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公开(公告)号:US08450308B2
公开(公告)日:2013-05-28
申请号:US13059879
申请日:2009-08-14
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: C07D311/94 , C07D239/00 , C07D487/10 , C07D279/04 , A61K31/547 , A61K31/4166 , A61K31/4168 , A61K31/4178 , A61K31/438 , A61K31/505
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。
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公开(公告)号:US20130053377A1
公开(公告)日:2013-02-28
申请号:US13575679
申请日:2011-02-23
申请人: Lawrence W. Dillard , Jing Yuan , Katerina Leftheris , Shankar Venkatraman , Guosheng Wu , Lanqi Jia , Zhenrong Xu , Salvacion Cacatian , Angel Morales-Ramos , Suresh Singh , Yajun Zheng
发明人: Lawrence W. Dillard , Jing Yuan , Katerina Leftheris , Shankar Venkatraman , Guosheng Wu , Lanqi Jia , Zhenrong Xu , Salvacion Cacatian , Angel Morales-Ramos , Suresh Singh , Yajun Zheng
IPC分类号: A61K31/5395 , C07D487/04 , A61K31/519 , C07D471/04 , A61K31/437 , C07D209/54 , A61K31/4035 , C07D401/10 , A61K31/4439 , C07D491/107 , C07D513/04 , A61K31/429 , A61P25/28 , A61P27/06 , C07D498/04
CPC分类号: C07D513/04 , C07D209/54 , C07D209/96 , C07D401/04 , C07D471/04 , C07D487/04 , C07D491/10 , C07D491/107 , C07D498/04
摘要: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
摘要翻译: 本发明涉及由结构式(I)表示的化合物或其药学上可接受的盐。 变量的定义在这里提供。
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公开(公告)号:US20110218192A1
公开(公告)日:2011-09-08
申请号:US13059879
申请日:2009-08-14
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: A61K31/547 , C07D487/10 , C07D221/00 , C07D279/04 , C07D239/00 , A61K31/4166 , A61K31/438 , A61K31/505 , A61P25/00 , A61P25/28 , A61P27/06
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。
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公开(公告)号:US08889703B2
公开(公告)日:2014-11-18
申请号:US13575679
申请日:2011-02-23
申请人: Lawrence W. Dillard , Jing Yuan , Katerina Leftheris , Shankar Venkatraman , Guosheng Wu , Lanqi Jia , Zhenrong Xu , Salvacion Cacatian , Angel Morales-Ramos , Suresh Singh , Yajun Zheng
发明人: Lawrence W. Dillard , Jing Yuan , Katerina Leftheris , Shankar Venkatraman , Guosheng Wu , Lanqi Jia , Zhenrong Xu , Salvacion Cacatian , Angel Morales-Ramos , Suresh Singh , Yajun Zheng
IPC分类号: C07D487/04 , A61K31/5395 , C07D471/04 , A61K31/519 , C07D401/10
CPC分类号: C07D513/04 , C07D209/54 , C07D209/96 , C07D401/04 , C07D471/04 , C07D487/04 , C07D491/10 , C07D491/107 , C07D498/04
摘要: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
摘要翻译: 本发明涉及由结构式(I)表示的化合物或其药学上可接受的盐。 变量的定义在这里提供。
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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。
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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。
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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。
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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: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: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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