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1. 发明申请

US20140113916A1 TRPV4 ANTAGONISTS 有权
公开(公告)号：US20140113916A1
公开(公告)日：2014-04-24
申请号：US14125370
申请日：2012-06-15
申请人： Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
发明人： Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
IPC分类号： C07D413/14 , C07D413/06
CPC分类号： C07D413/14 , C07D263/52 , C07D413/06 , C07D413/08
摘要： The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

2. 发明授权

US09187464B2 TRPV4 antagonists 有权
标题翻译： TRPV4拮抗剂
公开(公告)号：US09187464B2
公开(公告)日：2015-11-17
申请号：US14125378
申请日：2012-06-15
申请人： Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Tram H. Hoang , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
发明人： Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Tram H. Hoang , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
IPC分类号： C07D263/02 , A61K31/423 , C07D413/14 , C07D417/14 , C07D495/04 , C07F9/6558 , C07D419/14
CPC分类号： C07D413/14 , C07D417/14 , C07D419/14 , C07D495/04 , C07F9/65583
摘要： The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
摘要翻译：本发明涉及其中R1，（R2）Y，R3，R4，X和A具有本说明书中给出的含义的式（I）的螺氨酸甲酯化合物。本发明还提供含有化合物或其药学上可接受的盐的药物组合物，并且涉及它们在治疗或预防与TRPV4不平衡相关的病症中作为TRPV4拮抗剂的用途。

3. 发明授权

US09487507B2 TRPV4 antagonists 有权
公开(公告)号：US09487507B2
公开(公告)日：2016-11-08
申请号：US14125370
申请日：2012-06-15
申请人： Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
发明人： Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
IPC分类号： A01N43/76 , A61K31/42 , C07D263/52 , C07D498/00 , C07D413/14 , C07D413/06 , C07D413/08
CPC分类号： C07D413/14 , C07D263/52 , C07D413/06 , C07D413/08
摘要： The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

4. 发明申请

US20140121206A1 TRPV4 ANTAGONISTS 有权
公开(公告)号：US20140121206A1
公开(公告)日：2014-05-01
申请号：US14125378
申请日：2012-06-15
申请人： Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Tram H. Hoang , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
发明人： Carl Brooks , Mui Cheung , Hilary Schenck Eidam , Krista B. Goodman , Marlys Hammond , Mark A. Hilfiker , Tram H. Hoang , Jaclyn R. Patterson , Patrick Stoy , Guosen Ye
IPC分类号： C07D413/14 , C07D495/04 , C07D417/14
CPC分类号： C07D413/14 , C07D417/14 , C07D419/14 , C07D495/04 , C07F9/65583
摘要： The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
摘要翻译：本发明涉及其中R1，（R2）Y，R3，R4，X和A具有本说明书中给出的含义的式（I）的螺氨酸甲酯化合物。本发明还提供含有化合物或其药学上可接受的盐的药物组合物，并且涉及它们在治疗或预防与TRPV4不平衡相关的病症中作为TRPV4拮抗剂的用途。

5. 发明申请

US20100179109A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：US20100179109A1
公开(公告)日：2010-07-15
申请号：US12450631
申请日：2008-04-04
申请人： Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiano Ghirlanda , Alexey V. Ishchenko , Lara S. Kallander , Brian Lawhorn , Colin A. Leach , Qing Lu , Gerard McGeehan , Jaclyn R. Patterson , Robert D. Simpson , Suresh B. Singh , Patrick Stoy , Lamont R. Terrell , Colin Tice , Zhenrong Xu , Jing Yuan , Catherine C. K. Yuan , Jing Zhang , Wei Zhao
发明人： Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiano Ghirlanda , Alexey V. Ishchenko , Lara S. Kallander , Brian Lawhorn , Colin A. Leach , Qing Lu , Gerard McGeehan , Jaclyn R. Patterson , Robert D. Simpson , Suresh B. Singh , Patrick Stoy , Lamont R. Terrell , Colin Tice , Zhenrong Xu , Jing Yuan , Catherine C. K. Yuan , Jing Zhang , Wei Zhao
IPC分类号： A61K31/675 , C07D211/34 , A61K31/445 , C07D265/30 , A61K31/5375 , C07D413/06 , A61K31/5377 , A61K31/535 , A61K31/517 , A61K31/554 , A61K31/4965 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/47 , A61K31/566 , A61P25/28 , A61P33/06 , A61P31/18 , A61P9/12 , A61P9/10 , A61P25/22 , A61P27/06
CPC分类号： C07D211/96 , C07D211/22 , C07D401/10 , C07D401/12
摘要： Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译：公开了式（I）的化合物，其中R，R 1，R 2，R 3，X，Y，A，Q，E和G如本文所定义。这些化合物与天冬氨酸蛋白酶结合以抑制其活性，并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。还公开了使用式I化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。

