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：US20100144778A1

公开(公告)日：2010-06-10

申请号：US11922629

申请日：2006-06-26

申请人： Subharekha Raghavan ,  Steven L. Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James R. Tata ,  Ashley Rouse Lins ,  Abigail Lee Smenton ,  Weichun Chen ,  Darby Rye Schmidt ,  George Scott Tria

发明人： Subharekha Raghavan ,  Steven L. Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James R. Tata ,  Ashley Rouse Lins ,  Abigail Lee Smenton ,  Weichun Chen ,  Darby Rye Schmidt ,  George Scott Tria

IPC分类号： A61K31/437 ,  C07C233/02 ,  C07C229/38 ,  C07D413/04 ,  C07D513/04 ,  C07D471/14 ,  A61K31/165 ,  A61K31/192 ,  A61K31/4439 ,  A61K31/4245 ,  A61P9/10

CPC分类号： C07D261/20 ,  C07C233/52 ,  C07C233/55 ,  C07C235/36 ,  C07C237/20 ,  C07C2601/10 ,  C07C2601/16 ,  C07D231/12 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D271/06 ,  C07D277/30 ,  C07D307/79 ,  C07D309/14 ,  C07D309/28 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D513/04

摘要： The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明包括可用于治疗动脉粥样硬化，血脂异常等的式（I）化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。

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：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：US08168649B2

公开(公告)日：2012-05-01

申请号：US11922629

申请日：2006-06-26

申请人： Subharekha Raghavan ,  Steven L. Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James R. Tata ,  Ashley Rouse Lins ,  Abigail Lee Smenton ,  Weichun Chen ,  Darby Rye Schmidt ,  George Scott Tria

发明人： Subharekha Raghavan ,  Steven L. Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James R. Tata ,  Ashley Rouse Lins ,  Abigail Lee Smenton ,  Weichun Chen ,  Darby Rye Schmidt ,  George Scott Tria

IPC分类号： A61K31/44 ,  A01N43/40 ,  A61K31/19 ,  A61K31/165

CPC分类号： C07D261/20 ,  C07C233/52 ,  C07C233/55 ,  C07C235/36 ,  C07C237/20 ,  C07C2601/10 ,  C07C2601/16 ,  C07D231/12 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D271/06 ,  C07D277/30 ,  C07D307/79 ,  C07D309/14 ,  C07D309/28 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D513/04

摘要： The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明包括可用于治疗动脉粥样硬化，血脂异常等的式（I）化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。

公开(公告)号：US06589962B1

公开(公告)日：2003-07-08

申请号：US10031513

申请日：2002-04-16

申请人： James R Tata ,  Zhijian Lu ,  Subharekha Raghavan ,  Tracy T. Huening ,  Thomas A. Rano ,  Mark G. Charest

发明人： James R Tata ,  Zhijian Lu ,  Subharekha Raghavan ,  Tracy T. Huening ,  Thomas A. Rano ,  Mark G. Charest

IPC分类号： A01N4316

CPC分类号： C07D405/12 ,  A61K45/06 ,  C07D207/16 ,  C07D277/06 ,  C07D311/68 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04

摘要： Certain &agr;-hydroxy-&ggr;-[[(carbocyclic- or heterocyclic-substituted)amino]carbonyl]alkanamide derivatives are described as inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

摘要翻译： 某些α-羟基-γ - [[（碳环或杂环取代的）氨基]羰基]烷酰胺衍生物被描述为HIV蛋白酶抑制剂和HIV复制抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。 这些化合物对HIV病毒突变体有效，其对目前用于治疗AIDS和HIV感染的HIV蛋白酶抑制剂具有抗性。

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：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：US20090062269A1

公开(公告)日：2009-03-05

申请号：US12223492

申请日：2007-02-02

申请人： Subharekha Raghavan ,  Darby Rye Schmidt ,  Steven L. Colletti ,  Abigail Lee Smenton

发明人： Subharekha Raghavan ,  Darby Rye Schmidt ,  Steven L. Colletti ,  Abigail Lee Smenton

IPC分类号： A61K31/195 ,  C07D277/30 ,  C07C229/46 ,  C07D211/78 ,  C07D213/61 ,  C07D213/56 ,  A61K31/444 ,  A61K31/4418 ,  A61K31/381 ,  A61K31/538 ,  A61K31/4375 ,  A61K31/404 ,  A61K31/437 ,  A61P3/10 ,  A61K31/426 ,  A61K31/4439 ,  C07D413/14 ,  C07D403/04 ,  C07D401/04 ,  C07D333/24 ,  A61P3/00

CPC分类号： C07C235/34 ,  C07C233/52 ,  C07C2601/16 ,  C07D211/78 ,  C07D213/55 ,  C07D213/61 ,  C07D277/30 ,  C07D333/24 ,  C07D401/04 ,  C07D413/04

摘要： The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.