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公开(公告)号：US20110312967A1
公开(公告)日：2011-12-22
申请号：US13145152
申请日：2010-01-21
申请人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Jason L. Davis , Shuangyi Wan
发明人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Jason L. Davis , Shuangyi Wan
IPC分类号： A61K31/501 , C07D417/12 , C07D263/44 , C07D417/04 , A61P3/10 , A61K31/426 , A61K31/421 , A61K31/427 , A61K31/4439 , C07D277/34 , C07D417/14
CPC分类号： C07D417/14 , C07D263/44 , C07D277/34 , C07D417/04 , C07D417/12
摘要： This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译： 本发明提供了一些具有式G-L-A I的桥连和稠合化合物或其药学上可接受的盐，其溶剂合物的酯，其中：A是：（I），其它变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。 本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。
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公开(公告)号：US20110313008A1
公开(公告)日：2011-12-22
申请号：US13145025
申请日：2010-01-21
申请人： Hubert B. Josien , John W. Clader , Andrew Stamford , William J. Greenlee , Michael John Mayer , Jason L. Davis , Ming Min Hsia , Shuangyi Wan
发明人： Hubert B. Josien , John W. Clader , Andrew Stamford , William J. Greenlee , Michael John Mayer , Jason L. Davis , Ming Min Hsia , Shuangyi Wan
IPC分类号： A61K31/426 , A61P3/10 , A61P3/00 , C07D277/04
CPC分类号： C07D417/04 , C07D277/34
摘要： This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译： 本发明提供了具有下式的某些五氟丁烷化合物或其药学上可接受的盐，酯，溶剂合物或前药，其中变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。 本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。
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公开(公告)号：US20110312995A1
公开(公告)日：2011-12-22
申请号：US13145359
申请日：2010-01-21
申请人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Robert Jason Herr , Jason L. Davis , Kai Deng , Ming Min Hsia , Shuangyi Wan
发明人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Robert Jason Herr , Jason L. Davis , Kai Deng , Ming Min Hsia , Shuangyi Wan
IPC分类号： A61K31/4545 , C07D417/14 , C07D417/12 , A61K31/4709 , A61P3/00 , A61K31/4439 , A61P5/48 , A61P3/10 , A61P3/04 , A61P3/06 , C07D401/14 , A61K31/454
CPC分类号： C07D417/12 , C07D215/233 , C07D417/14
摘要： This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译： 本发明提供了一些式（I）的桥连和稠合杂环化合物或其药学上可接受的盐，酯溶剂合物或前药，其中：L是：（II），其它变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。 本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。
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公开(公告)号：US20110257156A1
公开(公告)日：2011-10-20
申请号：US13126056
申请日：2009-11-05
申请人： Zhaoning Zhu , William J. Greenlee , David James Cole , Dmitri A. Pissarnitski , Gioconda V. Gallo , Hongmei Li , Hubert B. Josien , Jun Qin , Chad E. Knutson , Mihirbaran Mandal , Monica L. Vicarel , Murali Rajagopalan , Pawan Kumar Dhondi , Ruo Xu , Zhong-Yue Sun , Thomas A. Bara , Xianhai Huang , Xiaohong Zhu , Zhiqiang Zhao , John W. Clader , Anandan Palani , Theodros Asberom , Troy McCracken , Chad E. Bennett
发明人： Zhaoning Zhu , William J. Greenlee , David James Cole , Dmitri A. Pissarnitski , Gioconda V. Gallo , Hongmei Li , Hubert B. Josien , Jun Qin , Chad E. Knutson , Mihirbaran Mandal , Monica L. Vicarel , Murali Rajagopalan , Pawan Kumar Dhondi , Ruo Xu , Zhong-Yue Sun , Thomas A. Bara , Xianhai Huang , Xiaohong Zhu , Zhiqiang Zhao , John W. Clader , Anandan Palani , Theodros Asberom , Troy McCracken , Chad E. Bennett
IPC分类号： A61K31/55 , A61K31/5383 , A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/438 , A61K31/437 , C07D413/10 , C07D498/20 , C07D498/04 , A61P25/00 , A61P25/28 , A61K31/4245 , A61K31/5386
CPC分类号： C07D471/04 , C07D413/10 , C07D498/04 , C07D498/20 , C07F7/0812
