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31. 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。

32. 发明申请

US20100144825A1 Renin Inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US20100144825A1
公开(公告)日：2010-06-10
申请号：US12665219
申请日：2008-06-20
申请人： John J. Baldwin , Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Patrick T. Fiaherty , Alexey V. Ishchenko , Lanqi Jia , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Jing Yuan , Wei Zhao , Linghang Zhuang
发明人： John J. Baldwin , Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Patrick T. Fiaherty , Alexey V. Ishchenko , Lanqi Jia , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Jing Yuan , Wei Zhao , Linghang Zhuang
IPC分类号： A61K31/4035 , C07C271/10 , C07D209/46 , A61K31/24 , A61P31/18
CPC分类号： C07C275/24 , C07C275/14 , C07C275/16 , C07C2601/14 , C07C2603/74 , C07D209/46 , C07D309/04 , C07D311/96 , C07D313/04
摘要： The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
摘要翻译：本发明涉及天冬氨酸蛋白酶抑制剂。本发明还涉及包含所公开的天冬氨酸蛋白酶抑制剂的药物组合物。本发明还涉及在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用所公开的天冬氨酸蛋白酶抑制剂治疗受试者中天冬氨酸蛋白酶介导的病症的方法。

33. 发明申请

US20100130471A1 Renin Inhibitors 审中-公开
标题翻译：肾素抑制剂
公开(公告)号：US20100130471A1
公开(公告)日：2010-05-27
申请号：US12450619
申请日：2008-04-04
申请人： John J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiamo Ghirlanda , Xiaoping Hou , Alexey V. Ishebenko , Lara S. Kallander , Beth A. Knapp-Reed , Brian Lawhorn , Qing Lu , Gerard McGeehan , Simon Semus , Robert D. Simpson , Suresh B. Singh , Lamont R. Terrell , Colin Tice , Tritin Tran , Zhenrong Xu , Jing Yuan , Jing Zhang , Wei Zhao
发明人： John J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiamo Ghirlanda , Xiaoping Hou , Alexey V. Ishebenko , Lara S. Kallander , Beth A. Knapp-Reed , Brian Lawhorn , Qing Lu , Gerard McGeehan , Simon Semus , Robert D. Simpson , Suresh B. Singh , Lamont R. Terrell , Colin Tice , Tritin Tran , Zhenrong Xu , Jing Yuan , Jing Zhang , Wei Zhao
IPC分类号： A61K31/445 , A61K31/554 , A61K31/55 , A61K31/551 , A61K31/549 , A61K31/5377 , A61K31/5375 , A61K31/4545 , C07D417/12 , C07D265/30 , C07D401/06 , C07D401/10 , C07D211/34 , A61P25/00 , A61P9/12 , A61P9/10
CPC分类号： C07D401/06 , C07D211/22 , C07D265/30
摘要： Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译：描述了结合天冬氨酸蛋白酶抑制其活性的化合物。它们可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。还描述了本文所述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。

34. 发明申请

US20090318501A1 Piperidine derivatives as renin inhibitors 审中-公开
标题翻译：哌啶衍生物作为肾素抑制剂
公开(公告)号：US20090318501A1
公开(公告)日：2009-12-24
申请号：US12311020
申请日：2007-09-17
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Patrick T. Flaherty
IPC分类号： A61K31/445 , C07D405/12 , C07D315/00
CPC分类号： C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula; or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.
摘要翻译：本发明涉及由以下结构式表示的天冬氨酸蛋白酶抑制剂; 或其药学上可接受的盐。本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。还公开了在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。

35. 发明授权

US6001579A Supports and combinatorial chemical libraries thereof encoded by non-sequencable tags 失效
标题翻译：由非可序列标签编码的支持体和组合化学文库
公开(公告)号：US6001579A
公开(公告)日：1999-12-14
申请号：US485018
申请日：1995-06-07
申请人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
发明人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
IPC分类号： C07D243/16 , G01N33/53 , G01N33/543 , G01N33/546 , G01N33/566 , G01N33/58
CPC分类号： C07D243/28 , C07D491/048 , C40B40/04 , C40B50/16 , C40B70/00 , G01N33/54313 , G01N33/54353 , C07B2200/11
摘要： Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
摘要翻译：提供了编码的组合化学，其中使用有机分子记录顺序合成方案，其定义了反应物的选择和阶段，作为相同或不同的信息位。可以在多级合成中产生各种产物，例如低聚物和合成的非重复有机分子。方便地，化合物的嵌套族可以用作标识符，其中取代基的数目和/或位置定义了选择。或者，可以使用可检测的官能团，例如放射性同位素，荧光剂，卤素等，其中两个不同基团的存在和比例可用于限定阶段或选择。特别地，可以使用多个标识符来提供二进制或更高代码，以便仅限定几个可拆卸标签来定义多个选择。可以筛选颗粒以获得感兴趣的特征，特别是结合亲和力，其中产物可以与颗粒分离或保留在颗粒上。对特征呈阳性的颗粒的反应历程可以通过标签的释放和分析来确定以确定颗粒的反应历程。

