair loss.<br /> <br /> <br /> * The inhibitor blocks the excessive sebum production produces greasy effect on hair and scalp and also responsible for thinning and loosing of hair.<br /> <br /> === Functions of Sebum Production Inhibitor ===<br /> [[http://en.wikipedia.org/wiki/Image:HairFollicle.jpg Sebum Production Inhibitor]]<br /> [[Image:Sebum1.jpg|thumb|center|500px|Functions of Sebum Production Inhibitor]]<br /> <br /> === IPMap for Sebum Production Inhibitor ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699] <br /> Unilever(2005)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Polyamine (putrescine, spermine or spermidine) analogs and/or derivatives; DFMO; N-acetyl cysteines; neutralized salts of a non-hydroxy C2-C40 dicarboxylic acids, preferably malonate salts; and mixtures thereof. <br /> |bgcolor=LightCyan|Decreasing sebum production and/or pore size <br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362] <br /> KAO COPR.(2004)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Avocado oil (Butyl esters of fatty acids) <br /> |bgcolor=LightCyan|Reduce sebum of the hair and scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587] <br /> Unilever(1982)<br /> |bgcolor=LightCyan|organic compound<br /> |bgcolor=LightCyan |Biotin antagonist or a salt thereof <br /> |bgcolor=LightCyan|Decrease activity of the enzyme acetyl-SCoA-carboxylase and hence reduce lipid synthesis in sebaceous glands so that less sebum is produced <br /> |}<br /> <br /> == Composition nature matrix ==<br /> <br /> === IPMap: Composition nature matrix ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;11&quot;, style=&quot;#008080&quot;<br /> !width=&quot;50&quot; bgcolor=DodgerBlue|'''Year'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Organic Compound'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extracts''' <br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Peptides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nucleotides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extract + Organic comp'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|2005 <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |- <br /> |bgcolor=LightCyan|2004 <br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|BLOTECH (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |- <br /> |bgcolor=LightCyan|2003<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|APHIOS (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|FUNDIACION (1)<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2002<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2001<br /> |bgcolor=LightCyan |PFIZER (1)<br /> |bgcolor=LightCyan|LG HEALTH-CARE (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2000<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1) / N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1999<br /> |bgcolor=LightCyan|SHISEDIO (1)<br /> |bgcolor=LightCyan|COLOMER (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1998<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1995<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |-<br /> |bgcolor=LightCyan|1987<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1982<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |}<br /> <br /> == Focus of patents ==<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;17&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Focus of patents'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Stimulating hair growth using benzopyrans<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Compositions to prevent or reduce hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Method of decreasing sebum production and pore size<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699 ]<br /> |bgcolor=LightCyan|16<br /> |- <br /> |bgcolor=LightCyan|Method for reducing sebum on the hair and skin<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |bgcolor=LightCyan|17<br /> |}<br /> <br /> === Focus of patents by technology ===<br /> [[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]<br /> <br /> == Distribution of patents ==<br /> <br /> === By patent types ===<br /> [[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]<br /> <br /> <br /> === By key ingredients ===<br /> [[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]<br /> <br /> === By target disease ===<br /> [[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]<br /> <br /> <br /> === Key ingredients vs. Target disease ===<br /> [[Image:key&amp;target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]<br /> <br /> <br /> === Target species ===<br /> [[Image:Species.jpg|thumb|center|700px|Target species]]<br /> <br /> <br /> === Mode of administration ===<br /> [[Image:Mode.jpg|thumb|center|700px|Mode of administration]]<br /> <br /> <br /> === Product type vs. Product form ===<br /> [[Image:prod.jpg|thumb|center|700px|Product type vs. Product form]]<br /> <br /> == Distribution based on different aspects ==<br /> <br /> === List of patents ===<br /> {| border=&quot;1&quot; cellpadding=&quot;9&quot;, style=&quot;#008080&quot;<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|1<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|10<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |- <br /> |bgcolor=LightCyan|2<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|11<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |- <br /> |bgcolor=LightCyan|3<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> |bgcolor=LightCyan|12<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |- <br /> |bgcolor=LightCyan|4<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427] <br /> |bgcolor=LightCyan|13<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |- <br /> |bgcolor=LightCyan|5<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282] <br /> |bgcolor=LightCyan|14<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |- <br /> |bgcolor=LightCyan|6<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467] <br /> |bgcolor=LightCyan|15<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |- <br /> |bgcolor=LightCyan|7<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|16<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699]<br /> |- <br /> |bgcolor=LightCyan|8<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|17<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |- <br /> |bgcolor=LightCyan|9<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010] <br /> |bgcolor=LightCyan|18<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |}<br /> <br /> === Patents by target diseases ===<br /> {| border=&quot;1&quot; cellpadding=&quot;16&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Target disease/ disorder'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness)<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, male pattern baldness and female pattern baldness<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|Inappropriate activation of the androgen receptor, acne, oily skin, alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Androgen-associated hair loss and androgen-skin related disorders. <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Androgenetic or androgenic alopecia or androgeno-genetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Diseases caused by testosterone (male-pattern alopecia)<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Alopecia, androgenic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Androgenetic, androgenic or androgenogenetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Curing other scalp related problems<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |bgcolor=LightCyan|16<br /> |}<br /> <br /> === Patents by application ===<br /> [[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]<br /> <br /> === Signaling Pathway and linkages ===<br /> [[Image:Slide1.GIF|thumb|center|700px|Alopecia pathways]]<br /> <br /> == Players of Wnt inhibition Pathway == [[Image:wnt.jpg|thumb|right|600px|Wnt inhibition]]<br /> {| border=&quot;1&quot; cellpadding=&quot;15&quot;, style=&quot;#008080&quot;<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Key compound'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Players of inhibition'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6989385.PN.&amp;OS=PN/6989385&amp;RS=PN/6989385 US6989385]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|CDK,GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6974819.PN.&amp;OS=PN/6974819&amp;RS=PN/6974819 US6974819]<br /> |bgcolor=LightCyan|Pyrimidine derivative<br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6743791.PN.&amp;OS=PN/6743791&amp;RS=PN/6743791 US6743791]<br /> |bgcolor=LightCyan|Heterocyclic compounds<br /> |bgcolor=LightCyan|AKT3, GSK-3, ERK2<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277773%22.PGNR.&amp;OS=DN/20050277773&amp;RS=DN/20050277773 US20050277773]<br /> |bgcolor=LightCyan|Pyrrolo[3,2-d]pyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040072836%22.PGNR.&amp;OS=DN/20040072836&amp;RS=DN/20040072836 US20040072836]<br /> |bgcolor=LightCyan|Aza-oxindole derivatives <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1477489&amp;F=0 EP1477489]<br /> |bgcolor=LightCyan|Pyrrolopyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO0056710&amp;F=0 WO0056710]<br /> |bgcolor=LightCyan|3-(Anilinomethylene) oxindoles <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO03011287&amp;F=0 WO2003011287]<br /> |bgcolor=LightCyan|Pyrazolon derivatives <br /> |bgcolor=LightCyan|GSK3, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6924141.PN.&amp;OS=PN/6924141&amp;RS=PN/6924141 US6924141]<br /> |bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7 <br /> |bgcolor=LightCyan|β-catenin, GSK3, Wnt<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6706685.PN.&amp;OS=PN/6706685&amp;RS=PN/6706685 US6706685]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6683048.PN.&amp;OS=PN/6683048&amp;RS=PN/6683048 US6683048]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|α-catenin, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6677116.PN.&amp;OS=PN/6677116&amp;RS=PN/6677116 US6677116]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6303576.PN.&amp;OS=PN/6303576&amp;RS=PN/6303576 US6303576]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |}<br /> [[Image:coloury.jpg]]- '''Target sites and Details'''<br /> <br /> == Pyrazole compounds ==<br /> <br /> * '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.<br /> * Pyrazoles are produced synthetically through the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation <br /> [[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]<br /> * Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.<br /> * Structurally related compounds are pyrazoline and pyrazolidine.<br /> [[Image:pyrazole2.jpg|thumb|center|500px|Structurally related compounds]]<br /> <br /> === GSK3 inhibition by pyrazole compounds ===<br /> [[Image:bold3.jpg]]<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?TERM1=6989385+&amp;Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=0&amp;f=S&amp;l=50 US6989385]<br /> [[Image:US6989385.jpg]]<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247] <br /> [[Image:US6664247.jpg]]<br /> !width=&quot;100&quot;|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256] <br /> [[Image:WO2005012256.jpg]]<br /> |- <br /> |bgcolor=lightcyan|R1=T-Ring D, wherein <br /> T is a valence bond and <br /> Ring D = 5-6 membered aryl or heteroaryl ring; <br /> <br /> R2 = hydrogen or C1-4 aliphatic and <br /> R2'= hydrogen; <br /> <br /> R3 = -R, -OR, or -N(R4)2, wherein <br /> R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and <br /> L is -O-, -S-, or -NH-; and <br /> Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R&lt;4&gt;), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring<br /> <br /> |bgcolor=lightcyan|X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; <br /> <br /> R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; <br /> <br /> R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and <br /> <br /> R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).<br /> <br /> |bgcolor=lightcyan|X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;<br /> A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy).<br /> |}<br /> <br /> === GSK3 inhibition by pryazole pyrimidine amine derivatives ===<br /> <br /> '''Patent Number''': US6989385<br /> '''Applicant''': ''Vertex Pharmaceuticals Incorporated''<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol1.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-p- yrimidin-4-yl]-amine <br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyl- sulfanyl]-pyrimidin-4-yl}-amine <br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-me- thyl-2H-pyrazol-3-yl)-amine <br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * {2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-y- l}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(- 5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfa- nyl)-pyrimidin-4-yl]-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mo- rpholin-4-yl-pyrimidin-4-yl}-amine <br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimi- din-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyri- midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * 5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-ylmethylsulf- anyl)-pyrimidin-4-yl]-amine <br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)-phenyl]-py- rimidin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methy- l-2H-pyrazol-3-yl)-amine <br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methylphenylamino)-6-phenyl-pyrimidi- n-4-yl]-amine <br /> * [2-(4-cyanomethylphenylamino)-6-phenyl-pyrimidin-4-yl]-(5-cyclopropyl-2H-p- yrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(pyridin-3-ylmethylamino)-pyri- midin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-methyl-2H-py- razol-3-yl)-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3,4,5-trimethoxyphenyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(4-sulfamoylphenylamino)-6-(3,4,5-trimethoxy- phenyl)-pyrimidin-4-yl]-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyraz- ol-3-yl]-amine <br /> * [2-(Benzimidazol-2-ylamino-)6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * (5-tert-Butyl-2H-pyrazol-3-yl)-[2-(3-chlorophenyl)amino-6-(3-nitrophenyl)-- pyrimidin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-phenyl-2H-py- razol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-a- mine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-[5-(Furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * [2-(4-Chlorophenylamino)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * (5,6-Dimethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Chlorophenyl)amino-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * (6-Methoxymethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-- amine <br /> * (6-Methyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyr- azol-3-yl]-amine <br /> * (6-methyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-phenyl-2H-pyrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenoxymethyl-pyrimidin-4-yl)- -amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-amine <br /> * [6-Methyl-2-(4-methyl-phenylsulfanylmethyl)-pyrimidin-4-yl]-(5-phenyl-2H-p- yrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-[6-Methyl-2-(4-methyl-phenylsulfanylmethy- l)-pyrimidin-4-yl]-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * (6-Ethyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)- -amine <br /> * (6-Ethyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Ethyl-2-(4-fluorophenoxymethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [6-Ethyl-2-(1-methyl-1-phenyl-ethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-p- yrazol-3-yl]-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(2-phenylsulfanylmethyl-5,6,7,8-tetrahydro-quin- azolin-4-yl)-amine <br /> * [2-(4-Methylphenylsulfanylmethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidi- n-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(1-Methyl-1-phenyl-ethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-y- l]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6,7,8-tetrahydro-quinazolin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * [7-Benzyl-2-(2,6-dichlorobenzyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-- 4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Benzyl-2-(4-chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimi- din-4-yl]-(5-methyl-2H-pyrazol-3-yl)-<br /> * [2-(4-Chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> ----<br /> '''Patent Number''': US7008948 <br /> '''Applicant''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure'''<br /> <br /> [[Image:pyrazol2.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(1H-i- ndazol-3-yl)-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[3,4-d]pyrimidin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(7-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5,7-- difluoro-1H-indazol-3-yl)-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetra- hydroquinazolin-4-yl]-amine <br /> * (5-Trifluoromethyl-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-- tetrahydroquinazolin-4-yl]-amine <br /> * (5,7-difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetra- hydro-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (6-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyr- imidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydro-5H-cycl- oheptapyrimidin-4-yl]-amine<br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[4,3-d]pyrimidin-4-yl]-amine<br /> * (1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydroquinazol- in-4-yl]-amine <br /> * (7-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine<br /> * (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> * 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> ----<br /> '''Patent Number''': US6977262<br /> '''Assignee''': Mitsubishi Pharma Corporation<br /> '''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol3.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate<br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-methyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Methyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * t-Butyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Isopropyl 4-(2-fluorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Benzyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * 4-(2-Chlorophenyl)-5-dimethylaminocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4-(2-Chlorophenyl)-5-hydrazinocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo[3,4 -b]pyridine <br /> * 4-(2-Fluorophenyl)-4,7-dihydro-6-methyl-5-isopropylthiocarbonyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4,7-Dihydro-6-methyl-5-nitro-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b] pyridine <br /> * Ethyl 4,7-dihydro-4-phenyl-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridine-5-carbox ylate <br /> * Ethyl 4-(2-fluorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate maleate <br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridi ne-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate <br /> * Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate<br /> ----<br /> '''Patent Number''': US6664247<br /> '''Assignee''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors'''<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol4.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine<br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine<br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine<br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine<br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine<br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine<br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine<br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine<br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.<br /> ----<br /> '''Patent Number''': US2004224944<br /> '''Assignee''': VERTEX PHARMACEUTICALS INC<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol5.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine <br /> * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine<br /> <br /> === Other derivates for alopecia ===<br /> [[Image:other derivates.jpeg]]<br /> <br /> == Inhibition of 5- - reductase by Finasteride ==<br /> [[Image:5-alpha-reductase inhibition.jpeg]]<br /> <br /> === Structure-Activity Relationships (SARs) of Finasteride ===<br /> [[Image:SAR_map.gif]]<br /> <br /> == Questions Dolcera Answers ==<br /> <br /> '''What’s hot?'''<br /> * What compositions/ approaches are the most promising?<br /> * What can I license?<br /> * Can you map blockbuster products to their patents?<br /> <br /> '''Can you save me some time?'''<br /> * What combinations/ compounds have already been tried?<br /> * Is any empirical data available?<br /> * Can you tell me the side effects?<br /> <br /> '''Where should I focus my R&amp;D investment?'''<br /> * What are the most promising approaches?<br /> * Where’s the ‘white space’ for me to play in?<br /> <br /> '''Any hints for research?'''<br /> * Are there any combinations I could develop?<br /> <br /> '''What should I do in this geography?'''<br /> * What are my competitors up to in this geography?<br /> * What are my strengths/ weaknesses here?<br /> <br /> '''What’s my competition up to?'''<br /> <br /> * What’s my top competitor investing in?<br /> * Are there any loopholes in their patents?<br /> * When are their patents expiring?<br /> * Will a competitor emerge from nowhere and surprise me?<br /> * What are the crowded areas?<br /> <br /> '''How do I play defense?'''<br /> * What should my blocking/reactive strategies be?<br /> <br /> <br /> == New Combinations based on IP study? ==<br /> <br /> Yes, new Combinations can be made with '''natural products''' based on IP study<br /> * Walnut extract containing [[Image:5ar.jpg]] inhibitor (as anti-androgen) and Flavnones (for vasodilation).<br /> * Sophora Flavnones (for vasodilation) in combination with Saw Palmetto berry (as anti-androgen).<br /> <br /> '''Note:''' The above combinations are based on limited study and are only possible examples<br /> <br /> == IP studies provides ==<br /> <br /> === Technology trends ===<br /> * Use of saw palmetto berry for treating alopecia was first patented in 1996.<br /> * Since then, 144 patents (including family patents) have been filed till 2006.<br /> * Most patents use saw palmetto berry in combination with other products.<br /> [[Image:Technology1.jpg|thumb|center|700px|Technology trends]]<br /> <br /> === New opportunities ===<br /> Yes, the IP studies provide new opportunities in the following area.<br /> * Sophora Flavescens contain flavnoids.<br /> * Natural extract Sophora Flavescens cited in LG patent of 2001.<br /> * Research shows fewer than 7 patents based on Sophora Flavescens for hair loss or alopecia.<br /> <br /> * What's this?<br /> <br /> == Conclusions ==<br /> * Hair loss medication is a very active area of research and intellectual property development.<br /> * One of the most promising areas of development is the area of Anti-androgens.<br /> * The top companies are Merck, L’Oreal and Smithkline.<br /> <br /> == Useful links ==<br /> * [http://www.biocarta.com/pathfiles/h_ghPathway.asp Pathways example]<br /> * [http://www.cellsignal.com/category.asp?catalog_name=CellSignal&amp;category_name=MAPK+Signaling Signaling Pathways]<br /> <br /> == Summary ==</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss&diff=1775 2006-05-21T01:51:11Z

<p>67.180.226.207: </p> <hr /> <div>{{TOCright}}<br /> == Rationale ==<br /> * &quot;Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year.&quot; March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55]<br /> <br /> * &quot;An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries.&quot; February 16, 2006 – [http://stophair.setupmyblog.com/]<br /> <br /> * &quot;There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting.&quot; June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&amp;STORY=/www/story/06-07-2005/0003821470&amp;EDATE=]<br /> <br /> == Alopecia IPMap == <br /> [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Dolcera IPMap for Alopecia]<br /> <br /> == Introduction ==<br /> <br /> === Hair Basics ===<br /> * Hair is a complex and delicate part of the body.<br /> * Keeping it healthy and beautiful is a challenge.<br /> * Hair grows everywhere on the body with the exception of the lips, eyelids, the palms of the hands and soles of the feet.<br /> * Hair is basically a form of skin. <br /> * Hair is made up of a protein called keratin.<br /> * Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin. <br /> * Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htm]<br /> * Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.html]<br /> [[Image:Hairbasics.jpg|thumb|center|500px|Structure of Hair root and Hair bulb]]<br /> <br /> === What causes Hair loss? === <br /> * Decreased growth of the hair <br /> * Increased shedding of the hair <br /> * Breakage of hairs <br /> * Conversion of thick terminal hairs to thin vellus hairs <br /> [[Image:Facts.jpg|thumb|right|400px|Survey results from Japan]]<br /> Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed '''“Male Pattern Baldness&quot;''' or '''&quot;Androgenetic Alopecia&quot;'''.<br /> <br /> === Androgenetic Alopecia ===<br /> * Gradual Onset.<br /> * Transition from large, thick, pigmented terminal hairs to thinner, shorter, indeterminate hairs and finally to short, wispy, nonpigmented vellus hairs in the involved areas.<br /> * Characterised by a receding hairline and/or hair loss on the top of the head.<br /> <br /> '''Main Causes'''<br /> * Genetic predisposition<br /> * Hormonal effect of androgen <br /> * Reduction of blood circulation around hair follicle<br /> * Deactivation of hair matrix cells<br /> <br /> '''Some facts from Japan''' <br /> <br /> * Market size: ¥ 30 Billion<br /> * Number of products: more than 100<br /> <br /> (JICST-EPlus - Japanese Science &amp; Technology)<br /> <br /> == Goals ==<br /> <br /> The goal of this report is to:<br /> * Summarize IP activity over the years<br /> * Identify major players<br /> * Conduct patent analysis<br /> a) Composition<br /> b) Nature<br /> c) Action<br /> <br /> '''And then'''<br /> <br /> * Analyze patents pertaining to high sebum activity<br /> <br /> == Approach ==<br /> <br /> * A broad search was conducted on hair loss patents.<br /> * Patent information was sourced through SIP.<br /> * A set of patents was selected for analysis.<br /> <br /> Composition of treatment for causes are identified and categorized as follows:<br /> <br /> * Anti-androgen<br /> * Minoxidil<br /> * Double action (Anti-androgen + Mindoxidil)<br /> * Hair matrix cells activator<br /> * Sebum production inhibitor<br /> <br /> == IP activity over years ==<br /> The graph indicates:<br /> * Number of patents filed every 5 years (except for first 7 years).<br /> * First solution proposed in 1973<br /> * Filing trend indicates steep rise in activity recently.<br /> [[Image:Year1.jpg|thumb|center|400px|IP Activity over years]]<br /> <br /> == Major Players ==<br /> [[Image:players.jpg|thumb|left|400px|Assignees with more than 20 patents ]]<br /> [[Image:players1.jpg|thumb|center|400px|Assignees with fewer than 20 patents ]]<br /> <br /> * '''Active Assignees'''<br /> Assignees currently active with more than 5 patents to their credit during 2000-2005. <br /> * Warner with 9 patents,<br /> * Bristol with 6 and<br /> * Abbott with 5.<br /> <br /> [[Image:Active.jpg|thumb|center|500px|Active Assignees]]<br /> <br /> == Anti-androgens == <br /> * Anti-androgens are used in hormone therapy.<br /> * Anti-androgens are designed to affect the hormones made in the adrenal glands. They don't stop the hormones from being made, but they stop them from having an effect leading to hair loss.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Testosterone is reduced to its active metabolite, Dihydrotestosterone (DHT) by the enzyme 5 alpha reductase.<br /> * DHT attaches to androgen receptor sites at the hair follicle. <br /> * DHT causes gradual miniaturization of the follicle, which eventually results in hair loss.<br /> <br /> '''How do anti-androgens treat hair loss?'''<br /> * Anti-androgens compete with DHT to bind to the androgen receptor.<br /> * Upon binding of anti-androgen in place of DHT, follicle miniaturization is lowered and hair loss prevented.