摘要： In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了新颖的杂环化合物作为γ-分泌酶的调节剂，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及治疗方法， 使用这种化合物或药物组合物预防，抑制或改善与中枢神经系统相关的一种或多种疾病。
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公开(公告)号：US08487099B2
公开(公告)日：2013-07-16
申请号：US12739315
申请日：2008-11-03
IPC分类号： C07D487/10 , C07D487/20 , C07D493/10 , C07D493/20 , C07D493/22 , C07F7/08 , C07F9/6571 , A61K31/397 , A61K31/4245 , A61K31/438 , A61P25/28
CPC分类号： C07D498/10 , C07D487/10 , C07D487/20 , C07D493/20 , C07D495/20 , C07D498/20 , C07D498/22 , C07F7/0812 , C07F9/657181
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 化合物具有式（I）。 还公开了使用式（I）化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。
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公开(公告)号：US20110009392A1
公开(公告)日：2011-01-13
申请号：US12671806
申请日：2008-08-04
申请人： Zhaoning Zhu , William J. Greenlee , John P. Caldwell , Robert D. Mazzola, JR. , Brian McKittrick , Chad E. Bennett , Xianhai Huang , Hubert B. Josien , Duane A. Burnett
发明人： Zhaoning Zhu , William J. Greenlee , John P. Caldwell , Robert D. Mazzola, JR. , Brian McKittrick , Chad E. Bennett , Xianhai Huang , Hubert B. Josien , Duane A. Burnett
IPC分类号： A61K31/55 , C07D487/04 , C07D235/02 , C07D498/04 , C07D491/04 , A61K31/4188 , A61K31/519 , A61K31/535 , A61K31/4353 , A61K31/435 , A61K31/47 , A61K31/505 , A61K31/397 , A61K31/4406 , A61K38/16 , A61P25/28
CPC分类号： C07D487/04 , C07D217/24 , C07D498/04
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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公开(公告)号：US20110306593A1
公开(公告)日：2011-12-15
申请号：US13128316
申请日：2009-11-11
申请人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
发明人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
IPC分类号： A61K31/553 , C07D498/10 , C07D498/04 , A61P25/28 , C07D413/14 , C07D498/14 , A61K31/5395 , C07D498/20 , C07D413/10
CPC分类号： C07D498/04 , C07D409/14 , C07D413/10 , C07D498/14 , C07D498/20
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。
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公开(公告)号：US20120107328A1
公开(公告)日：2012-05-03
申请号：US12739315
申请日：2008-11-03
IPC分类号： A61K39/395 , C07D498/20 , C07F7/10 , C07F9/6574 , C07D498/22 , A61K31/438 , A61K31/5386 , A61K31/695 , A61K31/675 , A61K31/5395 , A61K31/53 , A61P29/00 , A61P25/28 , A61P27/06 , A61P25/00 , A61P9/00 , C07D498/10
CPC分类号： C07D498/10 , C07D487/10 , C07D487/20 , C07D493/20 , C07D495/20 , C07D498/20 , C07D498/22 , C07F7/0812 , C07F9/657181
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 化合物具有式（I）。 还公开了使用式（I）化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。
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公开(公告)号：US08809318B2
公开(公告)日：2014-08-19
申请号：US13128316
申请日：2009-11-11
申请人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
发明人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
IPC分类号： A61K31/553 , C07D498/04 , C07D498/14 , C07D498/20
CPC分类号： C07D498/04 , C07D409/14 , C07D413/10 , C07D498/14 , C07D498/20
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。
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公开(公告)号：US08426403B2
公开(公告)日：2013-04-23
申请号：US12601322
申请日：2008-05-28
申请人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Brian A. McKittrick , John W. Clader , Mark D. McBriar , Anandan Palani
发明人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Brian A. McKittrick , John W. Clader , Mark D. McBriar , Anandan Palani
IPC分类号： A61K31/5365 , A61K31/5395 , C07D498/04 , A61P25/28
CPC分类号： C07D498/04 , C07D403/10 , C07D471/04 , C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。
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