公开(公告)号：EP3079700B1

公开(公告)日：2020-11-25

申请号：EP14869616.4

申请日：2014-12-05

申请人： Merck Sharp & Dohme Corp.

发明人： HAN, Xiaoqing ,  WHITEHEAD, Alan ,  RAGHAVAN, Subharekha ,  CERNAK, Timothy, A. ,  DREHER, Spencer ,  GROEPER, Jonathan ,  GUO, Jian ,  ZHANG, Yong

IPC分类号： A61K31/519 ,  C07D519/00 ,  A61P9/00 ,  A61P7/02 ,  A61P13/12 ,  A61P3/10 ,  A61K45/06

公开(公告)号：EP3394067B1

公开(公告)日：2020-04-01

申请号：EP16823455.7

申请日：2016-12-20

申请人： Merck Sharp & Dohme Corp.

发明人： BERGER, Raphelle ,  CHEN, Yi-Heng ,  LI, Guoqing ,  GARFUNKLE, Joie ,  LI, Hong ,  MIAO, Shouwu ,  RAGHAVAN, Subharekha ,  SMITH, Cameron, J. ,  STELMACH, John ,  WHITEHEAD, Alan ,  ZHANG, Rui ,  ZHANG, Yong ,  FU, Jianmin ,  JI, Gang ,  JIANG, Falong

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61K31/519 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/04

公开(公告)号：EP2464228A1

公开(公告)日：2012-06-20

申请号：EP10808529.1

申请日：2010-08-03

申请人： Merck Sharp & Dohme Corp.

发明人： WOOD, Harold, B. ,  ADAMS, Alan, D. ,  SZEWCZYK, Jason, W. ,  ZHANG, Yong ,  YANG, Meng

IPC分类号： A01N43/40 ,  A61K31/445

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/14

摘要： Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.

公开(公告)号：EP3079701A1

公开(公告)日：2016-10-19

申请号：EP14870523.9

申请日：2014-12-05

申请人： Merck Sharp & Dohme Corp.

发明人： HAN, Xiaoqing ,  WHITEHEAD, Alan ,  RAGHAVAN, Subharekha ,  GROEPER, Jonathan ,  GUO, Jian ,  ZHANG, Yong

IPC分类号： A61K31/519 ,  A61K31/52 ,  C07D473/00

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单磷酸（“cGMP”），并且通常适用于治疗和预防与扰乱的cGMP平衡有关的疾病。 本发明还涉及制备式I化合物或其药学上可接受的盐用于治疗和预防上述疾病和制备用于该目的的药物的方法，以及包含式I化合物 或其药学上可接受的盐。

公开(公告)号：EP3079700A1

公开(公告)日：2016-10-19

申请号：EP14869616.4

申请日：2014-12-05

申请人： Merck Sharp & Dohme Corp.

发明人： HAN, Xiaoqing ,  WHITEHEAD, Alan ,  RAGHAVAN, Subharekha ,  CERNAK, Timothy, A. ,  DREHER, Spencer ,  GROEPER, Jonathan ,  GUO, Jian ,  ZHANG, Yong

IPC分类号： A61K31/519 ,  A61K31/52 ,  C07D473/00

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 pharmaceuticall 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单磷酸（“cGMP”），并且通常适用于治疗和预防与扰乱的cGMP平衡有关的疾病。 本发明还涉及制备式I化合物或其可药用盐用于治疗和预防上述疾病和制备用于此目的的药物的方法以及包含式I化合物 或其药学上可接受的盐。

公开(公告)号：EP3394067A1

公开(公告)日：2018-10-31

申请号：EP16823455.7

申请日：2016-12-20

申请人： Merck Sharp & Dohme Corp.

发明人： BERGER, Raphelle ,  CHEN, Yi-Heng ,  LI, Guoqing ,  GARFUNKLE, Joie ,  LI, Hong ,  MIAO, Shouwu ,  RAGHAVAN, Subharekha ,  SMITH, Cameron, J. ,  STELMACH, John ,  WHITEHEAD, Alan ,  ZHANG, Rui ,  ZHANG, Yong ,  FU, Jianmin ,  JI, Gang ,  JIANG, Falong

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/04

摘要： or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate 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 also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.

公开(公告)号：EP2464228B1

公开(公告)日：2017-12-06

申请号：EP10808529.1

申请日：2010-08-03

申请人： Merck Sharp & Dohme Corp.

发明人： WOOD, Harold, B. ,  ADAMS, Alan, D. ,  SZEWCZYK, Jason, W. ,  ZHANG, Yong ,  YANG, Meng

IPC分类号： A61K31/445 ,  A61P3/10 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/14

摘要： Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.

公开(公告)号：EP2571855B1

公开(公告)日：2014-12-24

申请号：EP11783980.3

申请日：2011-05-12

申请人： Merck Sharp & Dohme Corp.

发明人： DEBENHAM, John, S. ,  SHEN, Dong-Ming ,  GRAHAM, Thomas, H. ,  CLEMENTS, Matthew, J. ,  ZHANG, Yong

IPC分类号： C07D235/02

CPC分类号： C07C237/24 ,  A61K31/165 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/4453 ,  A61K31/5375 ,  A61K31/5377 ,  A61K45/06 ,  C07C271/24 ,  C07C2601/02 ,  C07C2601/14 ,  C07D205/04 ,  C07D213/40 ,  C07D213/61 ,  C07D213/64 ,  C07D213/85 ,  C07D233/56 ,  C07D233/61 ,  C07D239/26 ,  C07D241/12 ,  C07D295/15 ,  C07D295/155

公开(公告)号：EP1861382B1

公开(公告)日：2012-10-10

申请号：EP06736976.9

申请日：2006-03-03

申请人： Merck Sharp & Dohme Corp.

发明人： WOOD, Harold, B. ,  MEINKE, Peter, T. ,  SHI, Guo, Q. ,  ZHANG, Yong

IPC分类号： C07D401/04 ,  C07D261/20 ,  C07D413/04 ,  C07D403/04 ,  C07D239/34 ,  C07D307/80 ,  A61K31/416 ,  A61K31/423 ,  A61K31/4439 ,  A61K31/513 ,  A61P3/10

CPC分类号： C07D401/04 ,  C07D239/34 ,  C07D261/20 ,  C07D307/80 ,  C07D403/04 ,  C07D413/04

公开(公告)号：EP2571855A1

公开(公告)日：2013-03-27

申请号：EP11783980.3

申请日：2011-05-12

申请人： Merck Sharp & Dohme Corp.

发明人： DEBENHAM, John, S. ,  SHEN, Dong-Ming ,  GRAHAM, Thomas, H. ,  CLEMENTS, Matthew, J. ,  ZHANG, Yong

IPC分类号： C07D235/02

CPC分类号： C07C237/24 ,  A61K31/165 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/4453 ,  A61K31/5375 ,  A61K31/5377 ,  A61K45/06 ,  C07C271/24 ,  C07C2601/02 ,  C07C2601/14 ,  C07D205/04 ,  C07D213/40 ,  C07D213/61 ,  C07D213/64 ,  C07D213/85 ,  C07D233/56 ,  C07D233/61 ,  C07D239/26 ,  C07D241/12 ,  C07D295/15 ,  C07D295/155

摘要： Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

摘要翻译： 结构式I的化合物是脯氨酰羧肽酶（PrCP）的抑制剂。 本发明的化合物可用于预防和治疗与PrCP的酶活性相关的病症，例如异常代谢，包括肥胖症; 糖尿病; 代谢综合征; 肥胖相关疾病; 和糖尿病相关的疾病。