<br /> <br /> === Functions of Anti-androgen === <br /> [http://www.revivogen.com/revivogen/work.html Anti-androgen]<br /> <br /> [[Image:Andogen1.jpg|thumb|center|500px|Functions of Anti-androgen]]<br /> <br /> === IP Map for Anti-androgen ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;8&quot;, style=&quot;#008080&quot;<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> BLOTECH (2004)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Palmetto berry extract (fatty acids &amp; sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans)<br /> |bgcolor=LightCyan|Fatty acids – Inhibit testosterone<br /> Sterols - Mechanism of action unknown.<br /> <br /> Quercetin results in cell growth cycle.<br /> <br /> Beta-sitosterol reduce inflammation on scalp<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 4-cycloalkoxy benzonitrile derivatives and salts<br /> |bgcolor=LightCyan|Acts as androgen receptor modulators and blocks formation of DHT.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives.<br /> |bgcolor=LightCyan|The compounds inhibit, or decrease, activation of androgen receptor by androgens.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> APHIOS Corp (2003)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives.<br /> |bgcolor=LightCyan|Modulates androgenic activity by inhibiting 5.alpha.-reductase activity.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> Fundacion Pablo Cassara (2003)<br /> |bgcolor=LightCyan|Nucleotide<br /> |bgcolor=LightCyan|Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond)<br /> |bgcolor=LightCyan|Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> PFIZER INC (2001)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate <br /> |bgcolor=LightCyan|Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> N/A (1995)<br /> |bgcolor=LightCyan|Peptides/nucleic acid<br /> |bgcolor=LightCyan|Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein)<br /> |bgcolor=LightCyan|Inhibit synthesis of bradykinin receptors or compounds by binding to B2 receptor<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> KAO Corp (1987)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Walnut extract (leaves/pericarps) with an organic solvent<br /> |bgcolor=LightCyan|Blocks formation of DHT<br /> |}<br /> <br /> == Minoxidil ==<br /> * Minoxidil is a &quot;potassium channel opener&quot; that leads to vasodilation.<br /> * The drug is available in two forms. Oral minoxidil is used to treat high blood pressure and the topical solution form is used to treat hair loss and baldness.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * A thick network of tiny veins and arteries lines the outer wall of the follicle. Blood pumps through the bulb and hair via this network.<br /> * DHT accumulates in the hair follicles and roots, constricting the blood supply of oxygen and nutrients to the hair roots; which is also seen to possibly contribute towards hair loss.<br /> <br /> '''How does Minoxidal treat hair loss?'''<br /> * Minoxidal is applied to the scalp topically, where it dilates blood vessels in the scalp and sustains the hair follicles for longer period of time.<br /> * Scientists and researchers are not exactly sure of how Minoxidil leads to this effect.<br /> * Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.<br /> <br /> === Functions of Monoxidil === [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 Minoxidil]<br /> <br /> [[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil]]<br /> <br /> === IP Map for Minoxidil ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> WARNER LAMBERT(2002)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Benzopyran compounds<br /> |bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> LG HOUSEHOLD &amp; HEALTH CARE(2001)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Sophora flavescens extract (alkaloids &amp; flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)<br /> |bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels<br /> |}<br /> <br /> == Double action (Anti-androgen + Minoxidil) ==<br /> * Combination of Minoxidil + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.<br /> <br /> <br /> '''What is the problem with using only Anti-androgen therapy?'''<br /> * Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.<br /> * Anti-androgen only prevent binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.<br /> <br /> '''What is the problem with using only Minoxidal therapy?'''<br /> * Minoxidil-based products are generally not effective in stopping hair loss as minoxidil does not block the harmful effects of DHT in the scalp and hair follicles. <br /> * Minoxidil simply dilates blood vessels in the scalp. However, the harmful DHT is still being produced in the body and still getting into the scalp and hair follicles and causing eventual hair loss.<br /> <br /> '''How is the combination of Anti-androgens and Minoxidil effective?'''<br /> * Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.<br /> * Minoxidil causes vasodilation and therefore improves supply of oxygen and nutrients to the hair follicle and roots.<br /> * Combination therapy therefore proves to be much more effective than individual therapy.<br /> <br /> === Functions of (Anti-androgen + Minoxidil) === [http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]<br /> [[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Minoxidil)]]<br /> <br /> === IP Map for (Anti-androgen + Minoxidil) ===<br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405] <br /> N/A(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhance and sunscreen<br /> |bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577] <br /> L'OREAL(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP<br /> |bgcolor=LightCyan|Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762] <br /> COLOMER GROUP(1999)<br /> |bgcolor=LightCyan|Natural extract<br /> |bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)<br /> |bgcolor=LightCyan|Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp<br /> |}<br /> <br /> <br /> == Hair matrix cell activator ==<br /> Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.<br /> * Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.<br /> * Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.<br /> * Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.<br /> <br /> <br /> '''How does hair cell matrix activator treat hair loss?'''<br /> * Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.<br /> * This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.<br /> * Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.<br /> <br /> === Functions of Hair matrix cell activator === [http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]<br /> [[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]<br /> <br /> === IP Map for Hair matrix cell activator ===<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> SHISEIDO(1999) <br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt<br /> |bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> L'OREAL(1998) <br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions<br /> |bgcolor=LightCyan|Reducing the expression of MMPs (Metalloproteases) in the scalp - slow down or inhibit the degradation of the perifollicular matrix (extracellular matrix surround the hair follicle) <br /> |}<br /> <br /> == Sebum Production Inhibitor ==<br /> Sebum Production Inhibitor is a substance that prevents the synthesis of sebum, mixture of lipid substances.<br /> <br /> '''What causes hair loss?'''<br /> * Sebum is a fatty acid substance secreted from sebaceous glands associated with hair follicles.<br /> * Hair can get heavy sebum build-up and mixes with cholesterol to form a hardened plug around the bottom part of the hair bulb.<br /> * Hardened plugs prevent cell respirations and eventually lead to hair loss.<br /> * Bacteria will also attach to the hardened plug and this can also cause further cause problems with hair growth.<br /> <br /> '''How does Sebum production inhibitor treat hair loss?'''<br /> * The inhibitor prevents synthesis of sebum and slows down accumulation and mixing of sebum with cholesterol leading to hardened plugs. <br /> * Reduction of sebum results in unclogged hair follicles/bulbs and allows oxygen and nutrients from reaching the hair follicle.<br /> * Reduction in sebum also prevents vasoconstriction.<br /> * Sum result of these effects of Sebum production inhibitor is prevention of hair loss.<br /> <br /> <br /> * The inhibitor blocks the excessive sebum production produces greasy effect on hair and scalp and also responsible for thinning and loosing of hair.<br /> <br /> === Functions of Sebum Production Inhibitor ===<br /> [[http://en.wikipedia.org/wiki/Image:HairFollicle.jpg Sebum Production Inhibitor]]<br /> [[Image:Sebum1.jpg|thumb|center|500px|Functions of Sebum Production Inhibitor]]<br /> <br /> === IPMap for Sebum Production Inhibitor ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699] <br /> Unilever(2005)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Polyamine (putrescine, spermine or spermidine) analogs and/or derivatives; DFMO; N-acetyl cysteines; neutralized salts of a non-hydroxy C2-C40 dicarboxylic acids, preferably malonate salts; and mixtures thereof. <br /> |bgcolor=LightCyan|Decreasing sebum production and/or pore size <br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362] <br /> KAO COPR.(2004)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Avocado oil (Butyl esters of fatty acids) <br /> |bgcolor=LightCyan|Reduce sebum of the hair and scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587] <br /> Unilever(1982)<br /> |bgcolor=LightCyan|organic compound<br /> |bgcolor=LightCyan |Biotin antagonist or a salt thereof <br /> |bgcolor=LightCyan|Decrease activity of the enzyme acetyl-SCoA-carboxylase and hence reduce lipid synthesis in sebaceous glands so that less sebum is produced <br /> |}<br /> <br /> == Composition nature matrix ==<br /> <br /> === IPMap: Composition nature matrix ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;11&quot;, style=&quot;#008080&quot;<br /> !width=&quot;50&quot; bgcolor=DodgerBlue|'''Year'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Organic Compound'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extracts''' <br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Peptides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nucleotides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extract + Organic comp'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|2005 <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |- <br /> |bgcolor=LightCyan|2004 <br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|BLOTECH (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |- <br /> |bgcolor=LightCyan|2003<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|APHIOS (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|FUNDIACION (1)<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2002<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2001<br /> |bgcolor=LightCyan |PFIZER (1)<br /> |bgcolor=LightCyan|LG HEALTH-CARE (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2000<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1) / N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1999<br /> |bgcolor=LightCyan|SHISEDIO (1)<br /> |bgcolor=LightCyan|COLOMER (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1998<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1995<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |-<br /> |bgcolor=LightCyan|1987<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1982<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |}<br /> <br /> == Focus of patents ==<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;17&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Focus of patents'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Stimulating hair growth using benzopyrans<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Compositions to prevent or reduce hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Method of decreasing sebum production and pore size<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699 ]<br /> |bgcolor=LightCyan|16<br /> |- <br /> |bgcolor=LightCyan|Method for reducing sebum on the hair and skin<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |bgcolor=LightCyan|17<br /> |}<br /> <br /> === Focus of patents by technology ===<br /> [[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]<br /> <br /> == Distribution of patents ==<br /> <br /> === By patent types ===<br /> [[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]<br /> <br /> <br /> === By key ingredients ===<br /> [[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]<br /> <br /> === By target disease ===<br /> [[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]<br /> <br /> <br /> === Key ingredients vs. Target disease ===<br /> [[Image:key&amp;target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]<br /> <br /> <br /> === Target species ===<br /> [[Image:Species.jpg|thumb|center|700px|Target species]]<br /> <br /> <br /> === Mode of administration ===<br /> [[Image:Mode.jpg|thumb|center|700px|Mode of administration]]<br /> <br /> <br /> === Product type vs. Product form ===<br /> [[Image:prod.jpg|thumb|center|700px|Product type vs. Product form]]<br /> <br /> == Distribution based on different aspects ==<br /> <br /> === List of patents ===<br /> {| border=&quot;1&quot; cellpadding=&quot;9&quot;, style=&quot;#008080&quot;<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|1<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|10<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |- <br /> |bgcolor=LightCyan|2<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|11<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |- <br /> |bgcolor=LightCyan|3<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> |bgcolor=LightCyan|12<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |- <br /> |bgcolor=LightCyan|4<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427] <br /> |bgcolor=LightCyan|13<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |- <br /> |bgcolor=LightCyan|5<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282] <br /> |bgcolor=LightCyan|14<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |- <br /> |bgcolor=LightCyan|6<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467] <br /> |bgcolor=LightCyan|15<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |- <br /> |bgcolor=LightCyan|7<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|16<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699]<br /> |- <br /> |bgcolor=LightCyan|8<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|17<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |- <br /> |bgcolor=LightCyan|9<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010] <br /> |bgcolor=LightCyan|18<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |}<br /> <br /> === Patents by target diseases ===<br /> {| border=&quot;1&quot; cellpadding=&quot;16&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Target disease/ disorder'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness)<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, male pattern baldness and female pattern baldness<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|Inappropriate activation of the androgen receptor, acne, oily skin, alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Androgen-associated hair loss and androgen-skin related disorders. <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Androgenetic or androgenic alopecia or androgeno-genetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Diseases caused by testosterone (male-pattern alopecia)<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Alopecia, androgenic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Androgenetic, androgenic or androgenogenetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Curing other scalp related problems<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |bgcolor=LightCyan|16<br /> |}<br /> <br /> === Patents by application ===<br /> [[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]<br /> <br /> === Signaling Pathway and linkages ===<br /> [[Image:Slide1.GIF|thumb|center|700px|Alopecia pathways]]<br /> <br /> == Players of Wnt inhibition Pathway == [[Image:wnt.jpg|thumb|right|600px|Wnt inhibition]]<br /> {| border=&quot;1&quot; cellpadding=&quot;15&quot;, style=&quot;#008080&quot;<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Key compound'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Players of inhibition'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6989385.PN.&amp;OS=PN/6989385&amp;RS=PN/6989385 US6989385]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|CDK,GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6974819.PN.&amp;OS=PN/6974819&amp;RS=PN/6974819 US6974819]<br /> |bgcolor=LightCyan|Pyrimidine derivative<br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6743791.PN.&amp;OS=PN/6743791&amp;RS=PN/6743791 US6743791]<br /> |bgcolor=LightCyan|Heterocyclic compounds<br /> |bgcolor=LightCyan|AKT3, GSK-3, ERK2<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277773%22.PGNR.&amp;OS=DN/20050277773&amp;RS=DN/20050277773 US20050277773]<br /> |bgcolor=LightCyan|Pyrrolo[3,2-d]pyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040072836%22.PGNR.&amp;OS=DN/20040072836&amp;RS=DN/20040072836 US20040072836]<br /> |bgcolor=LightCyan|Aza-oxindole derivatives <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1477489&amp;F=0 EP1477489]<br /> |bgcolor=LightCyan|Pyrrolopyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO0056710&amp;F=0 WO0056710]<br /> |bgcolor=LightCyan|3-(Anilinomethylene) oxindoles <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO03011287&amp;F=0 WO2003011287]<br /> |bgcolor=LightCyan|Pyrazolon derivatives <br /> |bgcolor=LightCyan|GSK3, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6924141.PN.&amp;OS=PN/6924141&amp;RS=PN/6924141 US6924141]<br /> |bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7 <br /> |bgcolor=LightCyan|β-catenin, GSK3, Wnt<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6706685.PN.&amp;OS=PN/6706685&amp;RS=PN/6706685 US6706685]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6683048.PN.&amp;OS=PN/6683048&amp;RS=PN/6683048 US6683048]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|α-catenin, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6677116.PN.&amp;OS=PN/6677116&amp;RS=PN/6677116 US6677116]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6303576.PN.&amp;OS=PN/6303576&amp;RS=PN/6303576 US6303576]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |}<br /> [[Image:coloury.jpg]]- '''Target sites and Details'''<br /> <br /> == Pyrazole compounds ==<br /> <br /> * '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.<br /> * Pyrazoles are produced synthetically through the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation <br /> [[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]<br /> * Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.<br /> * Structurally related compounds are pyrazoline and pyrazolidine.<br /> [[Image:pyrazole2.jpg|thumb|center|500px|Structurally related compounds]]<br /> <br /> === GSK3 inhibition by pyrazole compounds ===<br /> [[Image:bold3.jpg]]<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?TERM1=6989385+&amp;Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=0&amp;f=S&amp;l=50 US6989385]<br /> [[Image:US6989385.jpg]]<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247] <br /> [[Image:US6664247.jpg]]<br /> !width=&quot;100&quot;|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256] <br /> [[Image:WO2005012256.jpg]]<br /> |- <br /> |bgcolor=lightcyan|R1=T-Ring D, wherein <br /> T is a valence bond and <br /> Ring D = 5-6 membered aryl or heteroaryl ring; <br /> <br /> R2 = hydrogen or C1-4 aliphatic and <br /> R2'= hydrogen; <br /> <br /> R3 = -R, -OR, or -N(R4)2, wherein <br /> R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and <br /> L is -O-, -S-, or -NH-; and <br /> Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R&lt;4&gt;), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring<br /> <br /> |bgcolor=lightcyan|X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; <br /> <br /> R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; <br /> <br /> R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and <br /> <br /> R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).<br /> <br /> |bgcolor=lightcyan|X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;<br /> A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy).<br /> |}<br /> <br /> === GSK3 inhibition by pryazole pyrimidine amine derivatives ===<br /> <br /> '''Patent Number''': US6989385<br /> '''Applicant''': ''Vertex Pharmaceuticals Incorporated''<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol1.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-p- yrimidin-4-yl]-amine <br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyl- sulfanyl]-pyrimidin-4-yl}-amine <br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-me- thyl-2H-pyrazol-3-yl)-amine <br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * {2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-y- l}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(- 5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfa- nyl)-pyrimidin-4-yl]-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mo- rpholin-4-yl-pyrimidin-4-yl}-amine <br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimi- din-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyri- midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * 5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-ylmethylsulf- anyl)-pyrimidin-4-yl]-amine <br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)-phenyl]-py- rimidin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methy- l-2H-pyrazol-3-yl)-amine <br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methylphenylamino)-6-phenyl-pyrimidi- n-4-yl]-amine <br /> * [2-(4-cyanomethylphenylamino)-6-phenyl-pyrimidin-4-yl]-(5-cyclopropyl-2H-p- yrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(pyridin-3-ylmethylamino)-pyri- midin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-methyl-2H-py- razol-3-yl)-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3,4,5-trimethoxyphenyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(4-sulfamoylphenylamino)-6-(3,4,5-trimethoxy- phenyl)-pyrimidin-4-yl]-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyraz- ol-3-yl]-amine <br /> * [2-(Benzimidazol-2-ylamino-)6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * (5-tert-Butyl-2H-pyrazol-3-yl)-[2-(3-chlorophenyl)amino-6-(3-nitrophenyl)-- pyrimidin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-phenyl-2H-py- razol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-a- mine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-[5-(Furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * [2-(4-Chlorophenylamino)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * (5,6-Dimethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Chlorophenyl)amino-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * (6-Methoxymethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-- amine <br /> * (6-Methyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyr- azol-3-yl]-amine <br /> * (6-methyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-phenyl-2H-pyrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenoxymethyl-pyrimidin-4-yl)- -amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-amine <br /> * [6-Methyl-2-(4-methyl-phenylsulfanylmethyl)-pyrimidin-4-yl]-(5-phenyl-2H-p- yrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-[6-Methyl-2-(4-methyl-phenylsulfanylmethy- l)-pyrimidin-4-yl]-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * (6-Ethyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)- -amine <br /> * (6-Ethyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Ethyl-2-(4-fluorophenoxymethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [6-Ethyl-2-(1-methyl-1-phenyl-ethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-p- yrazol-3-yl]-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(2-phenylsulfanylmethyl-5,6,7,8-tetrahydro-quin- azolin-4-yl)-amine <br /> * [2-(4-Methylphenylsulfanylmethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidi- n-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(1-Methyl-1-phenyl-ethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-y- l]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6,7,8-tetrahydro-quinazolin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * [7-Benzyl-2-(2,6-dichlorobenzyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-- 4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Benzyl-2-(4-chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimi- din-4-yl]-(5-methyl-2H-pyrazol-3-yl)-<br /> * [2-(4-Chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> ----<br /> '''Patent Number''': US7008948 <br /> '''Applicant''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure'''<br /> <br /> [[Image:pyrazol2.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(1H-i- ndazol-3-yl)-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[3,4-d]pyrimidin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(7-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5,7-- difluoro-1H-indazol-3-yl)-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetra- hydroquinazolin-4-yl]-amine <br /> * (5-Trifluoromethyl-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-- tetrahydroquinazolin-4-yl]-amine <br /> * (5,7-difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetra- hydro-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (6-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyr- imidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydro-5H-cycl- oheptapyrimidin-4-yl]-amine<br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[4,3-d]pyrimidin-4-yl]-amine<br /> * (1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydroquinazol- in-4-yl]-amine <br /> * (7-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine<br /> * (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> * 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> ----<br /> '''Patent Number''': US6977262<br /> '''Assignee''': Mitsubishi Pharma Corporation<br /> '''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol3.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate<br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-methyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Methyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * t-Butyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Isopropyl 4-(2-fluorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Benzyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * 4-(2-Chlorophenyl)-5-dimethylaminocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4-(2-Chlorophenyl)-5-hydrazinocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo[3,4 -b]pyridine <br /> * 4-(2-Fluorophenyl)-4,7-dihydro-6-methyl-5-isopropylthiocarbonyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4,7-Dihydro-6-methyl-5-nitro-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b] pyridine <br /> * Ethyl 4,7-dihydro-4-phenyl-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridine-5-carbox ylate <br /> * Ethyl 4-(2-fluorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate maleate <br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridi ne-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate <br /> * Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate<br /> ----<br /> '''Patent Number''': US6664247<br /> '''Assignee''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors'''<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol4.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine<br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine<br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine<br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine<br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine<br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine<br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine<br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine<br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.<br /> ----<br /> '''Patent Number''': US2004224944<br /> '''Assignee''': VERTEX PHARMACEUTICALS INC<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol5.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine <br /> * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine<br /> <br /> === Other derivates for alopecia ===<br /> [[Image:other derivates.jpeg]]<br /> <br /> == Inhibition of 5- - reductase by Finasteride ==<br /> [[Image:5-alpha-reductase inhibition.jpeg]]<br /> <br /> === Structure-Activity Relationships (SARs) of Finasteride ===<br /> [[Image:SAR_map.gif]]<br /> <br /> == Questions Dolcera Answers ==<br /> <br /> '''What’s hot?'''<br /> * What compositions/ approaches are the most promising?<br /> * What can I license?<br /> * Can you map blockbuster products to their patents?<br /> <br /> '''Can you save me some time?'''<br /> * What combinations/ compounds have already been tried?<br /> * Is any empirical data available?<br /> * Can you tell me the side effects?<br /> <br /> '''Where should I focus my R&amp;D investment?'''<br /> * What are the most promising approaches?<br /> * Where’s the ‘white space’ for me to play in?<br /> <br /> '''Any hints for research?'''<br /> * Are there any combinations I could develop?<br /> <br /> '''What should I do in this geography?'''<br /> * What are my competitors up to in this geography?<br /> * What are my strengths/ weaknesses here?<br /> <br /> '''What’s my competition up to?'''<br /> <br /> * What’s my top competitor investing in?<br /> * Are there any loopholes in their patents?<br /> * When are their patents expiring?<br /> * Will a competitor emerge from nowhere and surprise me?<br /> * What are the crowded areas?<br /> <br /> '''How do I play defense?'''<br /> * What should my blocking/reactive strategies be?<br /> <br /> <br /> == New Combinations based on IP study? ==<br /> <br /> Yes, new Combinations can be made with '''natural products''' based on IP study<br /> * Walnut extract containing [[Image:5ar.jpg]] inhibitor (as anti-androgen) and Flavnones (for vasodilation).<br /> * Sophora Flavnones (for vasodilation) in combination with Saw Palmetto berry (as anti-androgen).<br /> <br /> '''Note:''' The above combinations are based on limited study and are only possible examples<br /> <br /> == IP studies provides ==<br /> <br /> === Technology trends ===<br /> * Use of saw palmetto berry for treating alopecia was first patented in 1996.<br /> * Since then, 144 patents (including family patents) have been filed till 2006.<br /> * Most patents use saw palmetto berry in combination with other products.<br /> [[Image:Technology1.jpg|thumb|center|700px|Technology trends]]<br /> <br /> === New opportunities ===<br /> Yes, the IP studies provide new opportunities in the following area.<br /> * Sophora Flavescens contain flavnoids.<br /> * Natural extract Sophora Flavescens cited in LG patent of 2001.<br /> * Research shows fewer than 7 patents based on Sophora Flavescens for hair loss or alopecia.<br /> <br /> * What's this?<br /> <br /> == Conclusions ==<br /> * Hair loss medication is a very active area of research and intellectual property development.<br /> * One of the most promising areas of development is the area of Anti-androgens.<br /> * The top companies are Merck, L’Oreal and Smithkline.<br /> <br /> == Useful links ==<br /> * [http://www.biocarta.com/pathfiles/h_ghPathway.asp Pathways example]<br /> * [http://www.cellsignal.com/category.asp?catalog_name=CellSignal&amp;category_name=MAPK+Signaling Signaling Pathways]<br /> <br /> == Summary ==</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss&diff=1774 2006-05-21T01:50:25Z

