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公开(公告)号：US09511052B2
公开(公告)日：2016-12-06
申请号：US14415210
申请日：2013-07-15
发明人： Timothy A. Cernak , Kevin D. Dykstra , Dong-Ming Shen , Kun Liu , Andrew Stamford , John Qiang Tan
IPC分类号： C07D231/56 , A61K31/416 , A61K45/06
CPC分类号： A61K31/416 , A61K45/06 , C07D231/56 , A61K2300/00
摘要： The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.
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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.
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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.
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公开(公告)号：US10195201B2
公开(公告)日：2019-02-05
申请号：US15571192
申请日：2016-05-02
IPC分类号： A61K31/513 , C07D239/36 , C07D403/04 , A61P25/06 , A61P25/28 , A61P25/18 , A61P25/22 , A61P25/16
摘要： The present invention is directed to substituted pyrimidinone 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：US10160762B2
公开(公告)日：2018-12-25
申请号：US15574411
申请日：2016-05-24
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 , William D. Shipe , Jianmin Fu , Zhigang Guo , Haitang Li , Yingjian Bo
IPC分类号： C07D487/04 , A61K31/519 , A61P25/14 , A61P25/28 , A61P25/18 , A61P25/00 , A61P25/16
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：US20180280390A1
公开(公告)日：2018-10-04
申请号：US15571192
申请日：2016-05-02
CPC分类号： A61K31/513 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , C07D239/36 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04
摘要： The present invention is directed to substituted pyrimidinone 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：US20180237422A1
公开(公告)日：2018-08-23
申请号：US15554614
申请日：2016-03-11
发明人： Dong-Ming Shen , Christopher J. Sinz , Alejandro Crespo , Johnathan E. Wilson , Troy McCraken , Shimin XU , Haitang Li
IPC分类号： C07D403/04 , C07D471/04 , C07D487/04 , C07D498/04
CPC分类号： C07D403/04 , A61K31/4192 , A61K31/4196 , A61K31/506 , A61P25/00 , C07D471/04 , C07D487/04 , C07D498/04
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：US20180057480A1
公开(公告)日：2018-03-01
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 , C07D405/14 , C07D401/14
CPC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：US10214512B2
公开(公告)日：2019-02-26
申请号：US15771538
申请日：2016-10-24
发明人： Jiayi Xu , Amjad Ali , Wei Zhou , Ying-Duo Gao , Scott D. Edmondson , Eric Mertz , Santhosh F. Neelamkavil , Weiguo Liu , Wanying Sun , Dong-Ming Shen , Bart Harper , Cheng Zhu , Thomas Bara , Yeon-Hee Lim , Meng Yang
IPC分类号： C07D471/08 , C07D471/18 , C07D401/14 , A61P7/02 , C07D487/08 , C07D413/14 , C07D401/04
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.
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公开(公告)号：US10143681B2
公开(公告)日：2018-12-04
申请号：US15681478
申请日：2017-08-21
发明人： Dong-Ming Shen , Rongze Kuang , Puneet Kumar , Joseph L. Duffy , Cheng Zhu , Amjad Ali , Meng Yang , John S. Debenham
IPC分类号： A61K31/4412 , C07D213/89 , A61K31/435
摘要： The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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