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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：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：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：US10272077B2
公开(公告)日：2019-04-30
申请号：US15830131
申请日：2017-12-04
发明人： Ian M. Bell , Mark E. Fraley , Steven N. Gallicchio , Anthony Ginetti , Helen J. Mitchell , Daniel V. Paone , Donnette D. Staas , Cheng Wang , C. Blair Zartman
IPC分类号： C07D471/10 , A61K31/4545 , A61K31/435 , A61K31/438 , C07D471/20
摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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公开(公告)号：US20180141952A1
公开(公告)日：2018-05-24
申请号：US15736202
申请日：2016-06-27
申请人： Shawn J. STACHEL , Christopher J. SINZ , Yili CHEN , Jonathan E. WILSON , Michael P. DWYER , Daniel V. PAONE , Shimin XU , Merck Sharp & Dohme Corp.
发明人： Shawn J. Stachel , Michael P. Dwyer , Christopher J. Sinz , Jonathan E. Wilson , Daniel V. Paone , Yili Chen , Shimin Xu
摘要： The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) 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：US20190275024A1
公开(公告)日：2019-09-12
申请号：US16396056
申请日：2019-04-26
发明人： Ian M. Bell , Mark E. Fraley , Steven N. Gallicchio , Anthony Ginnetti , Helen J. Mitchell , Daniel V. Paone , Donnette D. Staas , Cheng Wang , C. Blair Zartman
IPC分类号： A61K31/4545 , C07D471/20 , A61K31/438 , A61K31/435 , C07D471/10
摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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公开(公告)号：US09656990B2
公开(公告)日：2017-05-23
申请号：US15116518
申请日：2015-02-06
发明人： Shawn Stachel , Daniel V. Paone , Jing Li , Anthony Ginnetti , Jianmin Fu , Shimin Xu
IPC分类号： C07D401/10 , C07D231/12 , C07D401/04 , C07D403/04 , C07D403/10 , C07D471/04 , A61K31/415 , A61K31/4155 , A61K31/5377 , A61K31/541 , A61K31/496 , A61K31/454 , A61K45/06
CPC分类号： C07D401/10 , A61K31/415 , A61K31/4155 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D231/12 , C07D401/04 , C07D403/04 , C07D403/10 , C07D471/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
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公开(公告)号：US09458181B2
公开(公告)日：2016-10-04
申请号：US14506760
申请日：2014-10-06
发明人： Shawn Stachel , Daniel V. Paone , Jing Li , Kausik Nanda
IPC分类号： A61K31/421 , C07D263/32 , C07D263/34 , C07D277/30 , C07D413/04 , C07D413/10 , C07D417/10 , C07D417/14 , C07D495/08 , C07F7/08 , A61K31/695 , A61K31/422 , A61K31/547 , A61K31/541 , A61K31/5377 , A61K31/496 , C07D513/08 , A61K31/427 , A61K45/06 , C07D413/12
CPC分类号： C07F7/0807 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/547 , A61K31/695 , A61K45/06 , C07D263/32 , C07D263/34 , C07D277/30 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/14 , C07D495/08 , C07D513/08
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
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公开(公告)号：US10287293B2
公开(公告)日：2019-05-14
申请号：US15736202
申请日：2016-06-27
申请人： Merck Sharp & Dohme Corp. , Shawn J. Stachel , Christopher J. Sinz , Yili Chen , Jonathan E. Wilson , Michael P. Dwyer , Daniel V. Paone , Shimin Xu
发明人： Shawn J. Stachel , Michael P. Dwyer , Christopher J. Sinz , Jonathan E. Wilson , Daniel V. Paone , Yili Chen , Shimin Xu
摘要： The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) 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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