<p>67.180.226.207: /* Other derivates used by different assigness for the treatment of alopecia */</p> <hr /> <div>{{TOCleft}}<br /> == Rationale ==<br /> * &quot;Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year.&quot; March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55]<br /> <br /> * &quot;An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries.&quot; February 16, 2006 – [http://stophair.setupmyblog.com/]<br /> <br /> * &quot;There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting.&quot; June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&amp;STORY=/www/story/06-07-2005/0003821470&amp;EDATE=]<br /> <br /> == Alopecia IPMap == <br /> [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Dolcera IPMap for Alopecia]<br /> <br /> == Introduction ==<br /> <br /> === Hair Basics ===<br /> * Hair is a complex and delicate part of the body.<br /> * Keeping it healthy and beautiful is a challenge.<br /> * Hair grows everywhere on the body with the exception of the lips, eyelids, the palms of the hands and soles of the feet.<br /> * Hair is basically a form of skin. <br /> * Hair is made up of a protein called keratin.<br /> * Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin. <br /> * Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htm]<br /> * Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.html]<br /> [[Image:Hairbasics.jpg|thumb|center|500px|Structure of Hair root and Hair bulb]]<br /> <br /> === What causes Hair loss? === <br /> * Decreased growth of the hair <br /> * Increased shedding of the hair <br /> * Breakage of hairs <br /> * Conversion of thick terminal hairs to thin vellus hairs <br /> [[Image:Facts.jpg|thumb|right|400px|Survey results from Japan]]<br /> Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed '''“Male Pattern Baldness&quot;''' or '''&quot;Androgenetic Alopecia&quot;'''.<br /> <br /> === Androgenetic Alopecia ===<br /> * Gradual Onset.<br /> * Transition from large, thick, pigmented terminal hairs to thinner, shorter, indeterminate hairs and finally to short, wispy, nonpigmented vellus hairs in the involved areas.<br /> * Characterised by a receding hairline and/or hair loss on the top of the head.<br /> <br /> '''Main Causes'''<br /> * Genetic predisposition<br /> * Hormonal effect of androgen <br /> * Reduction of blood circulation around hair follicle<br /> * Deactivation of hair matrix cells<br /> <br /> '''Some facts from Japan''' <br /> <br /> * Market size: ¥ 30 Billion<br /> * Number of products: more than 100<br /> <br /> (JICST-EPlus - Japanese Science &amp; Technology)<br /> <br /> == Goals ==<br /> <br /> The goal of this report is to:<br /> * Summarize IP activity over the years<br /> * Identify major players<br /> * Conduct patent analysis<br /> a) Composition<br /> b) Nature<br /> c) Action<br /> <br /> '''And then'''<br /> <br /> * Analyze patents pertaining to high sebum activity<br /> <br /> == Approach ==<br /> <br /> * A broad search was conducted on hair loss patents.<br /> * Patent information was sourced through SIP.<br /> * A set of patents was selected for analysis.<br /> <br /> Composition of treatment for causes are identified and categorized as follows:<br /> <br /> * Anti-androgen<br /> * Minoxidil<br /> * Double action (Anti-androgen + Mindoxidil)<br /> * Hair matrix cells activator<br /> * Sebum production inhibitor<br /> <br /> == IP activity over years ==<br /> The graph indicates:<br /> * Number of patents filed every 5 years (except for first 7 years).<br /> * First solution proposed in 1973<br /> * Filing trend indicates steep rise in activity recently.<br /> [[Image:Year1.jpg|thumb|center|400px|IP Activity over years]]<br /> <br /> == Major Players ==<br /> [[Image:players.jpg|thumb|left|400px|Assignees with more than 20 patents ]]<br /> [[Image:players1.jpg|thumb|center|400px|Assignees with fewer than 20 patents ]]<br /> <br /> * '''Active Assignees'''<br /> Assignees currently active with more than 5 patents to their credit during 2000-2005. <br /> * Warner with 9 patents,<br /> * Bristol with 6 and<br /> * Abbott with 5.<br /> <br /> [[Image:Active.jpg|thumb|center|500px|Active Assignees]]<br /> <br /> == Anti-androgens == <br /> * Anti-androgens are used in hormone therapy.<br /> * Anti-androgens are designed to affect the hormones made in the adrenal glands. They don't stop the hormones from being made, but they stop them from having an effect leading to hair loss.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Testosterone is reduced to its active metabolite, Dihydrotestosterone (DHT) by the enzyme 5 alpha reductase.<br /> * DHT attaches to androgen receptor sites at the hair follicle. <br /> * DHT causes gradual miniaturization of the follicle, which eventually results in hair loss.<br /> <br /> '''How do anti-androgens treat hair loss?'''<br /> * Anti-androgens compete with DHT to bind to the androgen receptor.<br /> * Upon binding of anti-androgen in place of DHT, follicle miniaturization is lowered and hair loss prevented.<br /> <br /> === Functions of Anti-androgen === <br /> [http://www.revivogen.com/revivogen/work.html Anti-androgen]<br /> <br /> [[Image:Andogen1.jpg|thumb|center|500px|Functions of Anti-androgen]]<br /> <br /> === IP Map for Anti-androgen ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;8&quot;, style=&quot;#008080&quot;<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> BLOTECH (2004)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Palmetto berry extract (fatty acids &amp; sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans)<br /> |bgcolor=LightCyan|Fatty acids – Inhibit testosterone<br /> Sterols - Mechanism of action unknown.<br /> <br /> Quercetin results in cell growth cycle.<br /> <br /> Beta-sitosterol reduce inflammation on scalp<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 4-cycloalkoxy benzonitrile derivatives and salts<br /> |bgcolor=LightCyan|Acts as androgen receptor modulators and blocks formation of DHT.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives.<br /> |bgcolor=LightCyan|The compounds inhibit, or decrease, activation of androgen receptor by androgens.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> APHIOS Corp (2003)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives.<br /> |bgcolor=LightCyan|Modulates androgenic activity by inhibiting 5.alpha.-reductase activity.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> Fundacion Pablo Cassara (2003)<br /> |bgcolor=LightCyan|Nucleotide<br /> |bgcolor=LightCyan|Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond)<br /> |bgcolor=LightCyan|Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> PFIZER INC (2001)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate <br /> |bgcolor=LightCyan|Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> N/A (1995)<br /> |bgcolor=LightCyan|Peptides/nucleic acid<br /> |bgcolor=LightCyan|Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein)<br /> |bgcolor=LightCyan|Inhibit synthesis of bradykinin receptors or compounds by binding to B2 receptor<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> KAO Corp (1987)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Walnut extract (leaves/pericarps) with an organic solvent<br /> |bgcolor=LightCyan|Blocks formation of DHT<br /> |}<br /> <br /> == Minoxidil ==<br /> * Minoxidil is a &quot;potassium channel opener&quot; that leads to vasodilation.<br /> * The drug is available in two forms. Oral minoxidil is used to treat high blood pressure and the topical solution form is used to treat hair loss and baldness.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * A thick network of tiny veins and arteries lines the outer wall of the follicle. Blood pumps through the bulb and hair via this network.<br /> * DHT accumulates in the hair follicles and roots, constricting the blood supply of oxygen and nutrients to the hair roots; which is also seen to possibly contribute towards hair loss.<br /> <br /> '''How does Minoxidal treat hair loss?'''<br /> * Minoxidal is applied to the scalp topically, where it dilates blood vessels in the scalp and sustains the hair follicles for longer period of time.<br /> * Scientists and researchers are not exactly sure of how Minoxidil leads to this effect.<br /> * Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.<br /> <br /> === Functions of Monoxidil === [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 Minoxidil]<br /> <br /> [[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil]]<br /> <br /> === IP Map for Minoxidil ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> WARNER LAMBERT(2002)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Benzopyran compounds<br /> |bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> LG HOUSEHOLD &amp; HEALTH CARE(2001)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Sophora flavescens extract (alkaloids &amp; flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)<br /> |bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels<br /> |}<br /> <br /> == Double action (Anti-androgen + Minoxidil) ==<br /> * Combination of Minoxidil + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.<br /> <br /> <br /> '''What is the problem with using only Anti-androgen therapy?'''<br /> * Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.<br /> * Anti-androgen only prevent binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.<br /> <br /> '''What is the problem with using only Minoxidal therapy?'''<br /> * Minoxidil-based products are generally not effective in stopping hair loss as minoxidil does not block the harmful effects of DHT in the scalp and hair follicles. <br /> * Minoxidil simply dilates blood vessels in the scalp. However, the harmful DHT is still being produced in the body and still getting into the scalp and hair follicles and causing eventual hair loss.<br /> <br /> '''How is the combination of Anti-androgens and Minoxidil effective?'''<br /> * Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.<br /> * Minoxidil causes vasodilation and therefore improves supply of oxygen and nutrients to the hair follicle and roots.<br /> * Combination therapy therefore proves to be much more effective than individual therapy.<br /> <br /> === Functions of (Anti-androgen + Minoxidil) === [http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]<br /> [[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Minoxidil)]]<br /> <br /> === IP Map for (Anti-androgen + Minoxidil) ===<br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405] <br /> N/A(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhance and sunscreen<br /> |bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577] <br /> L'OREAL(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP<br /> |bgcolor=LightCyan|Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762] <br /> COLOMER GROUP(1999)<br /> |bgcolor=LightCyan|Natural extract<br /> |bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)<br /> |bgcolor=LightCyan|Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp<br /> |}<br /> <br /> <br /> == Hair matrix cell activator ==<br /> Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.<br /> * Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.<br /> * Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.<br /> * Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.<br /> <br /> <br /> '''How does hair cell matrix activator treat hair loss?'''<br /> * Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.<br /> * This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.<br /> * Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.<br /> <br /> === Functions of Hair matrix cell activator === [http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]<br /> [[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]<br /> <br /> === IP Map for Hair matrix cell activator ===<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> SHISEIDO(1999) <br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt<br /> |bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> L'OREAL(1998) <br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions<br /> |bgcolor=LightCyan|Reducing the expression of MMPs (Metalloproteases) in the scalp - slow down or inhibit the degradation of the perifollicular matrix (extracellular matrix surround the hair follicle) <br /> |}<br /> <br /> == Sebum Production Inhibitor ==<br /> Sebum Production Inhibitor is a substance that prevents the synthesis of sebum, mixture of lipid substances.<br /> <br /> '''What causes hair loss?'''<br /> * Sebum is a fatty acid substance secreted from sebaceous glands associated with hair follicles.<br /> * Hair can get heavy sebum build-up and mixes with cholesterol to form a hardened plug around the bottom part of the hair bulb.<br /> * Hardened plugs prevent cell respirations and eventually lead to hair loss.<br /> * Bacteria will also attach to the hardened plug and this can also cause further cause problems with hair growth.<br /> <br /> '''How does Sebum production inhibitor treat hair loss?'''<br /> * The inhibitor prevents synthesis of sebum and slows down accumulation and mixing of sebum with cholesterol leading to hardened plugs. <br /> * Reduction of sebum results in unclogged hair follicles/bulbs and allows oxygen and nutrients from reaching the hair follicle.<br /> * Reduction in sebum also prevents vasoconstriction.<br /> * Sum result of these effects of Sebum production inhibitor is prevention of hair loss.<br /> <br /> <br /> * The inhibitor blocks the excessive sebum production produces greasy effect on hair and scalp and also responsible for thinning and loosing of hair.<br /> <br /> === Functions of Sebum Production Inhibitor ===<br /> [[http://en.wikipedia.org/wiki/Image:HairFollicle.jpg Sebum Production Inhibitor]]<br /> [[Image:Sebum1.jpg|thumb|center|500px|Functions of Sebum Production Inhibitor]]<br /> <br /> === IPMap for Sebum Production Inhibitor ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699] <br /> Unilever(2005)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Polyamine (putrescine, spermine or spermidine) analogs and/or derivatives; DFMO; N-acetyl cysteines; neutralized salts of a non-hydroxy C2-C40 dicarboxylic acids, preferably malonate salts; and mixtures thereof. <br /> |bgcolor=LightCyan|Decreasing sebum production and/or pore size <br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362] <br /> KAO COPR.(2004)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Avocado oil (Butyl esters of fatty acids) <br /> |bgcolor=LightCyan|Reduce sebum of the hair and scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587] <br /> Unilever(1982)<br /> |bgcolor=LightCyan|organic compound<br /> |bgcolor=LightCyan |Biotin antagonist or a salt thereof <br /> |bgcolor=LightCyan|Decrease activity of the enzyme acetyl-SCoA-carboxylase and hence reduce lipid synthesis in sebaceous glands so that less sebum is produced <br /> |}<br /> <br /> == Composition nature matrix ==<br /> <br /> === IPMap: Composition nature matrix ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;11&quot;, style=&quot;#008080&quot;<br /> !width=&quot;50&quot; bgcolor=DodgerBlue|'''Year'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Organic Compound'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extracts''' <br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Peptides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nucleotides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extract + Organic comp'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|2005 <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |- <br /> |bgcolor=LightCyan|2004 <br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|BLOTECH (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |- <br /> |bgcolor=LightCyan|2003<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|APHIOS (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|FUNDIACION (1)<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2002<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2001<br /> |bgcolor=LightCyan |PFIZER (1)<br /> |bgcolor=LightCyan|LG HEALTH-CARE (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2000<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1) / N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1999<br /> |bgcolor=LightCyan|SHISEDIO (1)<br /> |bgcolor=LightCyan|COLOMER (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1998<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1995<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |-<br /> |bgcolor=LightCyan|1987<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1982<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |}<br /> <br /> == Focus of patents ==<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;17&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Focus of patents'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Stimulating hair growth using benzopyrans<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Compositions to prevent or reduce hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Method of decreasing sebum production and pore size<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699 ]<br /> |bgcolor=LightCyan|16<br /> |- <br /> |bgcolor=LightCyan|Method for reducing sebum on the hair and skin<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |bgcolor=LightCyan|17<br /> |}<br /> <br /> === Focus of patents by technology ===<br /> [[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]<br /> <br /> == Distribution of patents ==<br /> <br /> === By patent types ===<br /> [[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]<br /> <br /> <br /> === By key ingredients ===<br /> [[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]<br /> <br /> === By target disease ===<br /> [[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]<br /> <br /> <br /> === Key ingredients vs. Target disease ===<br /> [[Image:key&amp;target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]<br /> <br /> <br /> === Target species ===<br /> [[Image:Species.jpg|thumb|center|700px|Target species]]<br /> <br /> <br /> === Mode of administration ===<br /> [[Image:Mode.jpg|thumb|center|700px|Mode of administration]]<br /> <br /> <br /> === Product type vs. Product form ===<br /> [[Image:prod.jpg|thumb|center|700px|Product type vs. Product form]]<br /> <br /> == Distribution based on different aspects ==<br /> <br /> === List of patents ===<br /> {| border=&quot;1&quot; cellpadding=&quot;9&quot;, style=&quot;#008080&quot;<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|1<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|10<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |- <br /> |bgcolor=LightCyan|2<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|11<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |- <br /> |bgcolor=LightCyan|3<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> |bgcolor=LightCyan|12<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |- <br /> |bgcolor=LightCyan|4<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427] <br /> |bgcolor=LightCyan|13<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |- <br /> |bgcolor=LightCyan|5<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282] <br /> |bgcolor=LightCyan|14<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |- <br /> |bgcolor=LightCyan|6<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467] <br /> |bgcolor=LightCyan|15<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |- <br /> |bgcolor=LightCyan|7<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|16<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699]<br /> |- <br /> |bgcolor=LightCyan|8<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|17<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |- <br /> |bgcolor=LightCyan|9<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010] <br /> |bgcolor=LightCyan|18<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |}<br /> <br /> === Patents by target diseases ===<br /> {| border=&quot;1&quot; cellpadding=&quot;16&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Target disease/ disorder'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness)<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, male pattern baldness and female pattern baldness<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|Inappropriate activation of the androgen receptor, acne, oily skin, alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Androgen-associated hair loss and androgen-skin related disorders. <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Androgenetic or androgenic alopecia or androgeno-genetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Diseases caused by testosterone (male-pattern alopecia)<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Alopecia, androgenic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Androgenetic, androgenic or androgenogenetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Curing other scalp related problems<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |bgcolor=LightCyan|16<br /> |}<br /> <br /> === Patents by application ===<br /> [[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]<br /> <br /> === Signaling Pathway and linkages ===<br /> [[Image:Slide1.GIF|thumb|center|700px|Alopecia pathways]]<br /> <br /> == Players of Wnt inhibition Pathway == [[Image:wnt.jpg|thumb|right|600px|Wnt inhibition]]<br /> {| border=&quot;1&quot; cellpadding=&quot;15&quot;, style=&quot;#008080&quot;<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Key compound'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Players of inhibition'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6989385.PN.&amp;OS=PN/6989385&amp;RS=PN/6989385 US6989385]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|CDK,GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6974819.PN.&amp;OS=PN/6974819&amp;RS=PN/6974819 US6974819]<br /> |bgcolor=LightCyan|Pyrimidine derivative<br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6743791.PN.&amp;OS=PN/6743791&amp;RS=PN/6743791 US6743791]<br /> |bgcolor=LightCyan|Heterocyclic compounds<br /> |bgcolor=LightCyan|AKT3, GSK-3, ERK2<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277773%22.PGNR.&amp;OS=DN/20050277773&amp;RS=DN/20050277773 US20050277773]<br /> |bgcolor=LightCyan|Pyrrolo[3,2-d]pyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040072836%22.PGNR.&amp;OS=DN/20040072836&amp;RS=DN/20040072836 US20040072836]<br /> |bgcolor=LightCyan|Aza-oxindole derivatives <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1477489&amp;F=0 EP1477489]<br /> |bgcolor=LightCyan|Pyrrolopyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO0056710&amp;F=0 WO0056710]<br /> |bgcolor=LightCyan|3-(Anilinomethylene) oxindoles <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO03011287&amp;F=0 WO2003011287]<br /> |bgcolor=LightCyan|Pyrazolon derivatives <br /> |bgcolor=LightCyan|GSK3, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6924141.PN.&amp;OS=PN/6924141&amp;RS=PN/6924141 US6924141]<br /> |bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7 <br /> |bgcolor=LightCyan|β-catenin, GSK3, Wnt<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6706685.PN.&amp;OS=PN/6706685&amp;RS=PN/6706685 US6706685]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6683048.PN.&amp;OS=PN/6683048&amp;RS=PN/6683048 US6683048]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|α-catenin, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6677116.PN.&amp;OS=PN/6677116&amp;RS=PN/6677116 US6677116]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6303576.PN.&amp;OS=PN/6303576&amp;RS=PN/6303576 US6303576]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |}<br /> [[Image:coloury.jpg]]- '''Target sites and Details'''<br /> <br /> == Pyrazole compounds ==<br /> <br /> * '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.<br /> * Pyrazoles are produced synthetically through the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation <br /> [[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]<br /> * Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.<br /> * Structurally related compounds are pyrazoline and pyrazolidine.<br /> [[Image:pyrazole2.jpg|thumb|center|500px|Structurally related compounds]]<br /> <br /> === GSK3 inhibition by pyrazole compounds ===<br /> [[Image:bold3.jpg]]<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?TERM1=6989385+&amp;Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=0&amp;f=S&amp;l=50 US6989385]<br /> [[Image:US6989385.jpg]]<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247] <br /> [[Image:US6664247.jpg]]<br /> !width=&quot;100&quot;|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256] <br /> [[Image:WO2005012256.jpg]]<br /> |- <br /> |bgcolor=lightcyan|R1=T-Ring D, wherein <br /> T is a valence bond and <br /> Ring D = 5-6 membered aryl or heteroaryl ring; <br /> <br /> R2 = hydrogen or C1-4 aliphatic and <br /> R2'= hydrogen; <br /> <br /> R3 = -R, -OR, or -N(R4)2, wherein <br /> R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and <br /> L is -O-, -S-, or -NH-; and <br /> Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R&lt;4&gt;), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring<br /> <br /> |bgcolor=lightcyan|X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; <br /> <br /> R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; <br /> <br /> R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and <br /> <br /> R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).<br /> <br /> |bgcolor=lightcyan|X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;<br /> A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy).<br /> |}<br /> <br /> === GSK3 inhibition by pryazole pyrimidine amine derivatives ===<br /> <br /> '''Patent Number''': US6989385<br /> '''Applicant''': ''Vertex Pharmaceuticals Incorporated''<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol1.