-
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.
-
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.
-
公开(公告)号:US10357481B2
公开(公告)日:2019-07-23
申请号:US15579878
申请日:2016-06-27
申请人: MERCK SHARP & DOHME CORP. , Gregori J. Morriello , Lehua Chang , Ashley Forster , Yili Chen , Michael P. Dwyer , Zack Zhiqiang Guo , Ming Wang , Shimin Xu , Yingjian Bo , Jianmin Fu
发明人: Gregori J. Morriello , Lehua Chang , Ashley Forster , Yili Chen , Michael P. Dwyer , Zack Zhiqiang Guo , Ming Wang , Shimin Xu , Yingjian Bo , Jianmin Fu
IPC分类号: A61K31/4196 , C07D471/04 , C07D487/04 , A61P25/28 , A61P25/22 , A61P25/18 , A61P25/16 , A61P25/06 , A61K31/52
摘要: The present invention is directed to substituted triazolo bicyclic 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:US20180162874A1
公开(公告)日:2018-06-14
申请号:US15579115
申请日:2016-06-20
申请人: Gregori J. MORRIELLO , Lehua CHANG , Ashley FORSTER , Yili CHEN , Michael P. DWYER , Richard BERGER , Ming WANG , Kausik K. NADA , Jaime L. BUNDA , William D. SHIPE , Merck Sharp & Dohme Corp.
发明人: Gregori J. Morriello , Michael P. Dwyer , Lehua Chang , Yili Chen , Ming Wang , Ashley Forster , Richard Berger , Kausik k Nanda , Jaime L Bunda , William D Shipe
IPC分类号: C07D498/04 , C07D473/34 , A61P25/18 , A61P25/16 , A61P25/28
CPC分类号: C07D498/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/28 , C07D473/34 , C07D487/04
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.
-
公开(公告)号:US09695198B2
公开(公告)日:2017-07-04
申请号:US14652150
申请日:2013-12-16
申请人: Cameron James Smith , Edward Sherer , Louis-Charles Campeau , James Balkovec , William John Greenlee , Derun Li , Liangqin Guo , Tin-Yau Chan , Yi-Heng Chen , Yili Chen , Samuel Chackalamannil , John Qiang Tan , Tomokazu Hirabayashi , Mika Sekioka , MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD.
发明人: Cameron James Smith , Edward Sherer , Louis-Charles Campeau , James Balkovec , William John Greenlee , Derun Li , Liangqin Guo , Tin-Yau Chan , Yi-Heng Chen , Yili Chen , Samuel Chackalamannil , John Qiang Tan , Tomokazu Hirabayashi , Mika Sekioka
IPC分类号: C07D413/14 , C07D417/06 , C07D498/04 , C07D513/04 , C07D413/12 , C07D471/04 , C07D413/06
CPC分类号: C07D513/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要: The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, 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.
-
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.
-
公开(公告)号:US09708308B2
公开(公告)日:2017-07-18
申请号:US14652237
申请日:2013-12-16
发明人: Cameron James Smith , John Qiang Tan , Ting Zhang , James Balkovec , William John Greenlee , Liangqin Guo , Yi-Heng Chen , Yili Chen , Jiayi Xu , Samuel Chackalamannil , Tomokazu Hirabayashi , Hiroshi Nagasue , Kouki Ogawa
IPC分类号: C07D471/04 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
CPC分类号: C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要: The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
-
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.
-
公开(公告)号:US09914727B2
公开(公告)日:2018-03-13
申请号:US14652174
申请日:2013-12-16
发明人: Cameron James Smith , John Qiang Tan , Ting Zhang , James Balkovec , William John Greenlee , Liangqin Guo , Yi-Heng Chen , Yili Chen , Samuel Chackalamannil , Tomokazu Hirabayashi , Mika Sekioka
IPC分类号: C07D413/14 , C07D413/12 , C07D513/04
CPC分类号: C07D413/14 , C07D413/12 , C07D513/04
摘要: The present invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula I, and methods for using compounds of Formula I for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes.
-
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.
-
-
-
-
-
-
-
-
-