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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.
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公开(公告)号:US10287269B2
公开(公告)日:2019-05-14
申请号:US15559284
申请日:2016-03-21
发明人: Dong-Ming Shen , Jonathan E. Wilson , Meng Yang , Dann Parker , Zack Zhiqiang Guo , Alejandro Crespo , Deping Wang , Troy McCracken
IPC分类号: C07D403/04 , C07D401/14 , C07D405/14
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.
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公开(公告)号:US20180148453A1
公开(公告)日:2018-05-31
申请号:US15576351
申请日:2016-05-31
发明人: Dong-Ming Shen , Michael P. Dwyer , Christopher J. Sinz , Deping Wang , Shawn J. Stachel , Daniel V. Paone , Ashley Forster , Richard Berger , Yili Chen , Yimin Qian , Shimin Xu , Chunmei Hu
摘要: The present invention is directed to 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 hypofunction or basal ganglia dysfunction.
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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
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.
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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.
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公开(公告)号:US10285989B2
公开(公告)日:2019-05-14
申请号:US15573858
申请日:2016-05-10
发明人: Dong-Ming Shen , Deping Wang , XiaoXia Qian , Bart Harper , Meng Yang , Yingjian Bo
IPC分类号: C07D403/12 , A61K31/513 , C07D401/12 , C07D403/04 , C07D405/12 , C07D239/38 , C07D239/42 , C07D239/52 , C07D487/04 , A61P25/28 , A61P25/22 , A61P25/18 , A61P25/16 , A61P25/06
摘要: The present invention is directed to pyrimidinone amide compounds which may be useful as therapeutic agents for the treatment of central nervous system and/or peripheral 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, Alzheimer's, cognitive impairment, anxiety, depression, migraines, or Huntington's disease, Parkinson's disease, Parkinson's disease dementia (PDD), and other diseases associated with striatal hypofunction or basal ganglia dysfunction.
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公开(公告)号:US10174037B2
公开(公告)日:2019-01-08
申请号:US15576351
申请日:2016-05-31
发明人: Dong-Ming Shen , Michael P. Dwyer , Christopher J. Sinz , Deping Wang , Shawn J. Stachel , Daniel V. Paone , Ashley Forster , Richard Berger , Yili Chen , Yimin Qian , Shimin Xu , Chunmei Hu
摘要: The present invention is directed to 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 hypofunction or basal ganglia dysfunction.
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公开(公告)号:US09403807B2
公开(公告)日:2016-08-02
申请号:US14557980
申请日:2014-12-02
发明人: Alejandro Crespo , Ping Lan , Rudrajit Mal , Anthony Ogawa , Hong Shen , Peter J. Sinclair , Zhongxiang Sun , Ellen K. Vande Bunte , Zhicai Wu , Kun Liu , Robert J. DeVita , Dong-Ming Shen , Min Shu , John Qiang Tan , Changhe Qi , Yuguang Wang , Richard Beresis
IPC分类号: C07D413/06 , C07D231/56 , A61K31/404 , A61K31/416 , C07D403/06 , C07D209/08 , C07D209/10 , A61K31/405 , A61K31/4196 , A61K31/722 , A61K31/4245 , A61K45/06 , C07D403/04 , C07D405/06 , A61K31/4045 , A61K31/422
CPC分类号: C07D413/06 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/416 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K45/06 , C07D209/08 , C07D209/10 , C07D231/56 , C07D403/04 , C07D403/06 , C07D405/06
摘要: The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are useful for treating aldosterone-mediated diseases. 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 compositions which comprise compounds of the Formula I.
摘要翻译: 本发明涉及可用于治疗醛固酮介导的疾病的式I化合物及其药学上可接受的盐。 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此目的的药物,以及包含式I化合物的药物组合物。
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公开(公告)号:US20150284376A1
公开(公告)日:2015-10-08
申请号:US14557980
申请日:2014-12-02
发明人: Alejandro Crespo , Ping Lan , Rudrajit Mal , Anthony Ogawa , Hong Shen , Peter J. Sinclair , Zhongxiang Sun , Ellen K. Vande Bunte , Zhicai Wu , Kun Liu , Robert J. DeVita , Dong-Ming Shen , Min Shu , John Qiang Tan , Changhe Qi , Yuguang Wang , Richard Beresis
IPC分类号: C07D413/06 , A61K31/405 , C07D231/56 , A61K31/416 , A61K31/4045 , A61K45/06 , C07D403/06 , A61K31/4196 , A61K31/422 , C07D403/04 , A61K31/404 , C07D405/06 , C07D209/08 , A61K31/4245
CPC分类号: C07D413/06 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/416 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K45/06 , C07D209/08 , C07D209/10 , C07D231/56 , C07D403/04 , C07D403/06 , C07D405/06
摘要: The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are useful for treating aldosterone-mediated diseases. 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 compositions which comprise compounds of the Formula I.
摘要翻译: 本发明涉及可用于治疗醛固酮介导的疾病的式I化合物及其药学上可接受的盐。 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此目的的药物,以及包含式I化合物的药物组合物。
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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.
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