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-p- yrimidin-4-yl]-amine <br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyl- sulfanyl]-pyrimidin-4-yl}-amine <br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-me- thyl-2H-pyrazol-3-yl)-amine <br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * {2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-y- l}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(- 5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfa- nyl)-pyrimidin-4-yl]-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mo- rpholin-4-yl-pyrimidin-4-yl}-amine <br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimi- din-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyri- midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * 5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-ylmethylsulf- anyl)-pyrimidin-4-yl]-amine <br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)-phenyl]-py- rimidin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methy- l-2H-pyrazol-3-yl)-amine <br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methylphenylamino)-6-phenyl-pyrimidi- n-4-yl]-amine <br /> * [2-(4-cyanomethylphenylamino)-6-phenyl-pyrimidin-4-yl]-(5-cyclopropyl-2H-p- yrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(pyridin-3-ylmethylamino)-pyri- midin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-methyl-2H-py- razol-3-yl)-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3,4,5-trimethoxyphenyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(4-sulfamoylphenylamino)-6-(3,4,5-trimethoxy- phenyl)-pyrimidin-4-yl]-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyraz- ol-3-yl]-amine <br /> * [2-(Benzimidazol-2-ylamino-)6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * (5-tert-Butyl-2H-pyrazol-3-yl)-[2-(3-chlorophenyl)amino-6-(3-nitrophenyl)-- pyrimidin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-phenyl-2H-py- razol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-a- mine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-[5-(Furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * [2-(4-Chlorophenylamino)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * (5,6-Dimethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Chlorophenyl)amino-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * (6-Methoxymethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-- amine <br /> * (6-Methyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyr- azol-3-yl]-amine <br /> * (6-methyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-phenyl-2H-pyrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenoxymethyl-pyrimidin-4-yl)- -amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-amine <br /> * [6-Methyl-2-(4-methyl-phenylsulfanylmethyl)-pyrimidin-4-yl]-(5-phenyl-2H-p- yrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-[6-Methyl-2-(4-methyl-phenylsulfanylmethy- l)-pyrimidin-4-yl]-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * (6-Ethyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)- -amine <br /> * (6-Ethyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Ethyl-2-(4-fluorophenoxymethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [6-Ethyl-2-(1-methyl-1-phenyl-ethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-p- yrazol-3-yl]-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(2-phenylsulfanylmethyl-5,6,7,8-tetrahydro-quin- azolin-4-yl)-amine <br /> * [2-(4-Methylphenylsulfanylmethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidi- n-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(1-Methyl-1-phenyl-ethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-y- l]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6,7,8-tetrahydro-quinazolin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * [7-Benzyl-2-(2,6-dichlorobenzyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-- 4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Benzyl-2-(4-chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimi- din-4-yl]-(5-methyl-2H-pyrazol-3-yl)-<br /> * [2-(4-Chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> ----<br /> '''Patent Number''': US7008948 <br /> '''Applicant''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure'''<br /> <br /> [[Image:pyrazol2.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(1H-i- ndazol-3-yl)-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[3,4-d]pyrimidin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(7-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5,7-- difluoro-1H-indazol-3-yl)-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetra- hydroquinazolin-4-yl]-amine <br /> * (5-Trifluoromethyl-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-- tetrahydroquinazolin-4-yl]-amine <br /> * (5,7-difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetra- hydro-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (6-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyr- imidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydro-5H-cycl- oheptapyrimidin-4-yl]-amine<br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[4,3-d]pyrimidin-4-yl]-amine<br /> * (1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydroquinazol- in-4-yl]-amine <br /> * (7-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine<br /> * (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> * 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> ----<br /> '''Patent Number''': US6977262<br /> '''Assignee''': Mitsubishi Pharma Corporation<br /> '''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol3.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate<br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-methyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Methyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * t-Butyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Isopropyl 4-(2-fluorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Benzyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * 4-(2-Chlorophenyl)-5-dimethylaminocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4-(2-Chlorophenyl)-5-hydrazinocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo[3,4 -b]pyridine <br /> * 4-(2-Fluorophenyl)-4,7-dihydro-6-methyl-5-isopropylthiocarbonyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4,7-Dihydro-6-methyl-5-nitro-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b] pyridine <br /> * Ethyl 4,7-dihydro-4-phenyl-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridine-5-carbox ylate <br /> * Ethyl 4-(2-fluorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate maleate <br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridi ne-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate <br /> * Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate<br /> ----<br /> '''Patent Number''': US6664247<br /> '''Assignee''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors'''<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol4.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine<br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine<br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine<br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine<br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine<br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine<br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine<br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine<br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.<br /> ----<br /> '''Patent Number''': US2004224944<br /> '''Assignee''': VERTEX PHARMACEUTICALS INC<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol5.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine <br /> * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine<br /> <br /> === Other derivates for alopecia ===<br /> [[Image:other derivates.jpeg]]<br /> <br /> == Inhibition of 5- - reductase by Finasteride ==<br /> [[Image:5-alpha-reductase inhibition.jpeg]]<br /> <br /> === Structure-Activity Relationships (SARs) of Finasteride ===<br /> [[Image:SAR_map.gif]]<br /> <br /> == Questions Dolcera Answers ==<br /> <br /> '''What’s hot?'''<br /> * What compositions/ approaches are the most promising?<br /> * What can I license?<br /> * Can you map blockbuster products to their patents?<br /> <br /> '''Can you save me some time?'''<br /> * What combinations/ compounds have already been tried?<br /> * Is any empirical data available?<br /> * Can you tell me the side effects?<br /> <br /> '''Where should I focus my R&amp;D investment?'''<br /> * What are the most promising approaches?<br /> * Where’s the ‘white space’ for me to play in?<br /> <br /> '''Any hints for research?'''<br /> * Are there any combinations I could develop?<br /> <br /> '''What should I do in this geography?'''<br /> * What are my competitors up to in this geography?<br /> * What are my strengths/ weaknesses here?<br /> <br /> '''What’s my competition up to?'''<br /> <br /> * What’s my top competitor investing in?<br /> * Are there any loopholes in their patents?<br /> * When are their patents expiring?<br /> * Will a competitor emerge from nowhere and surprise me?<br /> * What are the crowded areas?<br /> <br /> '''How do I play defense?'''<br /> * What should my blocking/reactive strategies be?<br /> <br /> <br /> == New Combinations based on IP study? ==<br /> <br /> Yes, new Combinations can be made with '''natural products''' based on IP study<br /> * Walnut extract containing [[Image:5ar.jpg]] inhibitor (as anti-androgen) and Flavnones (for vasodilation).<br /> * Sophora Flavnones (for vasodilation) in combination with Saw Palmetto berry (as anti-androgen).<br /> <br /> '''Note:''' The above combinations are based on limited study and are only possible examples<br /> <br /> == IP studies provides ==<br /> <br /> === Technology trends ===<br /> * Use of saw palmetto berry for treating alopecia was first patented in 1996.<br /> * Since then, 144 patents (including family patents) have been filed till 2006.<br /> * Most patents use saw palmetto berry in combination with other products.<br /> [[Image:Technology1.jpg|thumb|center|700px|Technology trends]]<br /> <br /> === New opportunities ===<br /> Yes, the IP studies provide new opportunities in the following area.<br /> * Sophora Flavescens contain flavnoids.<br /> * Natural extract Sophora Flavescens cited in LG patent of 2001.<br /> * Research shows fewer than 7 patents based on Sophora Flavescens for hair loss or alopecia.<br /> <br /> * What's this?<br /> <br /> == Conclusions ==<br /> * Hair loss medication is a very active area of research and intellectual property development.<br /> * One of the most promising areas of development is the area of Anti-androgens.<br /> * The top companies are Merck, L’Oreal and Smithkline.<br /> <br /> == Useful links ==<br /> * [http://www.biocarta.com/pathfiles/h_ghPathway.asp Pathways example]<br /> * [http://www.cellsignal.com/category.asp?catalog_name=CellSignal&amp;category_name=MAPK+Signaling Signaling Pathways]<br /> <br /> == Summary ==</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss&diff=1773 2006-05-21T01:49:57Z

<p>67.180.226.207: </p> <hr /> <div>{{TOCleft}}<br /> == Rationale ==<br /> * &quot;Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year.&quot; March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55]<br /> <br /> * &quot;An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries.&quot; February 16, 2006 – [http://stophair.setupmyblog.com/]<br /> <br /> * &quot;There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting.&quot; June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&amp;STORY=/www/story/06-07-2005/0003821470&amp;EDATE=]<br /> <br /> == Alopecia IPMap == <br /> [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Dolcera IPMap for Alopecia]<br /> <br /> == Introduction ==<br /> <br /> === Hair Basics ===<br /> * Hair is a complex and delicate part of the body.<br /> * Keeping it healthy and beautiful is a challenge.<br /> * Hair grows everywhere on the body with the exception of the lips, eyelids, the palms of the hands and soles of the feet.<br /> * Hair is basically a form of skin. <br /> * Hair is made up of a protein called keratin.<br /> * Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin. <br /> * Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htm]<br /> * Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.html]<br /> [[Image:Hairbasics.jpg|thumb|center|500px|Structure of Hair root and Hair bulb]]<br /> <br /> === What causes Hair loss? === <br /> * Decreased growth of the hair <br /> * Increased shedding of the hair <br /> * Breakage of hairs <br /> * Conversion of thick terminal hairs to thin vellus hairs <br /> [[Image:Facts.jpg|thumb|right|400px|Survey results from Japan]]<br /> Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed '''“Male Pattern Baldness&quot;''' or '''&quot;Androgenetic Alopecia&quot;'''.<br /> <br /> === Androgenetic Alopecia ===<br /> * Gradual Onset.<br /> * Transition from large, thick, pigmented terminal hairs to thinner, shorter, indeterminate hairs and finally to short, wispy, nonpigmented vellus hairs in the involved areas.<br /> * Characterised by a receding hairline and/or hair loss on the top of the head.<br /> <br /> '''Main Causes'''<br /> * Genetic predisposition<br /> * Hormonal effect of androgen <br /> * Reduction of blood circulation around hair follicle<br /> * Deactivation of hair matrix cells<br /> <br /> '''Some facts from Japan''' <br /> <br /> * Market size: ¥ 30 Billion<br /> * Number of products: more than 100<br /> <br /> (JICST-EPlus - Japanese Science &amp; Technology)<br /> <br /> == Goals ==<br /> <br /> The goal of this report is to:<br /> * Summarize IP activity over the years<br /> * Identify major players<br /> * Conduct patent analysis<br /> a) Composition<br /> b) Nature<br /> c) Action<br /> <br /> '''And then'''<br /> <br /> * Analyze patents pertaining to high sebum activity<br /> <br /> == Approach ==<br /> <br /> * A broad search was conducted on hair loss patents.<br /> * Patent information was sourced through SIP.<br /> * A set of patents was selected for analysis.<br /> <br /> Composition of treatment for causes are identified and categorized as follows:<br /> <br /> * Anti-androgen<br /> * Minoxidil<br /> * Double action (Anti-androgen + Mindoxidil)<br /> * Hair matrix cells activator<br /> * Sebum production inhibitor<br /> <br /> == IP activity over years ==<br /> The graph indicates:<br /> * Number of patents filed every 5 years (except for first 7 years).<br /> * First solution proposed in 1973<br /> * Filing trend indicates steep rise in activity recently.<br /> [[Image:Year1.jpg|thumb|center|400px|IP Activity over years]]<br /> <br /> == Major Players ==<br /> [[Image:players.jpg|thumb|left|400px|Assignees with more than 20 patents ]]<br /> [[Image:players1.jpg|thumb|center|400px|Assignees with fewer than 20 patents ]]<br /> <br /> * '''Active Assignees'''<br /> Assignees currently active with more than 5 patents to their credit during 2000-2005. <br /> * Warner with 9 patents,<br /> * Bristol with 6 and<br /> * Abbott with 5.<br /> <br /> [[Image:Active.jpg|thumb|center|500px|Active Assignees]]<br /> <br /> == Anti-androgens == <br /> * Anti-androgens are used in hormone therapy.<br /> * Anti-androgens are designed to affect the hormones made in the adrenal glands. They don't stop the hormones from being made, but they stop them from having an effect leading to hair loss.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Testosterone is reduced to its active metabolite, Dihydrotestosterone (DHT) by the enzyme 5 alpha reductase.<br /> * DHT attaches to androgen receptor sites at the hair follicle. <br /> * DHT causes gradual miniaturization of the follicle, which eventually results in hair loss.<br /> <br /> '''How do anti-androgens treat hair loss?'''<br /> * Anti-androgens compete with DHT to bind to the androgen receptor.<br /> * Upon binding of anti-androgen in place of DHT, follicle miniaturization is lowered and hair loss prevented.<br /> <br /> === Functions of Anti-androgen === <br /> [http://www.revivogen.com/revivogen/work.html Anti-androgen]<br /> <br /> [[Image:Andogen1.jpg|thumb|center|500px|Functions of Anti-androgen]]<br /> <br /> === IP Map for Anti-androgen ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;8&quot;, style=&quot;#008080&quot;<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> BLOTECH (2004)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Palmetto berry extract (fatty acids &amp; sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans)<br /> |bgcolor=LightCyan|Fatty acids – Inhibit testosterone<br /> Sterols - Mechanism of action unknown.<br /> <br /> Quercetin results in cell growth cycle.<br /> <br /> Beta-sitosterol reduce inflammation on scalp<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 4-cycloalkoxy benzonitrile derivatives and salts<br /> |bgcolor=LightCyan|Acts as androgen receptor modulators and blocks formation of DHT.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives.<br /> |bgcolor=LightCyan|The compounds inhibit, or decrease, activation of androgen receptor by androgens.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> APHIOS Corp (2003)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives.<br /> |bgcolor=LightCyan|Modulates androgenic activity by inhibiting 5.alpha.-reductase activity.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> Fundacion Pablo Cassara (2003)<br /> |bgcolor=LightCyan|Nucleotide<br /> |bgcolor=LightCyan|Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond)<br /> |bgcolor=LightCyan|Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> PFIZER INC (2001)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate <br /> |bgcolor=LightCyan|Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> N/A (1995)<br /> |bgcolor=LightCyan|Peptides/nucleic acid<br /> |bgcolor=LightCyan|Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein)<br /> |bgcolor=LightCyan|Inhibit synthesis of bradykinin receptors or compounds by binding to B2 receptor<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> KAO Corp (1987)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Walnut extract (leaves/pericarps) with an organic solvent<br /> |bgcolor=LightCyan|Blocks formation of DHT<br /> |}<br /> <br /> == Minoxidil ==<br /> * Minoxidil is a &quot;potassium channel opener&quot; that leads to vasodilation.<br /> * The drug is available in two forms. Oral minoxidil is used to treat high blood pressure and the topical solution form is used to treat hair loss and baldness.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * A thick network of tiny veins and arteries lines the outer wall of the follicle. Blood pumps through the bulb and hair via this network.<br /> * DHT accumulates in the hair follicles and roots, constricting the blood supply of oxygen and nutrients to the hair roots; which is also seen to possibly contribute towards hair loss.<br /> <br /> '''How does Minoxidal treat hair loss?'''<br /> * Minoxidal is applied to the scalp topically, where it dilates blood vessels in the scalp and sustains the hair follicles for longer period of time.<br /> * Scientists and researchers are not exactly sure of how Minoxidil leads to this effect.<br /> * Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.<br /> <br /> === Functions of Monoxidil === [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 Minoxidil]<br /> <br /> [[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil]]<br /> <br /> === IP Map for Minoxidil ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> WARNER LAMBERT(2002)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Benzopyran compounds<br /> |bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> LG HOUSEHOLD &amp; HEALTH CARE(2001)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Sophora flavescens extract (alkaloids &amp; flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)<br /> |bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels<br /> |}<br /> <br /> == Double action (Anti-androgen + Minoxidil) ==<br /> * Combination of Minoxidil + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.<br /> <br /> <br /> '''What is the problem with using only Anti-androgen therapy?'''<br /> * Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.<br /> * Anti-androgen only prevent binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.<br /> <br /> '''What is the problem with using only Minoxidal therapy?'''<br /> * Minoxidil-based products are generally not effective in stopping hair loss as minoxidil does not block the harmful effects of DHT in the scalp and hair follicles. <br /> * Minoxidil simply dilates blood vessels in the scalp. However, the harmful DHT is still being produced in the body and still getting into the scalp and hair follicles and causing eventual hair loss.<br /> <br /> '''How is the combination of Anti-androgens and Minoxidil effective?'''<br /> * Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.<br /> * Minoxidil causes vasodilation and therefore improves supply of oxygen and nutrients to the hair follicle and roots.<br /> * Combination therapy therefore proves to be much more effective than individual therapy.<br /> <br /> === Functions of (Anti-androgen + Minoxidil) === [http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]<br /> [[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Minoxidil)]]<br /> <br /> === IP Map for (Anti-androgen + Minoxidil) ===<br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405] <br /> N/A(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhance and sunscreen<br /> |bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577] <br /> L'OREAL(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP<br /> |bgcolor=LightCyan|Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762] <br /> COLOMER GROUP(1999)<br /> |bgcolor=LightCyan|Natural extract<br /> |bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)<br /> |bgcolor=LightCyan|Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp<br /> |}<br /> <br /> <br /> == Hair matrix cell activator ==<br /> Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.<br /> * Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.<br /> * Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.<br /> * Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.<br /> <br /> <br /> '''How does hair cell matrix activator treat hair loss?'''<br /> * Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.<br /> * This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.<br /> * Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.<br /> <br /> === Functions of Hair matrix cell activator === [http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]<br /> [[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]<br /> <br /> === IP Map for Hair matrix cell activator ===<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> SHISEIDO(1999) <br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt<br /> |bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> L'OREAL(1998) <br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions<br /> |bgcolor=LightCyan|Reducing the expression of MMPs (Metalloproteases) in the scalp - slow down or inhibit the degradation of the perifollicular matrix (extracellular matrix surround the hair follicle) <br /> |}<br /> <br /> == Sebum Production Inhibitor ==<br /> Sebum Production Inhibitor is a substance that prevents the synthesis of sebum, mixture of lipid substances.<br /> <br /> '''What causes hair loss?'''<br /> * Sebum is a fatty acid substance secreted from sebaceous glands associated with hair follicles.<br /> * Hair can get heavy sebum build-up and mixes with cholesterol to form a hardened plug around the bottom part of the hair bulb.<br /> * Hardened plugs prevent cell respirations and eventually lead to hair loss.<br /> * Bacteria will also attach to the hardened plug and this can also cause further cause problems with hair growth.<br /> <br /> '''How does Sebum production inhibitor treat hair loss?'''<br /> * The inhibitor prevents synthesis of sebum and slows down accumulation and mixing of sebum with cholesterol leading to hardened plugs. <br /> * Reduction of sebum results in unclogged hair follicles/bulbs and allows oxygen and nutrients from reaching the hair follicle.<br /> * Reduction in sebum also prevents vasoconstriction.<br /> * Sum result of these effects of Sebum production inhibitor is prevention of hair loss.<br /> <br /> <br /> * The inhibitor blocks the excessive sebum production produces greasy effect on hair and scalp and also responsible for thinning and loosing of hair.<br /> <br /> === Functions of Sebum Production Inhibitor ===<br /> [[http://en.wikipedia.org/wiki/Image:HairFollicle.jpg Sebum Production Inhibitor]]<br /> [[Image:Sebum1.jpg|thumb|center|500px|Functions of Sebum Production Inhibitor]]<br /> <br /> === IPMap for Sebum Production Inhibitor ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699] <br /> Unilever(2005)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Polyamine (putrescine, spermine or spermidine) analogs and/or derivatives; DFMO; N-acetyl cysteines; neutralized salts of a non-hydroxy C2-C40 dicarboxylic acids, preferably malonate salts; and mixtures thereof. <br /> |bgcolor=LightCyan|Decreasing sebum production and/or pore size <br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362] <br /> KAO COPR.