公开(公告)号：US20090275581A1

公开(公告)日：2009-11-05

申请号：US12225987

申请日：2007-04-05

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 ,  Lara S. Kallander ,  Colin A. Leach ,  Brian Lawhorn ,  Qing Lu ,  Lamont R. Terrell ,  Bahman Ghavini-Alagha ,  Jing Zhang ,  Damiano Ghirlanda ,  Xiaoping Hou ,  Simon Semus

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 ,  Lara S. Kallander ,  Colin A. Leach ,  Brian Lawhorn ,  Qing Lu ,  Lamont R. Terrell ,  Bahman Ghavini-Alagha ,  Jing Zhang ,  Damiano Ghirlanda ,  Xiaoping Hou ,  Simon Semus

IPC分类号： A61K31/5377 ,  C07D207/14 ,  A61K31/40 ,  C07D211/32 ,  A61K31/445 ,  A61K31/4545 ,  C07D401/10 ,  C07D413/06 ,  A61P9/12

CPC分类号： C07D211/22 ,  C07D265/30 ,  C07D401/06

摘要： Disclosed are compounds according to Formula I: wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity.Also described herein are methods of antagonizing aspartic protease inhibitors in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound according to Formula I.

摘要翻译： 公开了根据式I的化合物：其中变量在本文中定义。 这些化合物可以结合天冬氨酸蛋白酶以抑制其活性。 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。 本文还描述了在有需要的受试者中拮抗天冬氨酸蛋白酶抑制剂的方法，包括向受试者施用治疗有效量的根据式I的化合物。

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。

公开(公告)号：US20100317697A1

公开(公告)日：2010-12-16

申请号：US12665217

申请日：2008-06-20

申请人： John 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 ,  Qing Lu ,  Gerard McGeehan ,  Beth A. Knapp-Reid ,  Simon Semus ,  Robert D. Simpson ,  Suresh B. Singh ,  Lamont R. Terrell ,  Colin Tice ,  Tritin Tran ,  Zherong Xu ,  Jing Yuan ,  Wei Zhao ,  Yongdong Y. Zhao

发明人： John 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 ,  Qing Lu ,  Gerard McGeehan ,  Beth A. Knapp-Reid ,  Simon Semus ,  Robert D. Simpson ,  Suresh B. Singh ,  Lamont R. Terrell ,  Colin Tice ,  Tritin Tran ,  Zherong Xu ,  Jing Yuan ,  Wei Zhao ,  Yongdong Y. Zhao

IPC分类号： A61K31/445 ,  C07D211/06

CPC分类号： C07D211/22 ,  C07D265/30

摘要： Disclosed are compounds having the formula (I): wherein the R1, R2, R3, X, Y, A, L, 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： 公开了具有式（I）的化合物：其中R1，R2，R3，X，Y，A，L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。

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。

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。

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。

公开(公告)号：US07872028B2

公开(公告)日：2011-01-18

申请号：US12225985

申请日：2007-04-05

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： C07D211/22 ,  A61K31/445

CPC分类号： C07D211/22 ,  C07D207/08 ,  C07D265/30 ,  C07D413/12

摘要： Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated. levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.

摘要翻译： 描述其二氨基丙醇是口服活性的并且结合肾素以抑制其活性。 它们可用于治疗或改善与升高相关的疾病。 肾素活性水平或治疗天冬氨酸蛋白酶介导的病症。 还描述了在有需要的受试者中使用二氨基丙醇来改善或治疗肾素相关疾病的方法。

公开(公告)号：US20100190829A1

公开(公告)日：2010-07-29

申请号：US12665198

申请日：2008-06-20

申请人： John J. Baldwin ,  Salvacion Cacatian ,  David A. Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Alexey V. Ishchenko ,  Lanqi Jia ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Colin M. Tice ,  Zhenrong Xu ,  Jing Yuan ,  Wei Zhao

发明人： John J. Baldwin ,  Salvacion Cacatian ,  David A. Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Alexey V. Ishchenko ,  Lanqi Jia ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Colin M. Tice ,  Zhenrong Xu ,  Jing Yuan ,  Wei Zhao

IPC分类号： A61K31/445 ,  C07D211/56 ,  C07C271/20 ,  A61K31/27 ,  A61P9/12 ,  A61P9/04 ,  A61P27/06 ,  A61P5/46 ,  A61P25/22

CPC分类号： C07D211/60 ,  C07C271/20 ,  C07C2601/14 ,  C07D309/04

摘要： Described are compounds that 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。

公开(公告)号：US20100160424A1

公开(公告)日：2010-06-24

申请号：US12665213

申请日：2008-06-20

申请人： John J. Baldwin ,  Salvacion Cacatian ,  David A. Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Alexey V. Ishchenko ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Colin M. Tice ,  Zhenrong Xu ,  Jing yuan ,  Wei Zhao

发明人： John J. Baldwin ,  Salvacion Cacatian ,  David A. Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Alexey V. Ishchenko ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Colin M. Tice ,  Zhenrong Xu ,  Jing yuan ,  Wei Zhao

IPC分类号： A61K31/335 ,  C07D309/04 ,  C07C271/10 ,  C07D313/04 ,  A61K31/351 ,  A61K31/24 ,  A61P9/10

CPC分类号： C07C271/16 ,  C07C2601/14 ,  C07D309/04 ,  C07D313/04

摘要： Described are compounds that 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.

公开(公告)号：US20120225906A1

公开(公告)日：2012-09-06

申请号：US13469562

申请日：2012-05-11

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： A61K31/453 ,  A61P3/04 ,  A61P9/12 ,  A61P9/04 ,  A61P9/00 ,  A61P25/28 ,  A61P25/00 ,  A61P27/02 ,  A61P27/06 ,  A61P5/42 ,  A61P25/22 ,  A61P13/12 ,  A61P9/10

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: 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。