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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.
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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。
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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。
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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：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：US20100184805A1
公开(公告)日：2010-07-22
申请号：US12665208
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： A61K31/454 , C07D211/32 , C07D401/12 , C07D405/12 , A61K31/453 , A61K31/4545 , A61K31/445 , A61P43/00
CPC分类号： C07D211/16 , C07D401/12
摘要： Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds 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. The present invention is also directed to pharmaceutical compositions comprising a compound described herein or enantiomers, diastereomers, or salts thereof and a pharmaceutically acceptable carrier or excipient.
摘要翻译： 公开了由以下结构式表示的天冬氨酸蛋白酶抑制剂及其药学上可接受的盐。 这些化合物是口服活性的，并结合天冬氨酸蛋白酶抑制其活性。 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。 本发明还涉及包含本文所述化合物或其对映异构体，非对映体或其盐和药学上可接受的载体或赋形剂的药物组合物。
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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：US08580823B2
公开(公告)日：2013-11-12
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： A61K31/445
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：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。
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