(2004)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Avocado oil (Butyl esters of fatty acids) <br /> |bgcolor=LightCyan|Reduce sebum of the hair and scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587] <br /> Unilever(1982)<br /> |bgcolor=LightCyan|organic compound<br /> |bgcolor=LightCyan |Biotin antagonist or a salt thereof <br /> |bgcolor=LightCyan|Decrease activity of the enzyme acetyl-SCoA-carboxylase and hence reduce lipid synthesis in sebaceous glands so that less sebum is produced <br /> |}<br /> <br /> == Composition nature matrix ==<br /> <br /> === IPMap: Composition nature matrix ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;11&quot;, style=&quot;#008080&quot;<br /> !width=&quot;50&quot; bgcolor=DodgerBlue|'''Year'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Organic Compound'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extracts''' <br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Peptides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nucleotides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extract + Organic comp'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|2005 <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |- <br /> |bgcolor=LightCyan|2004 <br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|BLOTECH (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |- <br /> |bgcolor=LightCyan|2003<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|APHIOS (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|FUNDIACION (1)<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2002<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2001<br /> |bgcolor=LightCyan |PFIZER (1)<br /> |bgcolor=LightCyan|LG HEALTH-CARE (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2000<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1) / N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1999<br /> |bgcolor=LightCyan|SHISEDIO (1)<br /> |bgcolor=LightCyan|COLOMER (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1998<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1995<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |-<br /> |bgcolor=LightCyan|1987<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1982<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |}<br /> <br /> == Focus of patents ==<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;17&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Focus of patents'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Stimulating hair growth using benzopyrans<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Compositions to prevent or reduce hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Method of decreasing sebum production and pore size<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699 ]<br /> |bgcolor=LightCyan|16<br /> |- <br /> |bgcolor=LightCyan|Method for reducing sebum on the hair and skin<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |bgcolor=LightCyan|17<br /> |}<br /> <br /> === Focus of patents by technology ===<br /> [[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]<br /> <br /> == Distribution of patents ==<br /> <br /> === By patent types ===<br /> [[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]<br /> <br /> <br /> === By key ingredients ===<br /> [[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]<br /> <br /> === By target disease ===<br /> [[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]<br /> <br /> <br /> === Key ingredients vs. Target disease ===<br /> [[Image:key&amp;target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]<br /> <br /> <br /> === Target species ===<br /> [[Image:Species.jpg|thumb|center|700px|Target species]]<br /> <br /> <br /> === Mode of administration ===<br /> [[Image:Mode.jpg|thumb|center|700px|Mode of administration]]<br /> <br /> <br /> === Product type vs. Product form ===<br /> [[Image:prod.jpg|thumb|center|700px|Product type vs. Product form]]<br /> <br /> == Distribution based on different aspects ==<br /> <br /> === List of patents ===<br /> {| border=&quot;1&quot; cellpadding=&quot;9&quot;, style=&quot;#008080&quot;<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|1<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|10<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |- <br /> |bgcolor=LightCyan|2<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|11<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |- <br /> |bgcolor=LightCyan|3<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> |bgcolor=LightCyan|12<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |- <br /> |bgcolor=LightCyan|4<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427] <br /> |bgcolor=LightCyan|13<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |- <br /> |bgcolor=LightCyan|5<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282] <br /> |bgcolor=LightCyan|14<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |- <br /> |bgcolor=LightCyan|6<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467] <br /> |bgcolor=LightCyan|15<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |- <br /> |bgcolor=LightCyan|7<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|16<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699]<br /> |- <br /> |bgcolor=LightCyan|8<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|17<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |- <br /> |bgcolor=LightCyan|9<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010] <br /> |bgcolor=LightCyan|18<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |}<br /> <br /> === Patents by target diseases ===<br /> {| border=&quot;1&quot; cellpadding=&quot;16&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Target disease/ disorder'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness)<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, male pattern baldness and female pattern baldness<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|Inappropriate activation of the androgen receptor, acne, oily skin, alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Androgen-associated hair loss and androgen-skin related disorders. <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Androgenetic or androgenic alopecia or androgeno-genetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Diseases caused by testosterone (male-pattern alopecia)<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Alopecia, androgenic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Androgenetic, androgenic or androgenogenetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Curing other scalp related problems<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |bgcolor=LightCyan|16<br /> |}<br /> <br /> === Patents by application ===<br /> [[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]<br /> <br /> === Signaling Pathway and linkages ===<br /> [[Image:Slide1.GIF|thumb|center|700px|Alopecia pathways]]<br /> <br /> == Players of Wnt inhibition Pathway == [[Image:wnt.jpg|thumb|right|600px|Wnt inhibition]]<br /> {| border=&quot;1&quot; cellpadding=&quot;15&quot;, style=&quot;#008080&quot;<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Key compound'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Players of inhibition'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6989385.PN.&amp;OS=PN/6989385&amp;RS=PN/6989385 US6989385]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|CDK,GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6974819.PN.&amp;OS=PN/6974819&amp;RS=PN/6974819 US6974819]<br /> |bgcolor=LightCyan|Pyrimidine derivative<br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6743791.PN.&amp;OS=PN/6743791&amp;RS=PN/6743791 US6743791]<br /> |bgcolor=LightCyan|Heterocyclic compounds<br /> |bgcolor=LightCyan|AKT3, GSK-3, ERK2<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277773%22.PGNR.&amp;OS=DN/20050277773&amp;RS=DN/20050277773 US20050277773]<br /> |bgcolor=LightCyan|Pyrrolo[3,2-d]pyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040072836%22.PGNR.&amp;OS=DN/20040072836&amp;RS=DN/20040072836 US20040072836]<br /> |bgcolor=LightCyan|Aza-oxindole derivatives <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1477489&amp;F=0 EP1477489]<br /> |bgcolor=LightCyan|Pyrrolopyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO0056710&amp;F=0 WO0056710]<br /> |bgcolor=LightCyan|3-(Anilinomethylene) oxindoles <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO03011287&amp;F=0 WO2003011287]<br /> |bgcolor=LightCyan|Pyrazolon derivatives <br /> |bgcolor=LightCyan|GSK3, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6924141.PN.&amp;OS=PN/6924141&amp;RS=PN/6924141 US6924141]<br /> |bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7 <br /> |bgcolor=LightCyan|β-catenin, GSK3, Wnt<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6706685.PN.&amp;OS=PN/6706685&amp;RS=PN/6706685 US6706685]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6683048.PN.&amp;OS=PN/6683048&amp;RS=PN/6683048 US6683048]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|α-catenin, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6677116.PN.&amp;OS=PN/6677116&amp;RS=PN/6677116 US6677116]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6303576.PN.&amp;OS=PN/6303576&amp;RS=PN/6303576 US6303576]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |}<br /> [[Image:coloury.jpg]]- '''Target sites and Details'''<br /> <br /> == Pyrazole compounds ==<br /> <br /> * '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.<br /> * Pyrazoles are produced synthetically through the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation <br /> [[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]<br /> * Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.<br /> * Structurally related compounds are pyrazoline and pyrazolidine.<br /> [[Image:pyrazole2.jpg|thumb|center|500px|Structurally related compounds]]<br /> <br /> === GSK3 inhibition by pyrazole compounds ===<br /> [[Image:bold3.jpg]]<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?TERM1=6989385+&amp;Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=0&amp;f=S&amp;l=50 US6989385]<br /> [[Image:US6989385.jpg]]<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247] <br /> [[Image:US6664247.jpg]]<br /> !width=&quot;100&quot;|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256] <br /> [[Image:WO2005012256.jpg]]<br /> |- <br /> |bgcolor=lightcyan|R1=T-Ring D, wherein <br /> T is a valence bond and <br /> Ring D = 5-6 membered aryl or heteroaryl ring; <br /> <br /> R2 = hydrogen or C1-4 aliphatic and <br /> R2'= hydrogen; <br /> <br /> R3 = -R, -OR, or -N(R4)2, wherein <br /> R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and <br /> L is -O-, -S-, or -NH-; and <br /> Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R&lt;4&gt;), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring<br /> <br /> |bgcolor=lightcyan|X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; <br /> <br /> R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; <br /> <br /> R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and <br /> <br /> R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).<br /> <br /> |bgcolor=lightcyan|X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;<br /> A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy).<br /> |}<br /> <br /> === GSK3 inhibition by pryazole pyrimidine amine derivatives ===<br /> <br /> '''Patent Number''': US6989385<br /> '''Applicant''': ''Vertex Pharmaceuticals Incorporated''<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol1.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-p- yrimidin-4-yl]-amine <br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyl- sulfanyl]-pyrimidin-4-yl}-amine <br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-me- thyl-2H-pyrazol-3-yl)-amine <br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * {2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-y- l}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(- 5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfa- nyl)-pyrimidin-4-yl]-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mo- rpholin-4-yl-pyrimidin-4-yl}-amine <br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimi- din-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyri- midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * 5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-ylmethylsulf- anyl)-pyrimidin-4-yl]-amine <br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)-phenyl]-py- rimidin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methy- l-2H-pyrazol-3-yl)-amine <br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methylphenylamino)-6-phenyl-pyrimidi- n-4-yl]-amine <br /> * [2-(4-cyanomethylphenylamino)-6-phenyl-pyrimidin-4-yl]-(5-cyclopropyl-2H-p- yrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(pyridin-3-ylmethylamino)-pyri- midin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-methyl-2H-py- razol-3-yl)-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3,4,5-trimethoxyphenyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(4-sulfamoylphenylamino)-6-(3,4,5-trimethoxy- phenyl)-pyrimidin-4-yl]-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyraz- ol-3-yl]-amine <br /> * [2-(Benzimidazol-2-ylamino-)6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * (5-tert-Butyl-2H-pyrazol-3-yl)-[2-(3-chlorophenyl)amino-6-(3-nitrophenyl)-- pyrimidin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-phenyl-2H-py- razol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-a- mine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-[5-(Furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * [2-(4-Chlorophenylamino)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * (5,6-Dimethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Chlorophenyl)amino-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * (6-Methoxymethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-- amine <br /> * (6-Methyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyr- azol-3-yl]-amine <br /> * (6-methyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-phenyl-2H-pyrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenoxymethyl-pyrimidin-4-yl)- -amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-amine <br /> * [6-Methyl-2-(4-methyl-phenylsulfanylmethyl)-pyrimidin-4-yl]-(5-phenyl-2H-p- yrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-[6-Methyl-2-(4-methyl-phenylsulfanylmethy- l)-pyrimidin-4-yl]-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * (6-Ethyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)- -amine <br /> * (6-Ethyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Ethyl-2-(4-fluorophenoxymethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [6-Ethyl-2-(1-methyl-1-phenyl-ethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-p- yrazol-3-yl]-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(2-phenylsulfanylmethyl-5,6,7,8-tetrahydro-quin- azolin-4-yl)-amine <br /> * [2-(4-Methylphenylsulfanylmethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidi- n-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(1-Methyl-1-phenyl-ethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-y- l]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6,7,8-tetrahydro-quinazolin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * [7-Benzyl-2-(2,6-dichlorobenzyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-- 4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Benzyl-2-(4-chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimi- din-4-yl]-(5-methyl-2H-pyrazol-3-yl)-<br /> * [2-(4-Chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> ----<br /> '''Patent Number''': US7008948 <br /> '''Applicant''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure'''<br /> <br /> [[Image:pyrazol2.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(1H-i- ndazol-3-yl)-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[3,4-d]pyrimidin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(7-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5,7-- difluoro-1H-indazol-3-yl)-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetra- hydroquinazolin-4-yl]-amine <br /> * (5-Trifluoromethyl-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-- tetrahydroquinazolin-4-yl]-amine <br /> * (5,7-difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetra- hydro-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (6-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyr- imidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydro-5H-cycl- oheptapyrimidin-4-yl]-amine<br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[4,3-d]pyrimidin-4-yl]-amine<br /> * (1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydroquinazol- in-4-yl]-amine <br /> * (7-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine<br /> * (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> * 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> ----<br /> '''Patent Number''': US6977262<br /> '''Assignee''': Mitsubishi Pharma Corporation<br /> '''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol3.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate<br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-methyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Methyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * t-Butyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Isopropyl 4-(2-fluorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Benzyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * 4-(2-Chlorophenyl)-5-dimethylaminocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4-(2-Chlorophenyl)-5-hydrazinocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo[3,4 -b]pyridine <br /> * 4-(2-Fluorophenyl)-4,7-dihydro-6-methyl-5-isopropylthiocarbonyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4,7-Dihydro-6-methyl-5-nitro-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b] pyridine <br /> * Ethyl 4,7-dihydro-4-phenyl-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridine-5-carbox ylate <br /> * Ethyl 4-(2-fluorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate maleate <br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridi ne-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate <br /> * Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate<br /> ----<br /> '''Patent Number''': US6664247<br /> '''Assignee''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors'''<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol4.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine<br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine<br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine<br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine<br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine<br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine<br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine<br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine<br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.<br /> ----<br /> '''Patent Number''': US2004224944<br /> '''Assignee''': VERTEX PHARMACEUTICALS INC<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol5.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine <br /> * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine<br /> <br /> === Other derivates used by different assigness for the treatment of alopecia ===<br /> [[Image:other derivates.jpeg]]<br /> <br /> == Inhibition of 5- - reductase by Finasteride ==<br /> [[Image:5-alpha-reductase inhibition.jpeg]]<br /> <br /> === Structure-Activity Relationships (SARs) of Finasteride ===<br /> [[Image:SAR_map.gif]]<br /> <br /> == Questions Dolcera Answers ==<br /> <br /> '''What’s hot?'''<br /> * What compositions/ approaches are the most promising?<br /> * What can I license?<br /> * Can you map blockbuster products to their patents?<br /> <br /> '''Can you save me some time?'''<br /> * What combinations/ compounds have already been tried?<br /> * Is any empirical data available?<br /> * Can you tell me the side effects?<br /> <br /> '''Where should I focus my R&amp;D investment?'''<br /> * What are the most promising approaches?<br /> * Where’s the ‘white space’ for me to play in?<br /> <br /> '''Any hints for research?'''<br /> * Are there any combinations I could develop?<br /> <br /> '''What should I do in this geography?'''<br /> * What are my competitors up to in this geography?<br /> * What are my strengths/ weaknesses here?<br /> <br /> '''What’s my competition up to?'''<br /> <br /> * What’s my top competitor investing in?<br /> * Are there any loopholes in their patents?<br /> * When are their patents expiring?<br /> * Will a competitor emerge from nowhere and surprise me?<br /> * What are the crowded areas?<br /> <br /> '''How do I play defense?'''<br /> * What should my blocking/reactive strategies be?<br /> <br /> <br /> == New Combinations based on IP study? ==<br /> <br /> Yes, new Combinations can be made with '''natural products''' based on IP study<br /> * Walnut extract containing [[Image:5ar.jpg]] inhibitor (as anti-androgen) and Flavnones (for vasodilation).<br /> * Sophora Flavnones (for vasodilation) in combination with Saw Palmetto berry (as anti-androgen).<br /> <br /> '''Note:''' The above combinations are based on limited study and are only possible examples<br /> <br /> == IP studies provides ==<br /> <br /> === Technology trends ===<br /> * Use of saw palmetto berry for treating alopecia was first patented in 1996.<br /> * Since then, 144 patents (including family patents) have been filed till 2006.<br /> * Most patents use saw palmetto berry in combination with other products.<br /> [[Image:Technology1.jpg|thumb|center|700px|Technology trends]]<br /> <br /> === New opportunities ===<br /> Yes, the IP studies provide new opportunities in the following area.<br /> * Sophora Flavescens contain flavnoids.<br /> * Natural extract Sophora Flavescens cited in LG patent of 2001.<br /> * Research shows fewer than 7 patents based on Sophora Flavescens for hair loss or alopecia.<br /> <br /> * What's this?<br /> <br /> == Conclusions ==<br /> * Hair loss medication is a very active area of research and intellectual property development.<br /> * One of the most promising areas of development is the area of Anti-androgens.<br /> * The top companies are Merck, L’Oreal and Smithkline.<br /> <br /> == Useful links ==<br /> * [http://www.biocarta.com/pathfiles/h_ghPathway.asp Pathways example]<br /> * [http://www.cellsignal.com/category.asp?catalog_name=CellSignal&amp;category_name=MAPK+Signaling Signaling Pathways]<br /> <br /> == Summary ==</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Template:TOCleft&diff=1772 2006-05-21T01:45:31Z

<p>67.180.226.207: </p> <hr /> <div>{| cellspacing=0 cellpadding=0 style=&quot;margin-bottom: .5em; float: left; margin-right: .5em; padding: .5em 1.4em .8em 0;&quot;<br /> |<br /> __TOC__<br /> |}</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss&diff=1771 2006-05-21T01:45:20Z

<p>67.180.226.207: </p> <hr /> <div>{{TOCleft}}<br /> == Rationale ==<br /> * &quot;Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year.&quot; March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55]<br /> <br /> * &quot;An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries.&quot; February 16, 2006 – [http://stophair.setupmyblog.com/]<br /> <br /> * &quot;There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting.&quot; June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&amp;STORY=/www/story/06-07-2005/0003821470&amp;EDATE=]<br /> <br /> == Alopecia IPMap == <br /> [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Dolcera IPMap for Alopecia]<br /> <br /> == Introduction ==<br /> <br /> === Hair Basics ===<br /> * Hair is a complex and delicate part of the body.<br /> * Keeping it healthy and beautiful is a challenge.<br /> * Hair grows everywhere on the body with the exception of the lips, eyelids, the palms of the hands and soles of the feet.<br /> * Hair is basically a form of skin. <br /> * Hair is made up of a protein called keratin.<br /> * Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin. <br /> * Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htm]<br /> * Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.html]<br /> [[Image:Hairbasics.jpg|thumb|center|500px|Structure of Hair root and Hair bulb]]<br /> <br /> === What causes Hair loss? === <br /> * Decreased growth of the hair <br /> * Increased shedding of the hair <br /> * Breakage of hairs <br /> * Conversion of thick terminal hairs to thin vellus hairs <br /> [[Image:Facts.jpg|thumb|right|400px|Survey results from Japan]]<br /> Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed '''“Male Pattern Baldness&quot;''' or '''&quot;Androgenetic Alopecia&quot;'''.<br /> <br /> === Androgenetic Alopecia ===<br /> * Gradual Onset.<br /> * Transition from large, thick, pigmented terminal hairs to thinner, shorter, indeterminate hairs and finally to short, wispy, nonpigmented vellus hairs in the involved areas.<br /> * Characterised by a receding hairline and/or hair loss on the top of the head.<br /> <br /> '''Main Causes'''<br /> * Genetic predisposition<br /> * Hormonal effect of androgen <br /> * Reduction of blood circulation around hair follicle<br /> * Deactivation of hair matrix cells<br /> <br /> '''Some facts from Japan''' <br /> <br /> * Market size: ¥ 30 Billion<br /> * Number of products: more than 100<br /> <br /> (JICST-EPlus - Japanese Science &amp; Technology)<br /> <br /> == Goals ==<br /> <br /> The goal of this report is to:<br /> * Summarize IP activity over the years<br /> * Identify major players<br /> * Conduct patent analysis<br /> a) Composition<br /> b) Nature<br /> c) Action<br /> <br /> '''And then'''<br /> <br /> * Analyze patents pertaining to high sebum activity<br /> <br /> == Approach ==<br /> <br /> * A broad search was conducted on hair loss patents.<br /> * Patent information was sourced through SIP.<br /> * A set of patents was selected for analysis.<br /> <br /> Composition of treatment for causes are identified and categorized as follows:<br /> <br /> * Anti-androgen<br /> * Minoxidil<br /> * Double action (Anti-androgen + Mindoxidil)<br /> * Hair matrix cells activator<br /> * Sebum production inhibitor<br /> <br /> == IP activity over years ==<br /> The graph indicates:<br /> * Number of patents filed every 5 years (except for first 7 years).<br /> * First solution proposed in 1973<br /> * Filing trend indicates steep rise in activity recently.<br /> [[Image:Year1.jpg|thumb|center|400px|IP Activity over years]]<br /> <br /> == Major Players ==<br /> [[Image:players.jpg|thumb|left|400px|Assignees with more than 20 patents ]]<br /> [[Image:players1.jpg|thumb|center|400px|Assignees with fewer than 20 patents ]]<br /> <br /> * '''Active Assignees'''<br /> Assignees currently active with more than 5 patents to their credit during 2000-2005. <br /> * Warner with 9 patents,<br /> * Bristol with 6 and<br /> * Abbott with 5.<br /> <br /> [[Image:Active.jpg|thumb|center|500px|Active Assignees]]<br /> <br /> == Anti-androgens == <br /> * Anti-androgens are used in hormone therapy.<br /> * Anti-androgens are designed to affect the hormones made in the adrenal glands. They don't stop the hormones from being made, but they stop them from having an effect leading to hair loss.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Testosterone is reduced to its active metabolite, Dihydrotestosterone (DHT) by the enzyme 5 alpha reductase.<br /> * DHT attaches to androgen receptor sites at the hair follicle. <br /> * DHT causes gradual miniaturization of the follicle, which eventually results in hair loss.<br /> <br /> '''How do anti-androgens treat hair loss?'''<br /> * Anti-androgens compete with DHT to bind to the androgen receptor.<br /> * Upon binding of anti-androgen in place of DHT, follicle miniaturization is lowered and hair loss prevented.<br /> <br /> === Functions of Anti-androgen === [http://www.revivogen.com/revivogen/work.html Anti-androgen]<br /> <br /> [[Image:Andogen1.jpg|thumb|center|500px|Functions of Anti-androgen]]<br /> <br /> === IP Map for Anti-androgen ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;8&quot;, style=&quot;#008080&quot;<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> BLOTECH (2004)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Palmetto berry extract (fatty acids &amp; sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans)<br /> |bgcolor=LightCyan|Fatty acids – Inhibit testosterone<br /> Sterols - Mechanism of action unknown.<br /> <br /> Quercetin results in cell growth cycle.<br /> <br /> Beta-sitosterol reduce inflammation on scalp<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 4-cycloalkoxy benzonitrile derivatives and salts<br /> |bgcolor=LightCyan|Acts as androgen receptor modulators and blocks formation of DHT.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives.<br /> |bgcolor=LightCyan|The compounds inhibit, or decrease, activation of androgen receptor by androgens.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> APHIOS Corp (2003)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives.<br /> |bgcolor=LightCyan|Modulates androgenic activity by inhibiting 5.alpha.-reductase activity.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> Fundacion Pablo Cassara (2003)<br /> |bgcolor=LightCyan|Nucleotide<br /> |bgcolor=LightCyan|Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond)<br /> |bgcolor=LightCyan|Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> PFIZER INC (2001)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate <br /> |bgcolor=LightCyan|Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> N/A (1995)<br /> |bgcolor=LightCyan|Peptides/nucleic acid<br /> |bgcolor=LightCyan|Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein)<br /> |bgcolor=LightCyan|Inhibit synthesis of bradykinin receptors or compounds by binding to B2 receptor<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> KAO Corp (1987)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Walnut extract (leaves/pericarps) with an organic solvent<br /> |bgcolor=LightCyan|Blocks formation of DHT<br /> |}<br /> <br /> == Minoxidil ==<br /> * Minoxidil is a &quot;potassium channel opener&quot; that leads to vasodilation.<br /> * The drug is available in two forms. Oral minoxidil is used to treat high blood pressure and the topical solution form is used to treat hair loss and baldness.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * A thick network of tiny veins and arteries lines the outer wall of the follicle. Blood pumps through the bulb and hair via this network.<br /> * DHT accumulates in the hair follicles and roots, constricting the blood supply of oxygen and nutrients to the hair roots; which is also seen to possibly contribute towards hair loss.<br /> <br /> '''How does Minoxidal treat hair loss?'''<br /> * Minoxidal is applied to the scalp topically, where it dilates blood vessels in the scalp and sustains the hair follicles for longer period of time.<br /> * Scientists and researchers are not exactly sure of how Minoxidil leads to this effect.<br /> * Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.<br /> <br /> === Functions of Monoxidil === [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 Minoxidil]<br /> <br /> [[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil]]<br /> <br /> === IP Map for Minoxidil ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> WARNER LAMBERT(2002)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Benzopyran compounds<br /> |bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> LG HOUSEHOLD &amp; HEALTH CARE(2001)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Sophora flavescens extract (alkaloids &amp; flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)<br /> |bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels<br /> |}<br /> <br /> == Double action (Anti-androgen + Minoxidil) ==<br /> * Combination of Minoxidil + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.<br /> <br /> <br /> '''What is the problem with using only Anti-androgen therapy?'''<br /> * Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.<br /> * Anti-androgen only prevent binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.