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公开(公告)号：US20130072492A1
公开(公告)日：2013-03-21
申请号：US13699046
申请日：2011-05-24
申请人： Subharekha Raghavan , John E. Stelmach , Cameron J. Smith , Hong Li , Alan Whitehead , Sherman T. Waddell , Yi-Heng Chen , Shouwu Miao , Olga A. Ornoski , Joie Garfunkle , Xibin Liao , Jiang Chang , Xiaoqing Han , Jian Guo , Jonathan A. Groeper , Linda L. Brockunier , Keith Rosauer , Emma R. Parmee
发明人： Subharekha Raghavan , John E. Stelmach , Cameron J. Smith , Hong Li , Alan Whitehead , Sherman T. Waddell , Yi-Heng Chen , Shouwu Miao , Olga A. Ornoski , Joie Garfunkle , Xibin Liao , Jiang Chang , Xiaoqing Han , Jian Guo , Jonathan A. Groeper , Linda L. Brockunier , Keith Rosauer , Emma R. Parmee
IPC分类号： C07D487/04 , C07D495/04 , A61K31/5025 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/04 , A61P7/02 , A61P15/00 , A61P11/06 , A61P13/12 , A61P3/10 , A61P1/16 , A61P9/08 , A61P3/00 , A61P3/06 , A61P7/10 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519 , C07D519/00
摘要： A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译： 式（I）的化合物或其药学上可接受的盐能够调节人体的环鸟苷酸（cGMP）的产生，并且通常适用于治疗和预防与扰动的cGMP平衡有关的疾病。 本发明还涉及用于制备式I化合物或其药学上可接受的盐的方法，用于治疗和预防上述疾病和用于制备用于该目的的药物以及包含式（III）化合物的药物制剂 I）或其药学上可接受的盐。
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2.发明申请公开(公告)号：US20110172256A1
公开(公告)日：2011-07-14
申请号：US13063820
申请日：2009-09-10
申请人： Songnian Lin , Christian P. Stevenson , Emma R. Parmee , Libo Xu , Xibin Liao , Edward metzger , Rui Liang , Fengqi Zhang , John E. Stelmach
发明人： Songnian Lin , Christian P. Stevenson , Emma R. Parmee , Libo Xu , Xibin Liao , Edward metzger , Rui Liang , Fengqi Zhang , John E. Stelmach
IPC分类号： A61K31/517 , C07D215/14 , A61K31/47 , A61P3/10 , C07D215/227 , C07D471/04 , A61K31/4375 , C07D239/74
CPC分类号： C07D215/18 , C07D215/227 , C07D217/22 , C07D217/24 , C07D239/70 , C07D403/04 , C07D413/04
摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
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3.发明申请Substituted Aryl and Heteroaryl Derivatives, Compositions Containing Such Compounds and Methods of Use 有权取代的芳基和杂芳基衍生物，含有这些化合物的组合物和使用方法公开(公告)号：US20080161347A1
公开(公告)日：2008-07-03
申请号：US11886136
申请日：2006-03-17
IPC分类号： A61K31/472 , C07D209/04 , C07D231/06 , A61K31/404 , A61P3/10 , A61P9/10 , A61K31/415 , C07D217/24
CPC分类号： C07C323/62 , C07C235/42 , C07C235/52 , C07C255/57 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07C2602/10 , C07D209/12 , C07D213/30 , C07D213/61 , C07D213/68 , C07D215/14 , C07D217/24 , C07D231/12 , C07D231/56 , C07D233/60 , C07D239/26 , C07D257/06
摘要： Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译： 公开了取代的芳基和杂芳基衍生物。 该化合物可用于治疗2型糖尿病及相关病症。 还包括药物组合物和治疗方法。
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公开(公告)号：US20110218202A1
公开(公告)日：2011-09-08
申请号：US13127334
申请日：2009-11-16
申请人： Linda L. Brockunier , Jian Guo , Emma R. Parmee , Subharekha Raghavan , Keith Rosauer , Darby Schmidt , John E. Stelmach
发明人： Linda L. Brockunier , Jian Guo , Emma R. Parmee , Subharekha Raghavan , Keith Rosauer , Darby Schmidt , John E. Stelmach
IPC分类号： A61K31/519 , C07D487/04 , C07D495/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/04 , A61P7/02 , A61P13/12 , A61P1/16 , A61P3/10
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： Compounds of Formula I are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the Formula I.
