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：US08106221B2

公开(公告)日：2012-01-31

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. Flaherty ,  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. Flaherty ,  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： C07D325/00 ,  C07D315/00 ,  C07D493/00 ,  C07C275/04 ,  A61K31/351 ,  A61K31/17 ,  A01N47/28

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。

公开(公告)号：US08084485B2

公开(公告)日：2011-12-27

申请号：US12225756

申请日：2007-03-30

申请人： John J. Baldwin ,  David A. Claremon ,  Lawrence W. Dillard ,  Alexey V. Ishchenko ,  Jing Yuan ,  Zhenrong Xu ,  Gerard McGeehan ,  Wenguang Zeng

发明人： John J. Baldwin ,  David A. Claremon ,  Lawrence W. Dillard ,  Alexey V. Ishchenko ,  Jing Yuan ,  Zhenrong Xu ,  Gerard McGeehan ,  Wenguang Zeng

IPC分类号： A61K31/416 ,  C07D231/56

CPC分类号： C07D231/56

摘要： 6-(Aminoalkyl)indazoles of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, and renal, cardiac and vascular protecting medicinally active ingredients.

摘要翻译： 式（I）的6-（氨基烷基）吲唑及其盐具有肾素抑制性质，可用作抗高血压药和肾，心脏和血管保护的药物活性成分。

公开(公告)号：US20110105506A1

公开(公告)日：2011-05-05

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： A61K31/5375 ,  C07D211/22 ,  C07D417/04 ,  C07D405/10 ,  C07D211/60 ,  A61K31/451 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4525 ,  C07D265/30

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 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： 已经发现式I的二氨基烷烃是口服活性的并且结合天冬氨酸蛋白酶以抑制它们的活性。 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：US07754737B2

公开(公告)日：2010-07-13

申请号：US11664558

申请日：2005-10-07

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 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： 现已发现式I的二氨基烷烃是口服活性的并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：US20100168243A1

公开(公告)日：2010-07-01

申请号：US12665222

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. Ishehenko ,  Lanqi Jia ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Colin M. Tice ,  Zhenrong Xu ,  Jing Yuan ,  Wei Zhao ,  Linghang Zhuang ,  Jing Zhang

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

IPC分类号： A61K31/166 ,  C07C237/24 ,  A61K31/165 ,  C07C237/32 ,  A61P9/00 ,  A61P7/10 ,  A61P5/40 ,  A61P9/12

CPC分类号： C07C237/24 ,  C07C237/32 ,  C07C2601/08

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.

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：US20090264428A1

公开(公告)日：2009-10-22

申请号：US12225993

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

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

IPC分类号： A61K31/5377 ,  C07D211/32 ,  A61K31/445 ,  A61K31/4523 ,  C07D401/06 ,  C07D413/10 ,  A61P3/10

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

摘要： Described are compounds of the formula (I) 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 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： 描述了具有口服活性并结合天冬氨酸蛋白酶抑制其活性的式（I）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：US20090018103A1

公开(公告)日：2009-01-15

申请号：US11664558

申请日：2005-10-07

申请人： John J. Baldwin ,  David A. Claremon ,  Colin M. Tice ,  Salvacion Cacatian ,  Lawrence W. Dillar ,  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. Dillar ,  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： A61K31/695 ,  C07D211/00 ,  A61K31/445 ,  A61K31/27 ,  C07C233/00 ,  A61K31/164 ,  A61K31/5375 ,  A61P9/00 ,  A61P9/04 ,  A61P25/00 ,  A61P9/12 ,  A61K31/4545 ,  C07D295/00 ,  C07C63/00 ,  A61K31/4436 ,  C07C271/06 ,  C07F7/02

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 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： 现已发现式I的二氨基烷烃是口服活性的并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。