<br /> <br /> '''What is the problem with using only Minoxidal therapy?'''<br /> * Minoxidil-based products are generally not effective in stopping hair loss as minoxidil does not block the harmful effects of DHT in the scalp and hair follicles. <br /> * Minoxidil simply dilates blood vessels in the scalp. However, the harmful DHT is still being produced in the body and still getting into the scalp and hair follicles and causing eventual hair loss.<br /> <br /> '''How is the combination of Anti-androgens and Minoxidil effective?'''<br /> * Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.<br /> * Minoxidil causes vasodilation and therefore improves supply of oxygen and nutrients to the hair follicle and roots.<br /> * Combination therapy therefore proves to be much more effective than individual therapy.<br /> <br /> === Functions of (Anti-androgen + Minoxidil) === [http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]<br /> [[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Minoxidil)]]<br /> <br /> === IP Map for (Anti-androgen + Minoxidil) ===<br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405] <br /> N/A(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhance and sunscreen<br /> |bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577] <br /> L'OREAL(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP<br /> |bgcolor=LightCyan|Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762] <br /> COLOMER GROUP(1999)<br /> |bgcolor=LightCyan|Natural extract<br /> |bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)<br /> |bgcolor=LightCyan|Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp<br /> |}<br /> <br /> <br /> == Hair matrix cell activator ==<br /> Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.<br /> * Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.<br /> * Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.<br /> * Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.<br /> <br /> <br /> '''How does hair cell matrix activator treat hair loss?'''<br /> * Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.<br /> * This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.<br /> * Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.<br /> <br /> === Functions of Hair matrix cell activator === [http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]<br /> [[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]<br /> <br /> === IP Map for Hair matrix cell activator ===<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> SHISEIDO(1999) <br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt<br /> |bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> L'OREAL(1998) <br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions<br /> |bgcolor=LightCyan|Reducing the expression of MMPs (Metalloproteases) in the scalp - slow down or inhibit the degradation of the perifollicular matrix (extracellular matrix surround the hair follicle) <br /> |}<br /> <br /> == Sebum Production Inhibitor ==<br /> Sebum Production Inhibitor is a substance that prevents the synthesis of sebum, mixture of lipid substances.<br /> <br /> '''What causes hair loss?'''<br /> * Sebum is a fatty acid substance secreted from sebaceous glands associated with hair follicles.<br /> * Hair can get heavy sebum build-up and mixes with cholesterol to form a hardened plug around the bottom part of the hair bulb.<br /> * Hardened plugs prevent cell respirations and eventually lead to hair loss.<br /> * Bacteria will also attach to the hardened plug and this can also cause further cause problems with hair growth.<br /> <br /> '''How does Sebum production inhibitor treat hair loss?'''<br /> * The inhibitor prevents synthesis of sebum and slows down accumulation and mixing of sebum with cholesterol leading to hardened plugs. <br /> * Reduction of sebum results in unclogged hair follicles/bulbs and allows oxygen and nutrients from reaching the hair follicle.<br /> * Reduction in sebum also prevents vasoconstriction.<br /> * Sum result of these effects of Sebum production inhibitor is prevention of hair loss.<br /> <br /> <br /> * The inhibitor blocks the excessive sebum production produces greasy effect on hair and scalp and also responsible for thinning and loosing of hair.<br /> <br /> === Functions of Sebum Production Inhibitor ===<br /> [[http://en.wikipedia.org/wiki/Image:HairFollicle.jpg Sebum Production Inhibitor]]<br /> [[Image:Sebum1.jpg|thumb|center|500px|Functions of Sebum Production Inhibitor]]<br /> <br /> === IP map for Sebum Production Inhibitor ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699] <br /> Unilever(2005)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Polyamine (putrescine, spermine or spermidine) analogs and/or derivatives; DFMO; N-acetyl cysteines; neutralized salts of a non-hydroxy C2-C40 dicarboxylic acids, preferably malonate salts; and mixtures thereof. <br /> |bgcolor=LightCyan|Decreasing sebum production and/or pore size <br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362] <br /> KAO COPR.(2004)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Avocado oil (Butyl esters of fatty acids) <br /> |bgcolor=LightCyan|Reduce sebum of the hair and scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587] <br /> Unilever(1982)<br /> |bgcolor=LightCyan|organic compound<br /> |bgcolor=LightCyan |Biotin antagonist or a salt thereof <br /> |bgcolor=LightCyan|Decrease activity of the enzyme acetyl-SCoA-carboxylase and hence reduce lipid synthesis in sebaceous glands so that less sebum is produced <br /> |}<br /> <br /> == Composition nature matrix ==<br /> <br /> === IP map for Composition nature matrix ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;11&quot;, style=&quot;#008080&quot;<br /> !width=&quot;50&quot; bgcolor=DodgerBlue|'''Year'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Organic Compound'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extracts''' <br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Peptides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nucleotides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extract + Organic comp'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|2005 <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |- <br /> |bgcolor=LightCyan|2004 <br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|BLOTECH (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |- <br /> |bgcolor=LightCyan|2003<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|APHIOS (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|FUNDIACION (1)<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2002<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2001<br /> |bgcolor=LightCyan |PFIZER (1)<br /> |bgcolor=LightCyan|LG HEALTH-CARE (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2000<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1) / N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1999<br /> |bgcolor=LightCyan|SHISEDIO (1)<br /> |bgcolor=LightCyan|COLOMER (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1998<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1995<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |-<br /> |bgcolor=LightCyan|1987<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1982<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |}<br /> <br /> == Focus of patents ==<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;17&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Focus of patents'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Stimulating hair growth using benzopyrans<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Compositions to prevent or reduce hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Method of decreasing sebum production and pore size<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699 ]<br /> |bgcolor=LightCyan|16<br /> |- <br /> |bgcolor=LightCyan|Method for reducing sebum on the hair and skin<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |bgcolor=LightCyan|17<br /> |}<br /> <br /> === Focus of patents by technology ===<br /> [[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]<br /> <br /> == Distribution of patents ==<br /> <br /> === Distribution based on patent types ===<br /> [[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]<br /> <br /> <br /> === Distribution of patents by their key ingredients ===<br /> [[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]<br /> <br /> === Distribution based on target diseases ===<br /> [[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]<br /> <br /> <br /> === Key ingredients vs. Target disease/disorder ===<br /> [[Image:key&amp;target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]<br /> <br /> <br /> === Target species ===<br /> [[Image:Species.jpg|thumb|center|700px|Target species]]<br /> <br /> <br /> === Mode of administration ===<br /> [[Image:Mode.jpg|thumb|center|700px|Mode of administration]]<br /> <br /> <br /> === Product type vs. Product form ===<br /> [[Image:prod.jpg|thumb|center|700px|Product type vs. Product form]]<br /> <br /> == Distribution of patents based on different aspects ==<br /> <br /> === List of patents ===<br /> {| border=&quot;1&quot; cellpadding=&quot;9&quot;, style=&quot;#008080&quot;<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|1<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|10<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |- <br /> |bgcolor=LightCyan|2<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|11<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |- <br /> |bgcolor=LightCyan|3<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> |bgcolor=LightCyan|12<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |- <br /> |bgcolor=LightCyan|4<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427] <br /> |bgcolor=LightCyan|13<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |- <br /> |bgcolor=LightCyan|5<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282] <br /> |bgcolor=LightCyan|14<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |- <br /> |bgcolor=LightCyan|6<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467] <br /> |bgcolor=LightCyan|15<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |- <br /> |bgcolor=LightCyan|7<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|16<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699]<br /> |- <br /> |bgcolor=LightCyan|8<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|17<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |- <br /> |bgcolor=LightCyan|9<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010] <br /> |bgcolor=LightCyan|18<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |}<br /> <br /> === Distribution of patents based on target diseases ===<br /> {| border=&quot;1&quot; cellpadding=&quot;16&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Target disease/ disorder'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness)<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, male pattern baldness and female pattern baldness<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|Inappropriate activation of the androgen receptor, acne, oily skin, alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Androgen-associated hair loss and androgen-skin related disorders. <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Androgenetic or androgenic alopecia or androgeno-genetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Diseases caused by testosterone (male-pattern alopecia)<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Alopecia, androgenic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Androgenetic, androgenic or androgenogenetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Curing other scalp related problems<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |bgcolor=LightCyan|16<br /> |}<br /> <br /> === Distribution of patents based on application ===<br /> [[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]<br /> <br /> === Interactive Signaling Pathway and linkages ===<br /> [[Image:Slide1.GIF|thumb|center|700px|Alopecia pathways]]<br /> <br /> == Players of Wnt inhibition Pathway == [[Image:wnt.jpg|thumb|right|600px|Wnt inhibition]]<br /> {| border=&quot;1&quot; cellpadding=&quot;15&quot;, style=&quot;#008080&quot;<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Key compound'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Players of inhibition'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6989385.PN.&amp;OS=PN/6989385&amp;RS=PN/6989385 US6989385]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|CDK,GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6974819.PN.&amp;OS=PN/6974819&amp;RS=PN/6974819 US6974819]<br /> |bgcolor=LightCyan|Pyrimidine derivative<br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6743791.PN.&amp;OS=PN/6743791&amp;RS=PN/6743791 US6743791]<br /> |bgcolor=LightCyan|Heterocyclic compounds<br /> |bgcolor=LightCyan|AKT3, GSK-3, ERK2<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277773%22.PGNR.&amp;OS=DN/20050277773&amp;RS=DN/20050277773 US20050277773]<br /> |bgcolor=LightCyan|Pyrrolo[3,2-d]pyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040072836%22.PGNR.&amp;OS=DN/20040072836&amp;RS=DN/20040072836 US20040072836]<br /> |bgcolor=LightCyan|Aza-oxindole derivatives <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1477489&amp;F=0 EP1477489]<br /> |bgcolor=LightCyan|Pyrrolopyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO0056710&amp;F=0 WO0056710]<br /> |bgcolor=LightCyan|3-(Anilinomethylene) oxindoles <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO03011287&amp;F=0 WO2003011287]<br /> |bgcolor=LightCyan|Pyrazolon derivatives <br /> |bgcolor=LightCyan|GSK3, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6924141.PN.&amp;OS=PN/6924141&amp;RS=PN/6924141 US6924141]<br /> |bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7 <br /> |bgcolor=LightCyan|β-catenin, GSK3, Wnt<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6706685.PN.&amp;OS=PN/6706685&amp;RS=PN/6706685 US6706685]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6683048.PN.&amp;OS=PN/6683048&amp;RS=PN/6683048 US6683048]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|α-catenin, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6677116.PN.&amp;OS=PN/6677116&amp;RS=PN/6677116 US6677116]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6303576.PN.&amp;OS=PN/6303576&amp;RS=PN/6303576 US6303576]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |}<br /> [[Image:coloury.jpg]]- '''Target sites and Details'''<br /> <br /> == Pyrazole compounds ==<br /> <br /> * '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.<br /> * Pyrazoles are produced synthetically through the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation <br /> [[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]<br /> * Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.<br /> * Structurally related compounds are pyrazoline and pyrazolidine.<br /> [[Image:pyrazole2.jpg|thumb|center|500px|Structurally related compounds]]<br /> <br /> === GSK3 inhibition by pyrazole compounds ===<br /> [[Image:bold3.jpg]]<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?TERM1=6989385+&amp;Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=0&amp;f=S&amp;l=50 US6989385]<br /> [[Image:US6989385.jpg]]<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247] <br /> [[Image:US6664247.jpg]]<br /> !width=&quot;100&quot;|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256] <br /> [[Image:WO2005012256.jpg]]<br /> |- <br /> |bgcolor=lightcyan|R1=T-Ring D, wherein <br /> T is a valence bond and <br /> Ring D = 5-6 membered aryl or heteroaryl ring; <br /> <br /> R2 = hydrogen or C1-4 aliphatic and <br /> R2'= hydrogen; <br /> <br /> R3 = -R, -OR, or -N(R4)2, wherein <br /> R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and <br /> L is -O-, -S-, or -NH-; and <br /> Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R&lt;4&gt;), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring<br /> <br /> |bgcolor=lightcyan|X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; <br /> <br /> R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; <br /> <br /> R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and <br /> <br /> R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).<br /> <br /> |bgcolor=lightcyan|X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;<br /> A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy).<br /> |}<br /> <br /> === GSK3 inhibition by pryazole pyrimidine amine derivatives ===<br /> <br /> '''Patent Number''': US6989385<br /> '''Applicant''': ''Vertex Pharmaceuticals Incorporated''<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol1.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-p- yrimidin-4-yl]-amine <br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyl- sulfanyl]-pyrimidin-4-yl}-amine <br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-me- thyl-2H-pyrazol-3-yl)-amine <br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * {2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-y- l}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(- 5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfa- nyl)-pyrimidin-4-yl]-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mo- rpholin-4-yl-pyrimidin-4-yl}-amine <br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimi- din-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyri- midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * 5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-ylmethylsulf- anyl)-pyrimidin-4-yl]-amine <br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)-phenyl]-py- rimidin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methy- l-2H-pyrazol-3-yl)-amine <br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methylphenylamino)-6-phenyl-pyrimidi- n-4-yl]-amine <br /> * [2-(4-cyanomethylphenylamino)-6-phenyl-pyrimidin-4-yl]-(5-cyclopropyl-2H-p- yrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(pyridin-3-ylmethylamino)-pyri- midin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-methyl-2H-py- razol-3-yl)-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3,4,5-trimethoxyphenyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(4-sulfamoylphenylamino)-6-(3,4,5-trimethoxy- phenyl)-pyrimidin-4-yl]-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyraz- ol-3-yl]-amine <br /> * [2-(Benzimidazol-2-ylamino-)6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * (5-tert-Butyl-2H-pyrazol-3-yl)-[2-(3-chlorophenyl)amino-6-(3-nitrophenyl)-- pyrimidin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-phenyl-2H-py- razol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-a- mine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-[5-(Furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * [2-(4-Chlorophenylamino)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * (5,6-Dimethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Chlorophenyl)amino-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * (6-Methoxymethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-- amine <br /> * (6-Methyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyr- azol-3-yl]-amine <br /> * (6-methyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-phenyl-2H-pyrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenoxymethyl-pyrimidin-4-yl)- -amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-amine <br /> * [6-Methyl-2-(4-methyl-phenylsulfanylmethyl)-pyrimidin-4-yl]-(5-phenyl-2H-p- yrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-[6-Methyl-2-(4-methyl-phenylsulfanylmethy- l)-pyrimidin-4-yl]-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * (6-Ethyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)- -amine <br /> * (6-Ethyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Ethyl-2-(4-fluorophenoxymethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [6-Ethyl-2-(1-methyl-1-phenyl-ethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-p- yrazol-3-yl]-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(2-phenylsulfanylmethyl-5,6,7,8-tetrahydro-quin- azolin-4-yl)-amine <br /> * [2-(4-Methylphenylsulfanylmethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidi- n-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(1-Methyl-1-phenyl-ethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-y- l]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6,7,8-tetrahydro-quinazolin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * [7-Benzyl-2-(2,6-dichlorobenzyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-- 4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Benzyl-2-(4-chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimi- din-4-yl]-(5-methyl-2H-pyrazol-3-yl)-<br /> * [2-(4-Chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> ----<br /> '''Patent Number''': US7008948 <br /> '''Applicant''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure'''<br /> <br /> [[Image:pyrazol2.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(1H-i- ndazol-3-yl)-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[3,4-d]pyrimidin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(7-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5,7-- difluoro-1H-indazol-3-yl)-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetra- hydroquinazolin-4-yl]-amine <br /> * (5-Trifluoromethyl-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-- tetrahydroquinazolin-4-yl]-amine <br /> * (5,7-difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetra- hydro-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (6-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyr- imidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydro-5H-cycl- oheptapyrimidin-4-yl]-amine<br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[4,3-d]pyrimidin-4-yl]-amine<br /> * (1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydroquinazol- in-4-yl]-amine <br /> * (7-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine<br /> * (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> * 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> ----<br /> '''Patent Number''': US6977262<br /> '''Assignee''': Mitsubishi Pharma Corporation<br /> '''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol3.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate<br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-methyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Methyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * t-Butyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Isopropyl 4-(2-fluorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Benzyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * 4-(2-Chlorophenyl)-5-dimethylaminocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4-(2-Chlorophenyl)-5-hydrazinocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo[3,4 -b]pyridine <br /> * 4-(2-Fluorophenyl)-4,7-dihydro-6-methyl-5-isopropylthiocarbonyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4,7-Dihydro-6-methyl-5-nitro-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b] pyridine <br /> * Ethyl 4,7-dihydro-4-phenyl-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridine-5-carbox ylate <br /> * Ethyl 4-(2-fluorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate maleate <br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridi ne-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate <br /> * Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate<br /> ----<br /> '''Patent Number''': US6664247<br /> '''Assignee''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors'''<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol4.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine<br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine<br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine<br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine<br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine<br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine<br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine<br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine<br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.<br /> ----<br /> '''Patent Number''': US2004224944<br /> '''Assignee''': VERTEX PHARMACEUTICALS INC<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol5.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine <br /> * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine<br /> <br /> === Other derivates used by different assigness for the treatment of alopecia ===<br /> [[Image:other derivates.jpeg]]<br /> <br /> == Inhibition of 5- - reductase by Finasteride ==<br /> [[Image:5-alpha-reductase inhibition.jpeg]]<br /> <br /> === Structure-Activity Relationships (SARs) of Finasteride ===<br /> [[Image:SAR_map.gif]]<br /> <br /> == Questions Dolcera Answers ==<br /> <br /> '''What’s hot?'''<br /> * What compositions/ approaches are the most promising?<br /> * What can I license?<br /> * Can you map blockbuster products to their patents?<br /> <br /> '''Can you save me some time?'''<br /> * What combinations/ compounds have already been tried?<br /> * Is any empirical data available?<br /> * Can you tell me the side effects?<br /> <br /> '''Where should I focus my R&amp;D investment?'''<br /> * What are the most promising approaches?<br /> * Where’s the ‘white space’ for me to play in?<br /> <br /> '''Any hints for research?'''<br /> * Are there any combinations I could develop?<br /> <br /> '''What should I do in this geography?'''<br /> * What are my competitors up to in this geography?<br /> * What are my strengths/ weaknesses here?<br /> <br /> '''What’s my competition up to?'''<br /> <br /> * What’s my top competitor investing in?<br /> * Are there any loopholes in their patents?<br /> * When are their patents expiring?<br /> * Will a competitor emerge from nowhere and surprise me?<br /> * What are the crowded areas?<br /> <br /> '''How do I play defense?'''<br /> * What should my blocking/reactive strategies be?<br /> <br /> <br /> == New Combinations based on IP study? ==<br /> <br /> Yes, new Combinations can be made with '''natural products''' based on IP study<br /> * Walnut extract containing [[Image:5ar.jpg]] inhibitor (as anti-androgen) and Flavnones (for vasodilation).<br /> * Sophora Flavnones (for vasodilation) in combination with Saw Palmetto berry (as anti-androgen).<br /> <br /> '''Note:''' The above combinations are based on limited study and are only possible examples<br /> <br /> == IP studies provides ==<br /> <br /> === Technology trends ===<br /> * Use of saw palmetto berry for treating alopecia was first patented in 1996.<br /> * Since then, 144 patents (including family patents) have been filed till 2006.<br /> * Most patents use saw palmetto berry in combination with other products.<br /> [[Image:Technology1.jpg|thumb|center|700px|Technology trends]]<br /> <br /> === New opportunities ===<br /> Yes, the IP studies provide new opportunities in the following area.<br /> * Sophora Flavescens contain flavnoids.<br /> * Natural extract Sophora Flavescens cited in LG patent of 2001.<br /> * Research shows fewer than 7 patents based on Sophora Flavescens for hair loss or alopecia.<br /> <br /> * What's this?<br /> <br /> == Conclusions ==<br /> * Hair loss medication is a very active area of research and intellectual property development.<br /> * One of the most promising areas of development is the area of Anti-androgens.<br /> * The top companies are Merck, L’Oreal and Smithkline.<br /> <br /> == Useful links ==<br /> * [http://www.biocarta.com/pathfiles/h_ghPathway.asp Pathways example]<br /> * [http://www.cellsignal.com/category.asp?catalog_name=CellSignal&amp;category_name=MAPK+Signaling Signaling Pathways]<br /> <br /> == Summary ==</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Alopecia_-_Hair_Loss&diff=1770 2006-05-21T01:35:00Z