36. 发明授权

US08921359B2 Inhibitors of beta-secretase 有权
标题翻译： β-分泌酶抑制剂
公开(公告)号：US08921359B2
公开(公告)日：2014-12-30
申请号：US13867590
申请日：2013-04-22
申请人： Lawrence W. Dillard , Jing Yuan , Lanqi Jia , Yajun Zheng
发明人： Lawrence W. Dillard , Jing Yuan , Lanqi Jia , Yajun Zheng
IPC分类号： A61K31/54 , A61K31/415 , A61K31/44 , A61K31/41 , A61K31/4965 , A61K31/497 , A61K31/505 , C07D498/16 , C07D495/10 , C07D491/20 , C07D498/10 , C07D513/10 , C07D491/107 , C07D498/20
CPC分类号： C07D498/20 , C07D491/107 , C07D491/20 , C07D495/10 , C07D498/10 , C07D498/16 , C07D513/10
摘要： The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
摘要翻译：本发明涉及由以下结构式表示的化合物或其药学上可接受的盐。还描述了包含由结构式（I）表示的化合物和这些化合物用于抑制需要这种治疗的受试者中的BACE活性的方法的药物组合物。

37. 发明授权

US08633212B2 Inhibitors of beta-secretase 有权
标题翻译： β-分泌酶抑制剂
公开(公告)号：US08633212B2
公开(公告)日：2014-01-21
申请号：US12723137
申请日：2010-03-12
申请人： Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Klaus Fuchs , Niklas Heine , Lanqi Jia , Katerina Leftheris , Brian McKeever , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Guosheng Wu , Zhongren Wu , Zhenrong Xu , Jing Yuan , Yajun Zheng
发明人： Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Klaus Fuchs , Niklas Heine , Lanqi Jia , Katerina Leftheris , Brian McKeever , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Guosheng Wu , Zhongren Wu , Zhenrong Xu , Jing Yuan , Yajun Zheng
IPC分类号： A61K31/405 , A61K31/415 , A61K31/41 , A61K31/40 , C07D237/00 , C07D271/10 , C07D487/10 , C07D209/54
CPC分类号： C07D271/12 , C07D233/46 , C07D235/02 , C07D239/70 , C07D277/60 , C07D279/08 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/10 , C07D487/10 , C07D491/10 , C07D493/20 , C07D495/10 , C07D498/10 , C07D513/10
摘要： The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
摘要翻译：本发明涉及由以下结构式表示的化合物或其药学上可接受的盐。还描述了化合物的药物组合物和使用方法。

38. 发明申请

US20130317014A1 INHIBITORS OF BETA-SECRETASE 有权
标题翻译： BETA-SECRETASE的抑制剂
公开(公告)号：US20130317014A1
公开(公告)日：2013-11-28
申请号：US13867590
申请日：2013-04-22
申请人： Lawrence W. Dillard , Jing Yuan , Lanqi Jia , Yajun Zheng
发明人： Lawrence W. Dillard , Jing Yuan , Lanqi Jia , Yajun Zheng
IPC分类号： C07D498/20 , C07D513/10 , C07D498/10 , C07D495/10 , C07D491/107 , C07D491/20
CPC分类号： C07D498/20 , C07D491/107 , C07D491/20 , C07D495/10 , C07D498/10 , C07D498/16 , C07D513/10
摘要： The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
摘要翻译：本发明涉及由以下结构式表示的化合物或其药学上可接受的盐。还描述了包含由结构式（I）表示的化合物和这些化合物用于抑制需要这种治疗的受试者中的BACE活性的方法的药物组合物。

39. 发明授权

US08455521B2 Diaminoalkane aspartic protease inhibitors 失效
标题翻译：二氨基烷烃天冬氨酸蛋白酶抑制剂
公开(公告)号：US08455521B2
公开(公告)日：2013-06-04
申请号：US12802142
申请日：2010-05-28
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Patrick T. Flaherty , Jean-Pierre Wery
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Patrick T. Flaherty , Jean-Pierre Wery
IPC分类号： C07D417/04 , C07D409/06 , C07D405/06 , C07D401/06 , C07D417/06 , C07D265/30 , C07D211/22 , C07D211/26 , A61K31/5377 , A61K31/5375 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545
CPC分类号： C07D417/06 , C07C233/40 , C07C235/40 , C07C235/42 , C07C271/20 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D211/22 , C07D211/56 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/06 , C07F7/081 , C07F7/0812
摘要： Diaminoalkanes of below Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity: They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
摘要翻译：现已发现以下式I的二氨基烷烃是口服活性的并与天冬氨酸蛋白酶结合以抑制其活性：它们可用于治疗或改善与升高的天冬氨酸蛋白酶活性水平相关的疾病。本发明还涉及在有需要的受试者中使用式I化合物来改善或治疗天冬氨酸蛋白酶相关病症的方法，包括向所述受试者施用有效量的式I化合物。

40. 发明授权

US08198453B2 Piperidine renin inhibitors 失效
标题翻译：哌啶肾素抑制剂
公开(公告)号：US08198453B2
公开(公告)日：2012-06-12
申请号：US12311012
申请日：2007-09-18
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
IPC分类号： C07D405/12 , A61K31/453
CPC分类号： C07D309/04 , C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.
摘要翻译：本发明涉及由以下结构式（I）表示的天冬氨酸蛋白酶抑制剂或其药学上可接受的盐。本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。还公开了在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。

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