6. 发明申请

US20100311989A1 PROCESS FOR THE PREPARATION OF RENIN INHIBITORS 审中-公开
标题翻译：制备瑞宁抑制剂的方法
公开(公告)号：US20100311989A1
公开(公告)日：2010-12-09
申请号：US12678007
申请日：2008-09-17
申请人： Marlys Hammond , Patrick Stoy , Scott K. Thompson
发明人： Marlys Hammond , Patrick Stoy , Scott K. Thompson
IPC分类号： C07D309/04 , C07C33/42
CPC分类号： C07D309/04 , Y02P20/55
摘要： Disclosed is a process for the preparation of tetrahydropyran-di-amine represented by Structural Formula (I): wherein R1 is H or alkyl and E is H or an amine protecting group.
摘要翻译：公开了由结构式（I）表示的四氢吡喃二胺的制备方法：其中R1是H或烷基，E是H或胺保护基。

7. 发明申请

US20110160300A1 Renin Inhibitors and Methods of Use Thereof 审中-公开
标题翻译：肾素抑制剂及其使用方法
公开(公告)号：US20110160300A1
公开(公告)日：2011-06-30
申请号：US12999969
申请日：2009-06-18
申请人： Marlys Hammond , Patrick Stoy
发明人： Marlys Hammond , Patrick Stoy
IPC分类号： A61K31/351 , C07D309/06 , A61P9/12 , A61P9/04 , A61P13/12 , A61P25/22 , A61K31/27 , C07C271/16
CPC分类号： C07D309/04 , A61K31/27 , A61K31/351 , C07C271/16
摘要： Disclosed are aspartic protease inhibitors represented by the following Formula: wherein R1, R2, R3, R4, R5, R6, R7a, R7b and n are as defined herein, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods for treating an aspartic protease mediated disorder using the same.
摘要翻译：公开了由下式表示的天冬氨酸蛋白酶抑制剂：其中R1，R2，R3，R4，R5，R6，R7a，R7b和n如本文所定义，或其药学上可接受的盐，包含其的药物组合物和治疗方法使用其的天冬氨酸蛋白酶介导的病症。

8. 发明授权

US5939208A Method for creation of biomimetic surfaces 失效
标题翻译：创造仿生表面的方法
公开(公告)号：US5939208A
公开(公告)日：1999-08-17
申请号：US966343
申请日：1997-11-07
申请人： Patrick Stoy
发明人： Patrick Stoy
IPC分类号： A61L29/08 , A61L29/16 , A61L31/08 , A61L31/16 , C08J7/12 , B32B27/30 , B05D3/10
CPC分类号： C08J7/12 , A61L29/08 , A61L29/16 , A61L31/08 , A61L31/16 , A61L2300/208 , A61L2300/404 , A61L2400/18 , C08J2333/04 , Y10T428/31573 , Y10T428/31583 , Y10T428/31855
摘要： In the present invention method, the surface of articles made of acrylic polymers and methacrylic polymers are converted into thin biomimetic layers by using the process involving at least the following two steps:(a) The polymer surface is contacted, in the presence of water and for a predetermined reaction time necessary to form a continuous surface layer thinner than about 500 microns, with a solution containing one or more tetraalkylammonium hydroxides of the general formula:R.sub.1 R.sub.2 R.sub.3 R.sub.4 N.sup.+ OH.sup.-where R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the alkyl substituents, in which the sum of the number of carbon atoms is equal to or larger than 8 but smaller than 45; and,(b) The article is removed from the aqueous reaction solution and excess of tetraalkylammonium hydroxide is removed from the polymer surface by washing the polymer with a liquid miscible with the tetraalkylammonium hydroxide.
摘要翻译：在本发明的方法中，由丙烯酸类聚合物和甲基丙烯酸类聚合物制成的制品的表面通过使用涉及至少以下两个步骤的方法转化成薄的仿生层：（a）聚合物表面在水和对于形成薄于约500微米的连续表面层所需的预定反应时间，用含有一种或多种通式为R 1 R 2 R 3 R 4 N + OH的四烷基氢氧化铵的溶液，其中R 1，R 2，R 3，R 4为烷基取代基，其中碳原子数之和等于或大于8但小于45; 和（b）通过用与四烷基氢氧化铵混溶的液体洗涤聚合物，从反应溶液中除去物品并从聚合物表面除去过量的四烷基氢氧化铵。

