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。

公开(公告)号：US09365574B2

公开(公告)日：2016-06-14

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 ,  C07D519/00 ,  A61K31/519 ,  A61P29/00 ,  A61P9/12 ,  A61P3/10 ,  A61P9/10 ,  A61P11/06 ,  A61P15/10 ,  A61P9/04 ,  A61P13/12 ,  A61P1/16

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身体的环鸟苷酸（“cGMP”）的产生，并且通常适用于治疗和预防与受干扰的cGMP平衡相关的疾病 。 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。

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。

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。

公开(公告)号：US20160304537A1

公开(公告)日：2016-10-20

申请号：US15103148

申请日：2014-12-05

申请人： Xiaoqing HAN ,  Alan WHITEHEAD ,  Subharekha RAGHAVAN ,  Timothy A. CERNAK ,  Spencer DREHER ,  Jonathan GROEPER ,  Jian GUO ,  Yong ZHANG ,  MERCK SHARP & DOHME CORP.

发明人： Xiaoqing Han ,  Alan Whitehead ,  Subharekha Raghavan ,  Timothy A. Cernak ,  Spencer Dreher ,  Jonathan Groeper ,  Jian Guo ,  Yong Zhang

IPC分类号： C07D519/00 ,  A61K45/06 ,  A61K31/519

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06 ,  C07B2200/05 ,  A61K2300/00

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.

公开(公告)号：US20160304536A1

公开(公告)日：2016-10-20

申请号：US15103140

申请日：2014-12-05

申请人： Xiaoqing HAN ,  Alan WHITEHEAD ,  Subharekha RAGHAVAN ,  Jonathan GROEPER ,  Jian GUO ,  Yong ZHANG ,  MERCK SHARP & DOHME CORP.

发明人： Xiaoqing Han ,  Alan Whitehead ,  Subharekha Raghavan ,  Jonathan Groeper ,  Jian Guo ,  Yong Zhang

IPC分类号： C07D519/00 ,  A61K31/519 ,  A61K45/06

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06 ,  A61K2300/00

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化合物或其药学上可接受的盐能够调节身体产生环鸟苷酸（“cGMP”），并且通常适用于治疗和预防与受干扰的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I化合物的药物制剂 或其药学上可接受的盐。

公开(公告)号：US07625938B2

公开(公告)日：2009-12-01

申请号：US11632198

申请日：2005-07-19

申请人： Linda Brockunier ,  Jian Guo ,  Rui Liang ,  Emma R. Parmee ,  Subharekha Raghavan ,  George Scott Tria ,  Yusheng Xiong

发明人： Linda Brockunier ,  Jian Guo ,  Rui Liang ,  Emma R. Parmee ,  Subharekha Raghavan ,  George Scott Tria ,  Yusheng Xiong

IPC分类号： A61K31/502 ,  A61K31/4155 ,  C07D241/36 ,  C07D403/04

CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D407/04 ,  C07D413/04 ,  C07D417/04

摘要： The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.

摘要翻译： 本发明涉及取代的吡唑，含有这些化合物的组合物和处理方法。 该化合物是胰高血糖素受体拮抗剂，因此可用于治疗，预防或延缓2型糖尿病的发作。

公开(公告)号：US20080108620A1

公开(公告)日：2008-05-08

申请号：US11632198

申请日：2005-07-19

申请人： Linda Brockunier ,  Jian Guo ,  Rui Liang ,  Emma R. Parmee ,  Subharekha Raghavan ,  George Scott Tria ,  Yusheng Xiong

发明人： Linda Brockunier ,  Jian Guo ,  Rui Liang ,  Emma R. Parmee ,  Subharekha Raghavan ,  George Scott Tria ,  Yusheng Xiong

IPC分类号： A61K31/4155 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4709 ,  A61K31/498 ,  A61P3/10 ,  A61P9/10 ,  C07D401/04 ,  C07D403/04 ,  C07D405/02 ,  C07D413/04 ,  C07D417/04

CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D407/04 ,  C07D413/04 ,  C07D417/04

摘要： The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.

摘要翻译： 本发明涉及取代的吡唑，含有这些化合物的组合物和处理方法。 该化合物是胰高血糖素受体拮抗剂，因此可用于治疗，预防或延缓2型糖尿病的发作。

公开(公告)号：US09284301B2

公开(公告)日：2016-03-15

申请号：US13636760

申请日：2011-03-22

申请人： Darby Schmidt ,  Subharekha Raghavan ,  John Stelmach ,  Jian Guo ,  Jonathan Groeper ,  Linda Brockunier ,  Keith Rosauer ,  Hong Shen ,  Rui Liang ,  Fa-Xiang Ding

发明人： Darby Schmidt ,  Subharekha Raghavan ,  John Stelmach ,  Jian Guo ,  Jonathan Groeper ,  Linda Brockunier ,  Keith Rosauer ,  Hong Shen ,  Rui Liang ,  Fa-Xiang Ding

IPC分类号： C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds 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 compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.

摘要翻译： 本发明涉及具有式（I）结构的化合物及其药学上可接受的盐，它们是可溶性鸟苷酸环化酶活化剂。 这些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受干扰的cGMP平衡有关的疾病。 该化合物可用于治疗或预防心血管疾病，内皮功能障碍，舒张功能障碍，动脉粥样硬化，高血压，肺动脉高压，心绞痛，血栓形成，再狭窄，心肌梗死，中风，心功能不全，肺性高血压，勃起功能障碍，支气管哮喘，慢性 肾功能不全，糖尿病或肝硬化。

公开(公告)号：US20130012511A1

公开(公告)日：2013-01-10

申请号：US13636760

申请日：2011-03-22

申请人： Darby Schmidt ,  Subharekha Raghavan ,  John Stelmach ,  Jian Guo ,  Jonathan Groeper ,  Linda Brockunier ,  Keith Rosauer ,  Hong Shen ,  Rui Liang ,  Fa-Xiang Ding

发明人： Darby Schmidt ,  Subharekha Raghavan ,  John Stelmach ,  Jian Guo ,  Jonathan Groeper ,  Linda Brockunier ,  Keith Rosauer ,  Hong Shen ,  Rui Liang ,  Fa-Xiang Ding

IPC分类号： C07D403/14 ,  A61K31/506 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  A61K31/5377 ,  C07D417/14 ,  C07D403/04 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/04 ,  A61P7/02 ,  A61P11/00 ,  A61P15/00 ,  A61P11/06 ,  A61P13/12 ,  A61P3/10 ,  A61P1/16 ,  A61P9/08 ,  A61P7/10 ,  A61P3/00 ,  A61P3/06 ,  C07D487/04

CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds 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 compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.

摘要翻译： 本发明涉及具有式（I）结构的化合物及其药学上可接受的盐，它们是可溶性鸟苷酸环化酶活化剂。 这些化合物能够调节身体产生的环鸟苷酸（cGMP），通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 该化合物可用于治疗或预防心血管疾病，内皮功能障碍，舒张功能障碍，动脉粥样硬化，高血压，肺动脉高压，心绞痛，血栓形成，再狭窄，心肌梗死，中风，心功能不全，肺性高血压，勃起功能障碍，支气管哮喘，慢性 肾功能不全，糖尿病或肝硬化。