公开(公告)号：US20190276443A1

公开(公告)日：2019-09-12

申请号：US16461880

申请日：2017-11-13

申请人： Dong-Ming SHEN ,  Thomas H. GRAHAM ,  Jinlong JIANG ,  Fa-Xiang DING ,  Clare TUDGE ,  Merck Sharp & Dohme Corp.

发明人： Dong-Ming Shen ,  Thomas H. Graham ,  Jinlong Jiang ,  Fa-Xiang Ding ,  Clare Tudge

IPC分类号： C07D409/12 ,  A61P1/16 ,  C07D209/08 ,  C07D401/12 ,  C07D413/12 ,  C07D409/14

摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

公开(公告)号：US10947222B2

公开(公告)日：2021-03-16

申请号：US16461880

申请日：2017-11-13

申请人： Merck Sharp & Dohme Corp. ,  Dong-Ming Shen ,  Thomas H. Graham ,  Jinlong Jiang ,  Fa-Xiang Ding ,  Clare Tudge

发明人： Dong-Ming Shen ,  Thomas H. Graham ,  Jinlong Jiang ,  Fa-Xiang Ding ,  Clare Tudge

IPC分类号： C07D401/12 ,  C07D409/12 ,  A61P1/16 ,  C07D209/08 ,  C07D409/14 ,  C07D413/12 ,  A61K31/506 ,  A61K45/06 ,  C07D413/14 ,  A61K31/404 ,  A61K31/4439 ,  C07D209/10

摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

公开(公告)号：US20190330239A1

公开(公告)日：2019-10-31

申请号：US16461902

申请日：2017-11-13

申请人： Dong-Ming Shen ,  Thomas H. Graham ,  Wensheng LIU ,  Clare TUDGE ,  Andreas VERRAS ,  Jinlong JIANG ,  Merck Sharp & Dohme Corp.

发明人： Dong-Ming Shen ,  Thomas H. Graham ,  Wensheng Liu ,  Clare Tudge ,  Andreas Verras ,  Jinlong Jiang

IPC分类号： C07D515/08 ,  C07D409/12 ,  C07D401/12 ,  C07D403/12 ,  C07D231/56 ,  C07D405/12 ,  C07D487/04 ,  C07D417/12 ,  C07D413/12 ,  C07D409/14

摘要： The present invention relates to a compound represented by formula I′: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

公开(公告)号：US11104690B2

公开(公告)日：2021-08-31

申请号：US16461902

申请日：2017-11-13

申请人： Merck Sharp & Dohme Corp. ,  Dong-Ming Shen ,  Thomas H. Graham ,  Wensheng Liu ,  Clare Tudge ,  Andreas Verras ,  Jinlong Jiang

发明人： Dong-Ming Shen ,  Thomas H. Graham ,  Wensheng Liu ,  Clare Tudge ,  Andreas Verras ,  Jinlong Jiang

IPC分类号： C07D515/08 ,  C07D409/12 ,  C07D401/12 ,  C07D403/12 ,  C07D231/56 ,  C07D405/12 ,  C07D487/04 ,  C07D417/12 ,  C07D413/12 ,  C07D409/14

摘要： The present invention relates to a compound represented by formula I′: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

公开(公告)号：US20130059830A1

公开(公告)日：2013-03-07

申请号：US13696831

申请日：2011-05-16

申请人： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Cangming Yang

发明人： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Cangming Yang

IPC分类号： A61K31/506 ,  C07D413/14 ,  A61P3/00 ,  A61K31/55 ,  A61P3/04 ,  A61P3/10 ,  C07D401/14 ,  A61K31/5377

CPC分类号： C07D401/14 ,  C07D413/14

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.

公开(公告)号：US08785634B2

公开(公告)日：2014-07-22

申请号：US13638976

申请日：2011-04-21

申请人： Fa-Xiang Ding ,  JinLong Jiang ,  Dong-Ming Shen ,  Hong Shen ,  Zhi-Cai Shi

发明人： Fa-Xiang Ding ,  JinLong Jiang ,  Dong-Ming Shen ,  Hong Shen ,  Zhi-Cai Shi

IPC分类号： C07D401/00

CPC分类号： C07D491/20 ,  C07D491/10

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 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; 和糖尿病相关疾病。

公开(公告)号：US20130023515A1

公开(公告)日：2013-01-24

申请号：US13638976

申请日：2011-04-21

申请人： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Hong Shen ,  Zhi-Cai Shi

发明人： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Hong Shen ,  Zhi-Cai Shi

IPC分类号： C07D491/107 ,  C07D491/20 ,  A61K31/438 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/497 ,  A61K31/501 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/44 ,  A61P3/04 ,  A61P3/10 ,  A61P3/00 ,  A61K31/444

CPC分类号： C07D491/20 ,  C07D491/10

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 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; 肥胖相关障碍; 和糖尿病相关疾病。

公开(公告)号：US20180134712A1

公开(公告)日：2018-05-17

申请号：US15574411

申请日：2016-05-24

申请人： Dong-Ming SHEN ,  Michael P. DWYER ,  Christopher J. SINZ ,  Deping WANG ,  Shawn J. STACHEL ,  Daniel V. PAONE ,  Ashley FORSTER ,  Richard BERGER ,  William D. SHIPE ,  Yili CHEN ,  Yimin QIAN ,  Shimin XU ,  Chunmei HU ,  Jianmin FU ,  Zhigang GUO ,  Haitang LI ,  Yingjian BO ,  Merck Sharp & Dohme Corp. ,  MSD R & D (China) Co., LTD.

发明人： Dong-Ming Shen ,  Michael P. Dwyer ,  Christopher J. Sinz ,  Deping Wang ,  Shawn J. Stachel ,  Daniel V. Paone ,  Ashley Forster ,  Richard Berger ,  Yilli Chen ,  Yimin Qian ,  Shimin Xu ,  Chunmel Hu ,  William D. Shipe ,  Jianmin Fu ,  Zhigang Guo ,  HAITANG LI ,  Yingjian Bo

IPC分类号： C07D487/04 ,  A61P25/18 ,  A61P25/00 ,  A61P25/14 ,  A61P25/28 ,  A61P25/16

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

摘要： The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypo-function or basal ganglia dysfunction.

公开(公告)号：US10358435B2

公开(公告)日：2019-07-23

申请号：US15554614

申请日：2016-03-11

申请人： Merck Sharp & Dohme Corp. ,  Dong-Ming Shen ,  Christopher J. Sinz ,  Alejandro Crespo ,  Johnathan E. Wilson ,  Troy McCracken ,  Shimin Xu ,  Haitang Li

发明人： Dong-Ming Shen ,  Christopher J. Sinz ,  Alejandro Crespo ,  Johnathan E. Wilson ,  Troy McCracken ,  Shimin Xu ,  Haitang Li

IPC分类号： C07D471/04 ,  C07D403/04 ,  C07D487/04 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/506 ,  C07D498/04 ,  A61P25/00

摘要： The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

公开(公告)号：US09365539B2

公开(公告)日：2016-06-14

申请号：US13642646

申请日：2011-05-06

申请人： Jeffrey J. Hale ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Zhicai Wu ,  Cangming Yang

发明人： Jeffrey J. Hale ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Zhicai Wu ,  Cangming Yang

IPC分类号： A61K31/397 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D401/14

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.