9. 发明授权

US5688855A Thin film hydrophilic coatings 失效
标题翻译：薄膜亲水涂层
公开(公告)号：US5688855A
公开(公告)日：1997-11-18
申请号：US434573
申请日：1995-05-01
申请人： Vladimir A. Stoy , Gerald A. Gontarz, Jr. , Patrick Stoy
发明人： Vladimir A. Stoy , Gerald A. Gontarz, Jr. , Patrick Stoy
IPC分类号： A61L29/08 , A61L31/10 , C08G18/48 , C08G18/66 , C08G18/78 , C08G18/80 , C09D5/00 , C09D121/02 , C09D175/04 , C08K5/15 , C08K5/02 , C08K5/06 , C08K5/07
CPC分类号： C09D121/02 , A61L29/085 , A61L31/10 , C08G18/4833 , C08G18/6674 , C08G18/7825 , C08G18/8038 , C09D175/04 , C09D5/00 , C08G2210/00
摘要： A hydrophilic coating composition used to impart increased lubricity and wettability to the surface of a hydrophobic substrate which is comprised of three essential components: 1) Hydrogel-forming polymer component A 2) Water-soluble polymer component B 3) Common solvent C for the components A and B The water-insoluble, hydrogel-forming component A consists of a segmented copolymer with long, hydrophilic terminal blocks and the essentially hydrophobic central section. The two polymer components A and B have a limited miscibility in the absence of a common solvent C. Therefore, their blend tends to separate spontaneously into two polymer phases. The phase separation takes place during the solvent evaporation or extraction. A gradient of hydrophilicity and swelling within the coating layer is thus spontaneously created achieving a good adhesion to the substrate and high surface hydrophilicity at the same time.
摘要翻译：一种亲水性涂料组合物，其用于赋予疏水性基材表面增加的润滑性和润湿性，该疏水性基材由三种基本组分组成：1）水凝胶形成聚合物组分A 2）水溶性聚合物组分B 3）组分的常用溶剂C A和B水不溶性水凝胶形成组分A由具有长亲水性末端嵌段和基本上疏水性中心部分的分段共聚物组成。两种聚合物组分A和B在不存在共同溶剂C的情况下具有有限的混溶性。因此，它们的共混物倾向于自发分离成两个聚合物相。在溶剂蒸发或萃取过程中发生相分离。因此，自发产生涂层内的亲水性和溶胀的梯度，同时实现对基材的良好的粘合性和高的表面亲水性。

10. 发明申请

US20120157482A1 COMPOUNDS AND METHODS 审中-公开
标题翻译：化合物和方法
公开(公告)号：US20120157482A1
公开(公告)日：2012-06-21
申请号：US13392904
申请日：2010-08-25
申请人： Alan Peterson Graves, III , Lara S. Kallander , Patrick Stoy
发明人： Alan Peterson Graves, III , Lara S. Kallander , Patrick Stoy
IPC分类号： A61K31/505 , C12N9/99 , A61P9/04 , C07D239/47
CPC分类号： C07D239/47
摘要： Disclosed are compounds having the formula: wherein R1 and R2 are as defined herein, and methods of making and using the same.
摘要翻译：公开了具有下式的化合物：其中R1和R2如本文所定义，以及制备和使用它们的方法。

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