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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：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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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：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.
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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.
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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：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：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：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：US09840478B2
公开(公告)日：2017-12-12
申请号：US14908421
申请日：2014-07-29
发明人： Peter D. Williams , John A. McCauley , David Jonathan Bennett , Christopher J. Bungard , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Kartik M. Keertikar , H. Marie Loughran , Jessie J. Manikowski , Gregori J. Morriello , Dong-Ming Shen , Edward C. Sherer , Jurgen Schultz , Sherman T. Waddell , Catherine M. Wiscount , Nicolas Zorn , Xin-Jie Chu , Satyanarayana Tummanapalli , Vijayasaradhi Sivalenka , Bin Hu , Tao Ji , Bin Zhong
IPC分类号： C07D241/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/14
CPC分类号： C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to piperazine derivatives, 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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