<p>67.180.226.207: </p> <hr /> <div>__NOTOC__<br /> == Rationale ==<br /> * &quot;Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year.&quot; March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55]<br /> <br /> * &quot;An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries.&quot; February 16, 2006 – [http://stophair.setupmyblog.com/]<br /> <br /> * &quot;There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting.&quot; June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&amp;STORY=/www/story/06-07-2005/0003821470&amp;EDATE=]<br /> <br /> == Alopecia IPMap == <br /> [http://www.dolcera.com/client/ds94x0s90akq9d7xb402fm/hairloss_map.htm Dolcera IPMap for Alopecia]<br /> <br /> == Introduction ==<br /> <br /> === Hair Basics ===<br /> * Hair is a complex and delicate part of the body.<br /> * Keeping it healthy and beautiful is a challenge.<br /> * Hair grows everywhere on the body with the exception of the lips, eyelids, the palms of the hands and soles of the feet.<br /> * Hair is basically a form of skin. <br /> * Hair is made up of a protein called keratin.<br /> * Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin. <br /> * Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htm]<br /> * Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.html]<br /> [[Image:Hairbasics.jpg|thumb|center|500px|Structure of Hair root and Hair bulb]]<br /> <br /> === What causes Hair loss? === <br /> * Decreased growth of the hair <br /> * Increased shedding of the hair <br /> * Breakage of hairs <br /> * Conversion of thick terminal hairs to thin vellus hairs <br /> [[Image:Facts.jpg|thumb|right|400px|Survey results from Japan]]<br /> Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed '''“Male Pattern Baldness&quot;''' or '''&quot;Androgenetic Alopecia&quot;'''.<br /> <br /> === Androgenetic Alopecia ===<br /> * Gradual Onset.<br /> * Transition from large, thick, pigmented terminal hairs to thinner, shorter, indeterminate hairs and finally to short, wispy, nonpigmented vellus hairs in the involved areas.<br /> * Characterised by a receding hairline and/or hair loss on the top of the head.<br /> <br /> '''Main Causes'''<br /> * Genetic predisposition<br /> * Hormonal effect of androgen <br /> * Reduction of blood circulation around hair follicle<br /> * Deactivation of hair matrix cells<br /> <br /> '''Some facts from Japan''' <br /> <br /> * Market size: ¥ 30 Billion<br /> * Number of products: more than 100<br /> <br /> (JICST-EPlus - Japanese Science &amp; Technology)<br /> <br /> == Goals ==<br /> <br /> The goal of this report is to:<br /> * Summarize IP activity over the years<br /> * Identify major players<br /> * Conduct patent analysis<br /> a) Composition<br /> b) Nature<br /> c) Action<br /> <br /> '''And then'''<br /> <br /> * Analyze patents pertaining to high sebum activity<br /> <br /> == Approach ==<br /> <br /> * A broad search was conducted on hair loss patents.<br /> * Patent information was sourced through SIP.<br /> * A set of patents was selected for analysis.<br /> <br /> Composition of treatment for causes are identified and categorized as follows:<br /> <br /> * Anti-androgen<br /> * Minoxidil<br /> * Double action (Anti-androgen + Mindoxidil)<br /> * Hair matrix cells activator<br /> * Sebum production inhibitor<br /> <br /> == IP activity over years ==<br /> The graph indicates:<br /> * Number of patents filed every 5 years (except for first 7 years).<br /> * First solution proposed in 1973<br /> * Filing trend indicates steep rise in activity recently.<br /> [[Image:Year1.jpg|thumb|center|400px|IP Activity over years]]<br /> <br /> == Major Players ==<br /> [[Image:players.jpg|thumb|left|400px|Assignees with more than 20 patents ]]<br /> [[Image:players1.jpg|thumb|center|400px|Assignees with fewer than 20 patents ]]<br /> <br /> * '''Active Assignees'''<br /> Assignees currently active with more than 5 patents to their credit during 2000-2005. <br /> * Warner with 9 patents,<br /> * Bristol with 6 and<br /> * Abbott with 5.<br /> <br /> [[Image:Active.jpg|thumb|center|500px|Active Assignees]]<br /> <br /> == Anti-androgens == <br /> * Anti-androgens are used in hormone therapy.<br /> * Anti-androgens are designed to affect the hormones made in the adrenal glands. They don't stop the hormones from being made, but they stop them from having an effect leading to hair loss.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Testosterone is reduced to its active metabolite, Dihydrotestosterone (DHT) by the enzyme 5 alpha reductase.<br /> * DHT attaches to androgen receptor sites at the hair follicle. <br /> * DHT causes gradual miniaturization of the follicle, which eventually results in hair loss.<br /> <br /> '''How do anti-androgens treat hair loss?'''<br /> * Anti-androgens compete with DHT to bind to the androgen receptor.<br /> * Upon binding of anti-androgen in place of DHT, follicle miniaturization is lowered and hair loss prevented.<br /> <br /> === Functions of Anti-androgen === [http://www.revivogen.com/revivogen/work.html Anti-androgen]<br /> <br /> [[Image:Andogen1.jpg|thumb|center|500px|Functions of Anti-androgen]]<br /> <br /> === IP Map for Anti-androgen ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;8&quot;, style=&quot;#008080&quot;<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;30&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> BLOTECH (2004)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Palmetto berry extract (fatty acids &amp; sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans)<br /> |bgcolor=LightCyan|Fatty acids – Inhibit testosterone<br /> Sterols - Mechanism of action unknown.<br /> <br /> Quercetin results in cell growth cycle.<br /> <br /> Beta-sitosterol reduce inflammation on scalp<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 4-cycloalkoxy benzonitrile derivatives and salts<br /> |bgcolor=LightCyan|Acts as androgen receptor modulators and blocks formation of DHT.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> WARNER LAMBERT(2004)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives.<br /> |bgcolor=LightCyan|The compounds inhibit, or decrease, activation of androgen receptor by androgens.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> APHIOS Corp (2003)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives.<br /> |bgcolor=LightCyan|Modulates androgenic activity by inhibiting 5.alpha.-reductase activity.<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> Fundacion Pablo Cassara (2003)<br /> |bgcolor=LightCyan|Nucleotide<br /> |bgcolor=LightCyan|Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond)<br /> |bgcolor=LightCyan|Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> PFIZER INC (2001)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate <br /> |bgcolor=LightCyan|Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> N/A (1995)<br /> |bgcolor=LightCyan|Peptides/nucleic acid<br /> |bgcolor=LightCyan|Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein)<br /> |bgcolor=LightCyan|Inhibit synthesis of bradykinin receptors or compounds by binding to B2 receptor<br /> |- style=&quot;height:20px&quot; <br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> KAO Corp (1987)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Walnut extract (leaves/pericarps) with an organic solvent<br /> |bgcolor=LightCyan|Blocks formation of DHT<br /> |}<br /> <br /> == Minoxidil ==<br /> * Minoxidil is a &quot;potassium channel opener&quot; that leads to vasodilation.<br /> * The drug is available in two forms. Oral minoxidil is used to treat high blood pressure and the topical solution form is used to treat hair loss and baldness.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * A thick network of tiny veins and arteries lines the outer wall of the follicle. Blood pumps through the bulb and hair via this network.<br /> * DHT accumulates in the hair follicles and roots, constricting the blood supply of oxygen and nutrients to the hair roots; which is also seen to possibly contribute towards hair loss.<br /> <br /> '''How does Minoxidal treat hair loss?'''<br /> * Minoxidal is applied to the scalp topically, where it dilates blood vessels in the scalp and sustains the hair follicles for longer period of time.<br /> * Scientists and researchers are not exactly sure of how Minoxidil leads to this effect.<br /> * Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.<br /> <br /> === Functions of Monoxidil === [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 Minoxidil]<br /> <br /> [[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil]]<br /> <br /> === IP Map for Minoxidil ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> WARNER LAMBERT(2002)<br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|Benzopyran compounds<br /> |bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> LG HOUSEHOLD &amp; HEALTH CARE(2001)<br /> |bgcolor=LightCyan|Natural extracts<br /> |bgcolor=LightCyan|Sophora flavescens extract (alkaloids &amp; flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)<br /> |bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels<br /> |}<br /> <br /> == Double action (Anti-androgen + Minoxidil) ==<br /> * Combination of Minoxidil + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.<br /> <br /> <br /> '''What is the problem with using only Anti-androgen therapy?'''<br /> * Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.<br /> * Anti-androgen only prevent binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.<br /> <br /> '''What is the problem with using only Minoxidal therapy?'''<br /> * Minoxidil-based products are generally not effective in stopping hair loss as minoxidil does not block the harmful effects of DHT in the scalp and hair follicles. <br /> * Minoxidil simply dilates blood vessels in the scalp. However, the harmful DHT is still being produced in the body and still getting into the scalp and hair follicles and causing eventual hair loss.<br /> <br /> '''How is the combination of Anti-androgens and Minoxidil effective?'''<br /> * Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.<br /> * Minoxidil causes vasodilation and therefore improves supply of oxygen and nutrients to the hair follicle and roots.<br /> * Combination therapy therefore proves to be much more effective than individual therapy.<br /> <br /> === Functions of (Anti-androgen + Minoxidil) === [http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]<br /> [[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Minoxidil)]]<br /> <br /> === IP Map for (Anti-androgen + Minoxidil) ===<br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405] <br /> N/A(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhance and sunscreen<br /> |bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577] <br /> L'OREAL(2000)<br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP<br /> |bgcolor=LightCyan|Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762] <br /> COLOMER GROUP(1999)<br /> |bgcolor=LightCyan|Natural extract<br /> |bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)<br /> |bgcolor=LightCyan|Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp<br /> |}<br /> <br /> <br /> == Hair matrix cell activator ==<br /> Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.<br /> <br /> <br /> '''What causes hair loss?'''<br /> * Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.<br /> * Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.<br /> * Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.<br /> * Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.<br /> <br /> <br /> '''How does hair cell matrix activator treat hair loss?'''<br /> * Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.<br /> * This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.<br /> * Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.<br /> <br /> === Functions of Hair matrix cell activator === [http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]<br /> [[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]<br /> <br /> === IP Map for Hair matrix cell activator ===<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> SHISEIDO(1999) <br /> |bgcolor=LightCyan|Organic compound<br /> |bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt<br /> |bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> L'OREAL(1998) <br /> |bgcolor=LightCyan|Peptides<br /> |bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions<br /> |bgcolor=LightCyan|Reducing the expression of MMPs (Metalloproteases) in the scalp - slow down or inhibit the degradation of the perifollicular matrix (extracellular matrix surround the hair follicle) <br /> |}<br /> <br /> == Sebum Production Inhibitor ==<br /> Sebum Production Inhibitor is a substance that prevents the synthesis of sebum, mixture of lipid substances.<br /> <br /> '''What causes hair loss?'''<br /> * Sebum is a fatty acid substance secreted from sebaceous glands associated with hair follicles.<br /> * Hair can get heavy sebum build-up and mixes with cholesterol to form a hardened plug around the bottom part of the hair bulb.<br /> * Hardened plugs prevent cell respirations and eventually lead to hair loss.<br /> * Bacteria will also attach to the hardened plug and this can also cause further cause problems with hair growth.<br /> <br /> '''How does Sebum production inhibitor treat hair loss?'''<br /> * The inhibitor prevents synthesis of sebum and slows down accumulation and mixing of sebum with cholesterol leading to hardened plugs. <br /> * Reduction of sebum results in unclogged hair follicles/bulbs and allows oxygen and nutrients from reaching the hair follicle.<br /> * Reduction in sebum also prevents vasoconstriction.<br /> * Sum result of these effects of Sebum production inhibitor is prevention of hair loss.<br /> <br /> <br /> * The inhibitor blocks the excessive sebum production produces greasy effect on hair and scalp and also responsible for thinning and loosing of hair.<br /> <br /> === Functions of Sebum Production Inhibitor ===<br /> [[http://en.wikipedia.org/wiki/Image:HairFollicle.jpg Sebum Production Inhibitor]]<br /> [[Image:Sebum1.jpg|thumb|center|500px|Functions of Sebum Production Inhibitor]]<br /> <br /> === IP map for Sebum Production Inhibitor ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;3&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot; bgcolor=DodgerBlue|'''Pat/Pub#'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nature'''<br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition''' <br /> !width=&quot;300&quot; bgcolor=DodgerBlue|'''Composition action'''<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699] <br /> Unilever(2005)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Polyamine (putrescine, spermine or spermidine) analogs and/or derivatives; DFMO; N-acetyl cysteines; neutralized salts of a non-hydroxy C2-C40 dicarboxylic acids, preferably malonate salts; and mixtures thereof. <br /> |bgcolor=LightCyan|Decreasing sebum production and/or pore size <br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362] <br /> KAO COPR.(2004)<br /> |bgcolor=LightCyan|Natural extract and organic compound<br /> |bgcolor=LightCyan|Avocado oil (Butyl esters of fatty acids) <br /> |bgcolor=LightCyan|Reduce sebum of the hair and scalp<br /> |- style=&quot;height:100px&quot; <br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587] <br /> Unilever(1982)<br /> |bgcolor=LightCyan|organic compound<br /> |bgcolor=LightCyan |Biotin antagonist or a salt thereof <br /> |bgcolor=LightCyan|Decrease activity of the enzyme acetyl-SCoA-carboxylase and hence reduce lipid synthesis in sebaceous glands so that less sebum is produced <br /> |}<br /> <br /> == Composition nature matrix ==<br /> <br /> === IP map for Composition nature matrix ===<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;11&quot;, style=&quot;#008080&quot;<br /> !width=&quot;50&quot; bgcolor=DodgerBlue|'''Year'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Organic Compound'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extracts''' <br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Peptides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Nucleotides'''<br /> !width=&quot;75&quot; bgcolor=DodgerBlue|'''Natural extract + Organic comp'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|2005 <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |- <br /> |bgcolor=LightCyan|2004 <br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|BLOTECH (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |- <br /> |bgcolor=LightCyan|2003<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|APHIOS (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|FUNDIACION (1)<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2002<br /> |bgcolor=LightCyan|WARNER (1)<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2001<br /> |bgcolor=LightCyan |PFIZER (1)<br /> |bgcolor=LightCyan|LG HEALTH-CARE (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|2000<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1) / N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1999<br /> |bgcolor=LightCyan|SHISEDIO (1)<br /> |bgcolor=LightCyan|COLOMER (1) <br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |- <br /> |bgcolor=LightCyan|1998<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|L’OREAL (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1995<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |bgcolor=LightCyan|N/A (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|.... <br /> |-<br /> |bgcolor=LightCyan|1987<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|KAO (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |-<br /> |bgcolor=LightCyan|1982<br /> |bgcolor=LightCyan|UNILEVER (1)<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |bgcolor=LightCyan|....<br /> |}<br /> <br /> == Focus of patents ==<br /> <br /> {| border=&quot;1&quot; cellpadding=&quot;17&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Focus of patents'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Stimulating hair growth using benzopyrans<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Compositions to prevent or reduce hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Method of decreasing sebum production and pore size<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699 ]<br /> |bgcolor=LightCyan|16<br /> |- <br /> |bgcolor=LightCyan|Method for reducing sebum on the hair and skin<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |bgcolor=LightCyan|17<br /> |}<br /> <br /> === Focus of patents by technology ===<br /> [[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]<br /> <br /> == Distribution of patents ==<br /> <br /> === Distribution based on patent types ===<br /> [[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]<br /> <br /> <br /> === Distribution of patents by their key ingredients ===<br /> [[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]<br /> <br /> === Distribution based on target diseases ===<br /> [[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]<br /> <br /> <br /> === Key ingredients vs. Target disease/disorder ===<br /> [[Image:key&amp;target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]<br /> <br /> <br /> === Target species ===<br /> [[Image:Species.jpg|thumb|center|700px|Target species]]<br /> <br /> <br /> === Mode of administration ===<br /> [[Image:Mode.jpg|thumb|center|700px|Mode of administration]]<br /> <br /> <br /> === Product type vs. Product form ===<br /> [[Image:prod.jpg|thumb|center|700px|Product type vs. Product form]]<br /> <br /> == Distribution of patents based on different aspects ==<br /> <br /> === List of patents ===<br /> {| border=&quot;1&quot; cellpadding=&quot;9&quot;, style=&quot;#008080&quot;<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=LightCyan|1<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|10<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |- <br /> |bgcolor=LightCyan|2<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|11<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |- <br /> |bgcolor=LightCyan|3<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430] <br /> |bgcolor=LightCyan|12<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |- <br /> |bgcolor=LightCyan|4<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427] <br /> |bgcolor=LightCyan|13<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |- <br /> |bgcolor=LightCyan|5<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282] <br /> |bgcolor=LightCyan|14<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |- <br /> |bgcolor=LightCyan|6<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467] <br /> |bgcolor=LightCyan|15<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |- <br /> |bgcolor=LightCyan|7<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|16<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277699%22.PGNR.&amp;OS=DN/20050277699&amp;RS=DN/20050277699 US20050277699]<br /> |- <br /> |bgcolor=LightCyan|8<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|17<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |- <br /> |bgcolor=LightCyan|9<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010] <br /> |bgcolor=LightCyan|18<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=4529587.PN.&amp;OS=PN/4529587&amp;RS=PN/4529587 US4529587]<br /> |}<br /> <br /> === Distribution of patents based on target diseases ===<br /> {| border=&quot;1&quot; cellpadding=&quot;16&quot;, style=&quot;#008080&quot;<br /> !width=&quot;600&quot; bgcolor=DodgerBlue|'''Target disease/ disorder'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Rec. no.'''<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness)<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220020052498%22.PGNR.&amp;OS=DN/20020052498&amp;RS=DN/20020052498 US20020052498]<br /> |bgcolor=LightCyan|1<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, male pattern baldness and female pattern baldness<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030007941%22.PGNR.&amp;OS=DN/20030007941&amp;RS=DN/20030007941 US20030007941]<br /> |bgcolor=LightCyan|2<br /> |- <br /> |bgcolor=LightCyan|Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both.<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009430%22.PGNR.&amp;OS=DN/20060009430&amp;RS=DN/20060009430 US20060009430]<br /> |bgcolor=LightCyan|3<br /> |- <br /> |bgcolor=LightCyan|Inappropriate activation of the androgen receptor, acne, oily skin, alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009427%22.PGNR.&amp;OS=DN/20060009427&amp;RS=DN/20060009427 US20060009427]<br /> |bgcolor=LightCyan|4<br /> |- <br /> |bgcolor=LightCyan|Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050118282%22.PGNR.&amp;OS=DN/20050118282&amp;RS=DN/20050118282 US20050118282]<br /> |bgcolor=LightCyan|5<br /> |- <br /> |bgcolor=LightCyan|Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050085467%22.PGNR.&amp;OS=DN/20050085467&amp;RS=DN/20050085467 US20050085467]<br /> |bgcolor=LightCyan|6<br /> |- <br /> |bgcolor=LightCyan|Androgen-associated hair loss and androgen-skin related disorders. <br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060009429%22.PGNR.&amp;OS=DN/20060009429&amp;RS=DN/20060009429 US20060009429]<br /> |bgcolor=LightCyan|7<br /> |- <br /> |bgcolor=LightCyan|Androgenetic or androgenic alopecia or androgeno-genetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220030073616%22.PGNR.&amp;OS=DN/20030073616&amp;RS=DN/20030073616 US20030073616]<br /> |bgcolor=LightCyan|8<br /> |- <br /> |bgcolor=LightCyan|Diseases caused by testosterone (male-pattern alopecia)<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP0279010&amp;F=0 EP0279010]<br /> |bgcolor=LightCyan|9<br /> |- <br /> |bgcolor=LightCyan|Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040157856%22.PGNR.&amp;OS=DN/20040157856&amp;RS=DN/20040157856 US20040157856]<br /> |bgcolor=LightCyan|10<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050053572%22.PGNR.&amp;OS=DN/20050053572&amp;RS=DN/20050053572 US20050053572]<br /> |bgcolor=LightCyan|11<br /> |- <br /> |bgcolor=LightCyan|Alopecia, androgenic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220060052405%22.PGNR.&amp;OS=DN/20060052405&amp;RS=DN/20060052405 US20060052405]<br /> |bgcolor=LightCyan|12<br /> |- <br /> |bgcolor=LightCyan|Hair loss<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050123577%22.PGNR.&amp;OS=DN/20050123577&amp;RS=DN/20050123577 US20050123577]<br /> |bgcolor=LightCyan|13<br /> |- <br /> |bgcolor=LightCyan|Male pattern alopecia<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6447762.PN.&amp;OS=PN/6447762&amp;RS=PN/6447762 US6447762]<br /> |bgcolor=LightCyan|14<br /> |- <br /> |bgcolor=LightCyan|Androgenetic, androgenic or androgenogenetic alopecia<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040071647%22.PGNR.&amp;OS=DN/20040071647&amp;RS=DN/20040071647 US20040071647]<br /> |bgcolor=LightCyan|15<br /> |- <br /> |bgcolor=LightCyan|Curing other scalp related problems<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050244362%22.PGNR.&amp;OS=DN/20050244362&amp;RS=DN/20050244362 US20050244362]<br /> |bgcolor=LightCyan|16<br /> |}<br /> <br /> === Distribution of patents based on application ===<br /> [[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]<br /> <br /> === Interactive Signaling Pathway and linkages ===<br /> [[Image:Slide1.GIF|thumb|center|700px|Alopecia pathways]]<br /> <br /> == Players of Wnt inhibition Pathway == [[Image:wnt.jpg|thumb|right|600px|Wnt inhibition]]<br /> {| border=&quot;1&quot; cellpadding=&quot;15&quot;, style=&quot;#008080&quot;<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Patent no.'''<br /> !width=&quot;20&quot; bgcolor=DodgerBlue|'''Key compound'''<br /> !width=&quot;70&quot; bgcolor=DodgerBlue|'''Players of inhibition'''<br /> |- style=&quot;height:10px&quot;<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6989385.PN.&amp;OS=PN/6989385&amp;RS=PN/6989385 US6989385]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|GSK3<br /> |-<br /> |bgcolor=lightyellow|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256]<br /> |bgcolor=lightyellow|Pyrazole compounds <br /> |bgcolor=lightyellow|CDK,GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6974819.PN.&amp;OS=PN/6974819&amp;RS=PN/6974819 US6974819]<br /> |bgcolor=LightCyan|Pyrimidine derivative<br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6743791.PN.&amp;OS=PN/6743791&amp;RS=PN/6743791 US6743791]<br /> |bgcolor=LightCyan|Heterocyclic compounds<br /> |bgcolor=LightCyan|AKT3, GSK-3, ERK2<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220050277773%22.PGNR.&amp;OS=DN/20050277773&amp;RS=DN/20050277773 US20050277773]<br /> |bgcolor=LightCyan|Pyrrolo[3,2-d]pyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PG01&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.html&amp;r=1&amp;f=G&amp;l=50&amp;s1=%2220040072836%22.PGNR.&amp;OS=DN/20040072836&amp;RS=DN/20040072836 US20040072836]<br /> |bgcolor=LightCyan|Aza-oxindole derivatives <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=EP1477489&amp;F=0 EP1477489]<br /> |bgcolor=LightCyan|Pyrrolopyrimidine derivatives <br /> |bgcolor=LightCyan|GSK3<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO0056710&amp;F=0 WO0056710]<br /> |bgcolor=LightCyan|3-(Anilinomethylene) oxindoles <br /> |bgcolor=LightCyan|GSK3, AKT, PKC<br /> |-<br /> |bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO03011287&amp;F=0 WO2003011287]<br /> |bgcolor=LightCyan|Pyrazolon derivatives <br /> |bgcolor=LightCyan|GSK3, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6924141.PN.&amp;OS=PN/6924141&amp;RS=PN/6924141 US6924141]<br /> |bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7 <br /> |bgcolor=LightCyan|β-catenin, GSK3, Wnt<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6706685.PN.&amp;OS=PN/6706685&amp;RS=PN/6706685 US6706685]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6683048.PN.&amp;OS=PN/6683048&amp;RS=PN/6683048 US6683048]<br /> |bgcolor=LightCyan|Peptide sequence <br /> |bgcolor=LightCyan|α-catenin, β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6677116.PN.&amp;OS=PN/6677116&amp;RS=PN/6677116 US6677116]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |-<br /> |bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6303576.PN.&amp;OS=PN/6303576&amp;RS=PN/6303576 US6303576]<br /> |bgcolor=LightCyan|Peptide sequence LXXLL<br /> |bgcolor=LightCyan|β-catenin<br /> |}<br /> [[Image:coloury.jpg]]- '''Target sites and Details'''<br /> <br /> == Pyrazole compounds ==<br /> <br /> * '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.<br /> * Pyrazoles are produced synthetically through the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation <br /> [[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]<br /> * Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.<br /> * Structurally related compounds are pyrazoline and pyrazolidine.<br /> [[Image:pyrazole2.jpg|thumb|center|500px|Structurally related compounds]]<br /> <br /> === GSK3 inhibition by pyrazole compounds ===<br /> [[Image:bold3.jpg]]<br /> {| border=&quot;1&quot; cellpadding=&quot;2&quot;, style=&quot;#008080&quot;<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?TERM1=6989385+&amp;Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=0&amp;f=S&amp;l=50 US6989385]<br /> [[Image:US6989385.jpg]]<br /> !width=&quot;100&quot;|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&amp;Sect2=HITOFF&amp;d=PALL&amp;p=1&amp;u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&amp;r=1&amp;f=G&amp;l=50&amp;s1=6664247.PN.