摘要翻译： 式I的化合物能够调节人体的环鸟苷酸（“cGMP”）的产生，并且通常适用于治疗和预防与扰乱的cGMP平衡相关的疾病。 本发明还涉及制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于该目的的药物以及包含式I化合物的药物制剂。
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5.发明申请GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE 有权GLUCAGON受体拮抗剂化合物，包含这些化合物的组合物和使用方法公开(公告)号：US20100144824A1
公开(公告)日：2010-06-10
申请号：US12702358
申请日：2010-02-09
申请人： JOHN E. STELMACH , EMMA R. PARMEE , JAMES R. TATA , KEITH G. ROSAUER , RONALD M. KIM , AMY R. BITTNER , JIANG CHANG , CHRISTOPHER JOSEPH SINZ
发明人： JOHN E. STELMACH , EMMA R. PARMEE , JAMES R. TATA , KEITH G. ROSAUER , RONALD M. KIM , AMY R. BITTNER , JIANG CHANG , CHRISTOPHER JOSEPH SINZ
IPC分类号： A61K31/404 , C07D209/18 , A61P3/04 , A61P9/10
CPC分类号： C07D209/18
摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译： 公开了胰高血糖素受体拮抗剂化合物。 该化合物可用于治疗2型糖尿病及相关病症。 还包括药物组合物和治疗方法。
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公开(公告)号：US08741910B2
公开(公告)日：2014-06-03
申请号：US13127334
申请日：2009-11-16
申请人： Linda L. Brockunier , Jian Guo , Emma R. Parmee , Subharekha Raghavan , Keith Rosauer , Darby Schmidt , John E. Stelmach
发明人： Linda L. Brockunier , Jian Guo , Emma R. Parmee , Subharekha Raghavan , Keith Rosauer , Darby Schmidt , John E. Stelmach
IPC分类号： A61K31/519 , C07D471/04 , C07D487/04 , A61P9/12 , A61P9/04
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： Compounds of Formula I are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the Formula I.
摘要翻译： 式I的化合物能够调节人体的环鸟苷酸（“cGMP”）的产生，并且通常适用于治疗和预防与扰乱的cGMP平衡相关的疾病。 本发明还涉及制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于该目的的药物以及包含式I化合物的药物制剂。
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公开(公告)号：US08445538B2
公开(公告)日：2013-05-21
申请号：US13140260
申请日：2009-12-09
申请人： Songnian Lin , Xibin Liao , Roman Kats-Kagan , John E. Stelmach , Emma R. Parmee
发明人： Songnian Lin , Xibin Liao , Roman Kats-Kagan , John E. Stelmach , Emma R. Parmee
IPC分类号： A61K31/165 , C07C237/22
CPC分类号： C07C233/83 , C07C235/42 , C07C255/57 , C07C309/15 , C07C317/44 , C07C323/62
摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译： 公开了胰高血糖素受体拮抗剂化合物。 该化合物可用于治疗2型糖尿病及相关病症。 还包括药物组合物和治疗方法。
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8.发明授权Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use 有权胰高血糖素受体拮抗剂化合物，含有这些化合物的组合物和使用方法公开(公告)号：US08436015B2
公开(公告)日：2013-05-07
申请号：US13063820
申请日：2009-09-10
申请人： Songnian Lin , Christian P. Stevenson , Emma R. Parmee , Libo Xu , Xibin Liao , Edward Metzger , Rui Liang , Fengqi Zhang , John E. Stelmach
发明人： Songnian Lin , Christian P. Stevenson , Emma R. Parmee , Libo Xu , Xibin Liao , Edward Metzger , Rui Liang , Fengqi Zhang , John E. Stelmach
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00
CPC分类号： C07D215/18 , C07D215/227 , C07D217/22 , C07D217/24 , C07D239/70 , C07D403/04 , C07D413/04
摘要： Glucagon receptor antagonist compounds of formula I are disclosed: The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译： 公开了式I的胰高血糖素受体拮抗剂化合物：该化合物可用于治疗2型糖尿病和相关病症。 还包括药物组合物和治疗方法。
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公开(公告)号：US10968210B2
公开(公告)日：2021-04-06
申请号：US16345913
申请日：2017-11-13
申请人： Merck Sharp & Dohme Corp. , Thomas J. Greshock , James Mulhearn , Anthony J. Roecker , Tianying Jian , Gang Zhou , Liangqin Guo , Walter Won , Ting Zhang , Rajan Anand , John E. Stelmach , Deping Wang , Ronald M. Kim , Mark E. Layton , Christopher S. Burgey , Philippe G. Nantermet
发明人： Thomas J. Greshock , James Mulhearn , Anthony J. Roecker , Tianying Jian , Gang Zhou , Liangqin Guo , Walter Won , Ting Zhang , Rajan Anand , John E. Stelmach , Deping Wang , Ronald M. Kim , Mark E. Layton , Christopher S. Burgey , Philippe G. Nantermet
IPC分类号： C07D417/12 , C07D417/14 , C07D277/52 , C07D471/04 , C07D487/10 , C07D401/12 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08
摘要： Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.
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公开(公告)号：US20110251248A1
公开(公告)日：2011-10-13
申请号：US13140260
申请日：2009-12-09
申请人： Songnian Lin , Xibin Liao , Roman Kats-Kagan , John E. Stelmach , Emma R. Parmee
发明人： Songnian Lin , Xibin Liao , Roman Kats-Kagan , John E. Stelmach , Emma R. Parmee
IPC分类号： A61K31/41 , A61K31/197 , C07C233/87 , A61K31/166 , A61P3/10 , C07C309/70 , A61K31/255 , C07C255/60 , A61K31/277 , C07C229/36 , C07D257/04
CPC分类号： C07C233/83 , C07C235/42 , C07C255/57 , C07C309/15 , C07C317/44 , C07C323/62
摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译： 公开了胰高血糖素受体拮抗剂化合物。 该化合物可用于治疗2型糖尿病及相关病症。 还包括药物组合物和治疗方法。
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