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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。
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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。
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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。
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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。
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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。
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公开(公告)号:US20090312369A1
公开(公告)日:2009-12-17
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: A61K31/453 , C07D405/12 , A61P9/10 , A61P9/12 , A61P9/04 , C07D315/00
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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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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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。
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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。
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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.
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