&amp;OS=PN/6664247&amp;RS=PN/6664247 US6664247] <br /> [[Image:US6664247.jpg]]<br /> !width=&quot;100&quot;|[http://v3.espacenet.com/textdoc?DB=EPODOC&amp;IDX=WO2005012256&amp;F=0 WO2005012256] <br /> [[Image:WO2005012256.jpg]]<br /> |- <br /> |bgcolor=lightcyan|R1=T-Ring D, wherein <br /> T is a valence bond and <br /> Ring D = 5-6 membered aryl or heteroaryl ring; <br /> <br /> R2 = hydrogen or C1-4 aliphatic and <br /> R2'= hydrogen; <br /> <br /> R3 = -R, -OR, or -N(R4)2, wherein <br /> R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and <br /> L is -O-, -S-, or -NH-; and <br /> Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R&lt;4&gt;), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring<br /> <br /> |bgcolor=lightcyan|X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; <br /> <br /> R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; <br /> <br /> R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and <br /> <br /> R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).<br /> <br /> |bgcolor=lightcyan|X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;<br /> A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy).<br /> |}<br /> <br /> === GSK3 inhibition by pryazole pyrimidine amine derivatives ===<br /> <br /> '''Patent Number''': US6989385<br /> '''Applicant''': ''Vertex Pharmaceuticals Incorporated''<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol1.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-p- yrimidin-4-yl]-amine <br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyl- sulfanyl]-pyrimidin-4-yl}-amine <br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-me- thyl-2H-pyrazol-3-yl)-amine <br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * {2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-y- l}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(- 5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- -pyrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfa- nyl)-pyrimidin-4-yl]-amine <br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-- 2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mo- rpholin-4-yl-pyrimidin-4-yl}-amine <br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimi- din-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyri- midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-- methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-meth- yl-2H-pyrazol-3-yl)-amine <br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * 5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-ylmethylsulf- anyl)-pyrimidin-4-yl]-amine <br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)-phenyl]-py- rimidin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methy- l-2H-pyrazol-3-yl)-amine <br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m- ethyl-2H-pyrazol-3-yl)-amine <br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- -methyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methylphenylamino)-6-phenyl-pyrimidi- n-4-yl]-amine <br /> * [2-(4-cyanomethylphenylamino)-6-phenyl-pyrimidin-4-yl]-(5-cyclopropyl-2H-p- yrazol-3-yl)-amine <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(pyridin-3-ylmethylamino)-pyri- midin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-methyl-2H-py- razol-3-yl)-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3,4,5-trimethoxyphenyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(4-sulfamoylphenylamino)-6-(3,4,5-trimethoxy- phenyl)-pyrimidin-4-yl]-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyraz- ol-3-yl]-amine <br /> * [2-(Benzimidazol-2-ylamino-)6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(4-Chlorophenyl)amino-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-6-ethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * (5-tert-Butyl-2H-pyrazol-3-yl)-[2-(3-chlorophenyl)amino-6-(3-nitrophenyl)-- pyrimidin-4-yl]-amine <br /> * [2-(3-Chlorophenyl)amino-6-(3-nitrophenyl)-pyrimidin-4-yl]-(5-phenyl-2H-py- razol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-phenyl-2-phenylamino-pyrimidin-4-yl)-a- mine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methyl-pyrimidin-4-yl]-[5-(Furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * [2-(4-Chlorophenylamino)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y- l)-amine <br /> * [2-(4-Chlorophenyl)amino-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * (5,6-Dimethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Chlorophenyl)amino-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-pyra- zol-3-yl)-amine <br /> * [2-(Benzimidazol-2-ylamino)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * (6-Methoxymethyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-- amine <br /> * (6-Methyl-2-phenylamino-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-3- -yl)-amine <br /> * [2-(2-Chlorophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-pyr- azol-3-yl]-amine <br /> * (6-methyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-phenyl-2H-pyrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenoxymethyl-pyrimidin-4-yl)- -amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-(6-methyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-amine <br /> * [6-Methyl-2-(4-methyl-phenylsulfanylmethyl)-pyrimidin-4-yl]-(5-phenyl-2H-p- yrazol-3-yl)-amine <br /> * [5-(Furan-2-yl)-2H-pyrazol-3-yl]-[6-Methyl-2-(4-methyl-phenylsulfanylmethy- l)-pyrimidin-4-yl]-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Fluoro-phenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-py- razol-3-yl]-amine <br /> * (6-Ethyl-2-phenylsulfanylmethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)- -amine <br /> * (6-Ethyl-2-phenoxymethyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Ethyl-2-(4-fluorophenoxymethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-- yl)-amine <br /> * [6-Ethyl-2-(1-methyl-1-phenyl-ethyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-phenyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol- -3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-methyl-2H-- pyrazol-3-yl)-amine <br /> * [2-(4-Chlororophenoxymethyl)-6-methyl-pyrimidin-4-yl]-[5-(furan-2-yl)-2H-p- yrazol-3-yl]-amine <br /> * (5-Methyl-2H-pyrazol-3-yl)-(2-phenylsulfanylmethyl-5,6,7,8-tetrahydro-quin- azolin-4-yl)-amine <br /> * [2-(4-Methylphenylsulfanylmethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidi- n-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(1-Methyl-1-phenyl-ethyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-y- l]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6,7,8-tetrahydro-quinazolin-4-yl]-(5-methyl-2H-p- yrazol-3-yl)-amine <br /> * [7-Benzyl-2-(2,6-dichlorobenzyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-- 4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [6-Benzyl-2-(4-chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimi- din-4-yl]-(5-methyl-2H-pyrazol-3-yl)-<br /> * [2-(4-Chlorophenoxymethyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl]- -(5-methyl-2H-pyrazol-3-yl)-amine <br /> * [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine <br /> * [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine <br /> ----<br /> '''Patent Number''': US7008948 <br /> '''Applicant''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure'''<br /> <br /> [[Image:pyrazol2.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(1H-i- ndazol-3-yl)-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[3,4-d]pyrimidin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(7-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5-fl- uoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-4-yl]-(5,7-- difluoro-1H-indazol-3-yl)-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- oquinazolin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetra- hydroquinazolin-4-yl]-amine <br /> * (5-Trifluoromethyl-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-- tetrahydroquinazolin-4-yl]-amine <br /> * (5,7-difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetra- hydro-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (6-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyr- imidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydro-5H-cycl- oheptapyrimidin-4-yl]-amine<br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-6,7,8,9-tetrahydr- o-5H-cycloheptapyrimidin-4-yl]-amine<br /> * (5-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydr- o-pyrido[4,3-d]pyrimidin-4-yl]-amine<br /> * (1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydroquinazol- in-4-yl]-amine <br /> * (7-Benzyl-2-(2-trifluoromethyl-phenyl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(5-fluoro-1H-indazol-3-yl)-amine<br /> * (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> * 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine <br /> ----<br /> '''Patent Number''': US6977262<br /> '''Assignee''': Mitsubishi Pharma Corporation<br /> '''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof<br /> '''Basic Structure''':<br /> <br /> [[Image:pyrazol3.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate<br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-methyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Methyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * t-Butyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Isopropyl 4-(2-fluorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * Benzyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate <br /> * 4-(2-Chlorophenyl)-5-dimethylaminocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4-(2-Chlorophenyl)-5-hydrazinocarbonyl-4,7-dihydro-6-methyl-2H-pyrazolo[3,4 -b]pyridine <br /> * 4-(2-Fluorophenyl)-4,7-dihydro-6-methyl-5-isopropylthiocarbonyl-2H-pyrazolo [3,4-b]pyridine <br /> * 4,7-Dihydro-6-methyl-5-nitro-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4-b] pyridine <br /> * Ethyl 4,7-dihydro-4-phenyl-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridine-5-carbox ylate <br /> * Ethyl 4-(2-fluorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate <br /> * Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate maleate <br /> * Ethyl 4,7-dihydro-4-(2-methoxyphenyl)-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridi ne-5-carboxylate <br /> * Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate <br /> * Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate<br /> ----<br /> '''Patent Number''': US6664247<br /> '''Assignee''': Vertex Pharmaceuticals Incorporated<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors'''<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol4.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine<br /> * (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine<br /> * [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine<br /> * [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine<br /> * [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine<br /> * [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine<br /> * [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine<br /> * [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine<br /> * 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine<br /> * [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine<br /> * {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine<br /> * [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine<br /> * (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine<br /> * {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine<br /> * [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine<br /> * [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine<br /> * [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine<br /> * [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.<br /> ----<br /> '''Patent Number''': US2004224944<br /> '''Assignee''': VERTEX PHARMACEUTICALS INC<br /> '''Title''': Pyrazole compounds useful as protein kinase inhibitors<br /> '''Basic Structure''': <br /> <br /> [[Image:pyrazol5.jpeg]]<br /> <br /> '''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''<br /> <br /> * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine <br /> * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine <br /> * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine <br /> * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine <br /> * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster <br /> * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-<br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine <br /> * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine<br /> <br /> === Other derivates used by different assigness for the treatment of alopecia ===<br /> [[Image:other derivates.jpeg]]<br /> <br /> == Inhibition of 5- - reductase by Finasteride ==<br /> [[Image:5-alpha-reductase inhibition.jpeg]]<br /> <br /> === Structure-Activity Relationships (SARs) of Finasteride ===<br /> [[Image:SAR_map.gif]]<br /> <br /> == Questions Dolcera Answers ==<br /> <br /> '''What’s hot?'''<br /> * What compositions/ approaches are the most promising?<br /> * What can I license?<br /> * Can you map blockbuster products to their patents?<br /> <br /> '''Can you save me some time?'''<br /> * What combinations/ compounds have already been tried?<br /> * Is any empirical data available?<br /> * Can you tell me the side effects?<br /> <br /> '''Where should I focus my R&amp;D investment?'''<br /> * What are the most promising approaches?<br /> * Where’s the ‘white space’ for me to play in?<br /> <br /> '''Any hints for research?'''<br /> * Are there any combinations I could develop?<br /> <br /> '''What should I do in this geography?'''<br /> * What are my competitors up to in this geography?<br /> * What are my strengths/ weaknesses here?<br /> <br /> '''What’s my competition up to?'''<br /> <br /> * What’s my top competitor investing in?<br /> * Are there any loopholes in their patents?<br /> * When are their patents expiring?<br /> * Will a competitor emerge from nowhere and surprise me?<br /> * What are the crowded areas?<br /> <br /> '''How do I play defense?'''<br /> * What should my blocking/reactive strategies be?<br /> <br /> <br /> == New Combinations based on IP study? ==<br /> <br /> Yes, new Combinations can be made with '''natural products''' based on IP study<br /> * Walnut extract containing [[Image:5ar.jpg]] inhibitor (as anti-androgen) and Flavnones (for vasodilation).<br /> * Sophora Flavnones (for vasodilation) in combination with Saw Palmetto berry (as anti-androgen).<br /> <br /> '''Note:''' The above combinations are based on limited study and are only possible examples<br /> <br /> == IP studies provides ==<br /> <br /> === Technology trends ===<br /> * Use of saw palmetto berry for treating alopecia was first patented in 1996.<br /> * Since then, 144 patents (including family patents) have been filed till 2006.<br /> * Most patents use saw palmetto berry in combination with other products.<br /> [[Image:Technology1.jpg|thumb|center|700px|Technology trends]]<br /> <br /> === New opportunities ===<br /> Yes, the IP studies provide new opportunities in the following area.<br /> * Sophora Flavescens contain flavnoids.<br /> * Natural extract Sophora Flavescens cited in LG patent of 2001.<br /> * Research shows fewer than 7 patents based on Sophora Flavescens for hair loss or alopecia.<br /> <br /> * What's this?<br /> <br /> == Conclusions ==<br /> * Hair loss medication is a very active area of research and intellectual property development.<br /> * One of the most promising areas of development is the area of Anti-androgens.<br /> * The top companies are Merck, L’Oreal and Smithkline.<br /> <br /> == Useful links ==<br /> * [http://www.biocarta.com/pathfiles/h_ghPathway.asp Pathways example]<br /> * [http://www.cellsignal.com/category.asp?catalog_name=CellSignal&amp;category_name=MAPK+Signaling Signaling Pathways]<br /> <br /> == Summary ==</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Template:Btot&diff=1742 2006-05-14T07:08:24Z

<p>67.180.226.207: </p> <hr /> <div>&lt;div class=&quot;editsection&quot; style=&quot;float: right; margin-left: 5px;&quot;&gt;[&lt;span&gt;[[#top|top of page]]&lt;/span&gt;]&lt;/div&gt;</div>

67.180.226.207 https://www.dolcera.com/wiki/index.php?title=Hybrid_Electric_Vehicle_Battery_System&diff=1741 2006-05-14T07:08:09Z

<p>67.180.226.207: /* Summary */</p> <hr /> <div>== Introduction ==<br /> <br /> == Rationale ==<br /> [[image:globalwarming.jpg|thumb|right|220px|Global warming emissions by sector]]<br /> <br /> * Automobiles are a source of considerable pollution at the global level, including a significant fraction of the total greenhouse gas emissions. <br /> * On July 22, 2002 California Governor Gray Davis signed into law AB 1493 (commonly known as the &quot;Pavley law&quot;) — precedent-setting legislation to reduce global warming pollution from motor vehicles.<br /> * This bill directs the California Air Resources Board (CARB) to develop and adopt regulations that achieve the maximum feasible and cost-effective reduction of greenhouse gas emissions (GHG) from passenger cars and light trucks sold in California.<br /> <br /> == New Developments ==<br /> <br /> '''Sample visual interactive model (&quot;dummy&quot; data):'''<br /> &lt;gflash&gt;545 375 http://www.dolcera.com/HEV_model.swf&lt;/gflash&gt;<br /> <br /> The new millennium is bringing a millennial change to the family car. A few years back, the key concerns were:<br /> * Pollution, <br /> * Nagging worries about global warming, and<br /> * Oil shortages.<br /> These concerns led to the development of Electric Vehicle (EV’s) powered by batteries. But current battery technology does not provide EV's with a range that is acceptable to consumers. <br /> <br /> '''Limitations of EV’s''':<br /> * An average commute to work is around 40 miles. <br /> * EV's have a range of 80-100 miles using advanced battery technology.<br /> * While batteries need frequent recharging, they are not the only way to power an electric car.<br /> <br /> == Hybrid Electric Vehicle (HEV) ==<br /> The Hybrid Electric Vehicle (HEV) is just the first step in reducing the environmental impacts of automobile use without losing comfort, performance, storage room and extended driving range. <br /> <br /> '''Advantages of HEV’s''':<br /> * The HEV contains parts of both gasoline and electric vehicles in an attempt to get the best of both worlds.<br /> * It is able to operate nearly twice as efficiently as traditional internal combustion vehicles.<br /> * It has equivalent power, range, cost and safety of a conventional vehicle while reducing fuel costs and harmful emissions.<br /> * The battery is continuously recharged by a motor/generator driven by the Internal Combustion Engine (ICE) or by regenerative braking.<br /> <br /> == Components of the HEV Battery System ==<br /> The battery in an HEV is the energy storage device for the electric motor. Unlike the gasoline in the fuel tank, which can only power the gasoline engine, the electric motor in a hybrid car can put energy into the battery as well as draw energy from it. <br /> <br /> * '''Battery''': Two or more electrochemical energy cells connected together to provide electrical energy.<br /> * '''Generator''': The generator is similar to an electric motor, but it acts only to produce electrical power.<br /> * '''Electric motor''': Advanced electronics allow it to act as a motor as well as a generator. For example, when it needs to, it can draw energy from the batteries to accelerate the car. But acting as a generator, it can slow the car down and return energy to the batteries. <br /> * '''SOC''': The State of Charge of a battery is its available capacity expressed as a percentage of its rated capacity<br /> <br /> [[Image:Hev layout.jpg|thumb|center|700px|Components of the HEV Battery System]]<br /> <br /> == HEV battery system design parameters ==<br /> <br /> Factors affecting battery performance:<br /> * Temperature: Battery performance is highly dependent on temperature. Each type of battery works best within a limited range of temperatures.<br /> * Battery age/Shelf life: Corrosion is the main culprit behind decreased performance in lead acid type batteries with age.<br /> * Depth of discharge: Batteries are able to maintain their performance longer when they are not deeply discharged regularly.<br /> <br /> Design parameters:<br /> * How much space is available for the batteries?<br /> * How much can they weigh? <br /> * What is the desired range? <br /> * What is the weight of the vehicle? <br /> * What is the targeted vehicle cost? <br /> * How will the batteries be recharged and <br /> * What kind of drive system requirements is needed? <br /> <br /> These questions are necessary because of the variety of battery types available and the differences between them. The chart below lists the characteristics of the most common types of batteries. (Source [http://www.atti-info.org/technology/ev_tech.html])<br /> <br /> [[Image:batterytypes.jpg|thumb|center|400px|Battery types by descending order of popularity]]<br /> <br /> == Comparison of top 3 batteries used in HEVs ==<br /> During recharging, it is important to maintain the balance of battery. The balance of battery is maintained by controlling battery from overcharging and over discharging.<br /> <br /> The battery is controlled by defining State of Charge (SOC) of the battery:<br /> * Upper limit value – overcharge and <br /> * Lower limit value – over discharge<br /> <br /> When overcharge is detected, power generation is controlled/cut-off and when over discharge is detected, power supply to electric motor is stopped. Detection is achieved by appropriate sensors.<br /> '''''This report investigates various procedures available/adopted by various assignees in order to maintain balanced battery pack by avoiding overcharge and/or over discharge.<br /> '''''<br /> <br /> &lt;blockquote style=&quot;background: white; border: 2px solid black; padding: 1em;&quot;&gt;<br /> {| class=&quot;wikitable&quot; style=&quot;text-align:center&quot;<br /> |-<br /> ! Lead Acid !! Advanced Lead Acid !! Nickel-Metal Hydride<br /> |-<br /> | Low cost || Longer lifecycle than conventional lead acid || High cost<br /> |-<br /> | Low energy density || Valve regulated lead/acid (VRLA) batteries showing promise || Higher energy density than lead acid; not as susceptible to heat<br /> |-<br /> | Longer recharging time (6-8 hours) || || Shorter recharging time<br /> |-<br /> | Only fair cycle life || || <br /> |-<br /> | Can be ruined by completely discharging them || || <br /> |}<br /> &lt;/blockquote&gt;<br /> <br /> == HEV battery system concerns ==<br /> The ultimate goal of HEV can only be achieved with the balance battery pack since the main source of energy is batteries and recharging is carried out on board. <br /> <br /> '''Advantages of balance battery pack''':<br /> * Balancing of battery SOC’s increases battery life<br /> * Automated balancing circuitry will decrease overcharging (and gassing) and decrease manual maintenance.<br /> <br /> This, in turn, provides:<br /> * Equivalent power range at low cost as conventional vehicle while reducing fuel costs and harmful emissions. <br /> * Twice the travel distance of a conventional vehicle on the same amount of energy.<br /> <br /> == Goal ==<br /> This report attempts to summarize various approaches involved in maintaining battery balance. We have selected a few patents, and will show:<br /> * IP activity over the years<br /> * Competitors<br /> * Competitor and Market Landscape<br /> * Technology map<br /> * Technology approaches<br /> <br /> === IP activity over the years ===<br /> [[Image:patentsoveryears.jpg|thumb|center|500px|IP activity over the years]]<br /> <br /> === Assignee wise IP activity ===<br /> Companies with many patents of HEV battery are arranged in decreasing order in the graph given below. Top three players are Nissan motors with (5) patent records to its credit, followed by Toyota with (4) and Acqueous (3). <br /> [[Image:Assignee wise IP.jpg|thumb|center|500px|Assignee wise IP activity]] <br /> <br /> === Competitor and Market Landscape ===<br /> <br /> The left graph given below displays the assignee wise IP activity over years, according to the present data the very first patent pertaining to HEV battery charging system was filed by HYBRICON in 1978 but is not in the race anymore. Though NISSAN, AQUEOUS and TOYOTA seems to be ahead in acquiring max. number of patent to their credits, but not active since 2000. GM and HONDA have bagged single-single patent of same age in 2003. <br /> <br /> The right graph given below displays the market (countries) eyed by various competitors. The hot market place for most competitors is Japan (17) followed by United States (11) and Germany (04). According to the present data, Nissan seems to be having strong presence in Japan market that rests with 5 patents protected, followed by Aqueous and Toyota.<br /> <br /> We will look into their technologies in competitor approaches section latter in the report.<br /> [[Image:Competitor.jpg|thumb|center|700px|Competitor and Market Landscape]]<br /> <br /> === Distribution of patents based on Technology focus ===<br /> [[Image:Distribution.jpg|thumb|right|500px|Distribution of patents based on Technology focus]]<br /> <br /> The above pie chart displaying various factors has effect on battery charge and discharge. The numbers indicating the distribution of patents in that area are from selected list of patents. The distribution of patents is based on technology focused in the patent.<br /> <br /> * '''Power generation''': Technologies disclosed in patents for modes of power generation in HEV for charging the battery and ways of handling them.<br /> <br /> * '''Power management''': Technologies disclosed in patents for managing the battery balance during power generating and/or consuming.<br /> <br /> * '''Fluctuating HEV operating mode''': Technologies disclosed in patents for managing battery balance during fluctuating operating modes, especially in composite HEV.<br /> <br /> * '''Power supply''': Technology disclosed in patent for starting engine with auxiliary battery current when main battery current is not sufficient to start engine<br /> <br /> === IPMap ===<br /> [[Image:hev_ipmap.jpg]]<br /> <br /> == Clustering - Technology focus ==<br /> [[Image:Cluster.jpg|thumb|center|1000px|Clustering - Technology focus]]<br /> <br /> == Technology approach ==<br /> <br /> === Competitor's ===<br /> In technology approach patent and non-patent literature is used to extract information about the technology profile of various assignees such as<br /> <br /> * Years in this activity<br /> <br /> * Type of batteries used<br /> <br /> * Battery charging system<br /> <br /> * Types of HEV (Series (SHV)/Parallel (PHV)/Composite (SPHVS))<br /> <br /> * Technological strength based on citation analysis<br /> <br /> * Product Vs patent identification<br /> <br /> * Battery management solutions proposed (i.e. current control/cut-off system and SOC detection <br /> technique)<br /> <br /> * Scientific literature and technology news to strengthen the report, since patent activity is a slow process.<br /> <br /> === Toyota Motors ===<br /> <br /> * '''Battery type''': Lead-Acid battery<br /> <br /> * '''Battery charging system''': The charge to the DC-battery is provided from the power generated by the generator and the regeneration power from the drive motor at the time of braking.<br /> <br /> * '''Approach1:'''<br /> [[Image:Toyota.jpg]]<br /> <br /> * '''Approach2:'''<br /> [[Image:Toyota2.jpg|thumb|center|1000px|Toyota Motors - Technology Approach2]]<br /> <br /> * '''Findings:'''<br /> [[Image:Toyotafindings.jpg|thumb|center|700px|Findings]]<br /> <br /> === Nissan Motors ===<br /> <br /> * '''Battery type:-''' Lead-acid and/or Nickel-Hydrogen battery<br /> <br /> * '''Battery charging system:-'''<br /> The battery is charged from the power generated by the generator and regeneration power from a motor.Electric motor functions as a generator to charge the battery when a hybrid vehicle is restarted after an idling stop released.<br /> <br /> * '''Approach1:'''<br /> [[Image:Nissan1.jpg|thumb|center|1000px|Nissan Motors - Technology Approach1]]<br /> <br /> * '''Approach2:'''<br /> [[Image:Nissan2.jpg|thumb|center|1000px|Nissan Motors - Technology Approach2]]<br /> <br /> * '''Findings:'''<br /> <br /> * JP10295045 (1997):- Battery management system, received 21 forward citations from all big names in a span of 5 years and self- cited twice the same technology indicating strong technology strength and building on its own technology.<br /> <br /> * Patent and non-patent information indicate that Nissan has focused much on circuit arrangements for charging or depolarizing batteries or for supplying loads from batteries (H02J 7/00).<br /> <br /> * Jointly worked with Sony corp. (1998) developing high power density Li-ion battery for parallel HEV.<br /> <br /> * Proposed a novel charge/discharge control system based on car navigation information.<br /> <br /> {{btot}}</div>

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