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公开(公告)号：US20170073354A1
公开(公告)日：2017-03-16
申请号：US15124635
申请日：2015-03-06
申请人： Jurgen SCHULZ , Peter D. WILLIAMS , John A. MCCAULEY , Christopher J. BUNGARD , David Jonathan BENNETT , Sherman T. WADDELL , Gregori J. MORRIELLO , Lehua CHANG , Michael P. DWYER , Katharine M. HOLLOWAY , Alejandro CRESPO , Xin-Jie CHU , Catherine WISCOUNT , Marie H. LOUGHRAN , Jesse J. MANIKOWSKI , Kartik M. KEERTIKAR , Bin HU , Bin ZHONG , Tao JI , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd.
发明人： Peter D. Williams , John A. McCauley , Christopher J. Bungard , David Jonathan Bennett , Sherman T. Waddell , Gregori J. Morriello , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Alejandro Crespo , Xin-Jie Chu , Catherine Wiscount , H. Marie Loughran , Jesse J. Manikowski , Jurgen Schulz , Kartik M. Keertikar , Bin Hu , Bin Zhong , Tao Ji
IPC分类号： C07D513/08 , A61K31/554 , A61K45/06
CPC分类号： C07D513/08 , A61K31/554 , A61K45/06
摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
摘要翻译： 本发明涉及含有该化合物的式I药物组合物的化合物及其在抑制HIV蛋白酶，抑制HIV复制，预防HIV感染，HIV感染治疗和预防， 治疗和延迟艾滋病的发病或进展。
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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：US10000501B2
公开(公告)日：2018-06-19
申请号：US15513852
申请日：2015-09-23
发明人： Jiaqiang Cai , Vincent Colandrea , Alejandro Crespo , John Debenham , Xiaoxing Du , Deodialsingh Guiadeen , Ping Liu , Rongqiang Liu , Christina B. Madsen-Duggan , Joshua G. McCoy , Weiguo Quan , Christopher Sinz , Liping Wang
IPC分类号： C07D491/052 , C07D221/22 , C07D417/06 , C07D471/04 , C07D215/56
CPC分类号： C07D491/052 , C07D215/56 , C07D221/22 , C07D417/06 , C07D471/04
摘要： The present invention concerns a compound of formula I or a pharmaceutically acceptable salt thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
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公开(公告)号：US09969752B2
公开(公告)日：2018-05-15
申请号：US15514536
申请日：2015-09-23
发明人： Jiaqiang Cai , Alejandro Crespo , Xiaoxing Du , Byron Gabriel Dubois , Deodialsingh Guiadeen , Shankaran Kothandaraman , Ping Liu , Rongqiang Liu , Weiguo Quan , Christopher Sinz , Liping Wang
IPC分类号： C07D471/06 , C07D498/06 , C07D513/06 , C07D498/16
CPC分类号： C07D513/06 , C07D471/04 , C07D471/06 , C07D498/04 , C07D498/06 , C07D498/16 , C07D513/04
摘要： The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
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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：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：US10138255B2
公开(公告)日：2018-11-27
申请号：US15124635
申请日：2015-03-06
发明人： Peter D. Williams , John A. McCauley , Christopher J. Bungard , David Jonathan Bennett , Sherman T. Waddell , Gregori J. Morriello , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Alejandro Crespo , Xin-Jie Chu , Catherine Wiscount , H. Marie Loughran , Jesse J. Manikowski , Jurgen Schulz , Kartik M. Keertikar , Bin Hu , Bin Zhong , Tao Ji
IPC分类号： A61K31/554 , C07D513/08 , A61K45/06
摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
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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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