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1.发明申请C6-SPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权C6-SPIRO三嗪二氧化物作为BACE抑制剂，组合物及其使用公开(公告)号：US20160264538A1
公开(公告)日：2016-09-15
申请号：US14653671
申请日：2013-12-16
申请人： Jared N. CUMMING , Jack D. SCOTT , Andrew W. STAMFORD , Ulrich ISERLOH , Santhosh Francis NEELAMKAVIL , Pengcheng Patrick SHAO , Jonathan E. WILSON , MERCK SHARP & DOHME CORP.
发明人： Jared N. Cumming , Jack D. Scott, JR. , Andrew W. Stamford , Ulrich Iserloh , Santhosh Francis Neelamkavil , Pengcheng Patrick Shao , Jonathan E. Wilson
IPC分类号： C07D285/24 , C07D471/04 , C07D417/12 , C07D513/10 , C07D519/00
CPC分类号： C07D285/24 , C07D285/20 , C07D417/12 , C07D471/04 , C07D513/10 , C07D519/00
摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed:
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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：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：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：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：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：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：US09688630B2
公开(公告)日：2017-06-27
申请号：US15028306
申请日：2014-10-06
IPC分类号： C07D491/107 , C07D417/06 , C07D413/10 , C07D405/12 , C07D403/10 , C07D401/04 , C07D401/06 , C07D401/10 , A61K31/5377 , A61K31/4439 , A61K31/454 , A61K31/427 , A61K31/404 , C07D209/12 , A61K45/06 , C07D209/10 , C07D209/24 , C07D209/14 , C07D209/18
CPC分类号： C07D209/12 , A61K31/404 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D209/10 , C07D209/14 , C07D209/18 , C07D209/24 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/12 , C07D413/10 , C07D417/06 , C07D491/107
摘要： 3,3′-Disubstituted indoline compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
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9.发明授权C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use 有权作为BACE抑制剂，组合物及其用途的C6-螺亚麻醇二氮杂二恶英公开(公告)号：US09580396B2
公开(公告)日：2017-02-28
申请号：US14653671
申请日：2013-12-16
发明人： Jared N. Cumming , Jack D. Scott, Jr. , Andrew W. Stamford , Ulrich Iserloh , Santhosh Francis Neelamkavil , Pengcheng Patrick Shao , Jonathan E. Wilson
IPC分类号： C07D285/24 , C07D417/12 , C07D471/04 , C07D513/10 , C07D519/00 , C07D285/20
CPC分类号： C07D285/24 , C07D285/20 , C07D417/12 , C07D471/04 , C07D513/10 , C07D519/00
摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
摘要翻译： 在其许多实施方案中，本发明提供某些C5-螺亚氨基二嗪二氧化物化合物，包括式（I）化合物：（结构表示）或其互变异构体及所述化合物的药学上可接受的盐，其中R1，R2，R3，X，Y ，s，环A，RA，m，-L1-和RL如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物，
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公开(公告)号：US20170015633A1
公开(公告)日：2017-01-19
申请号：US15107233
申请日：2014-12-17
发明人： Dong Ming Shen , Melissa Egbertson , Richard Berger , XiaoXia Qian , Yimin Qian , Bart Harper , Meng Yang , Zack Zhi Qiang Guo , Vanessa L. Rada , Deping Wang , Timothy A. Cernak , Christopher Sinz , Ming Wang , Jonathan E. Wilson , Shimin Xu
IPC分类号： C07D239/36 , C07D401/12 , C07D403/04 , C07D403/06 , C07D487/04 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/04 , C07D401/06 , C07D403/12
CPC分类号： C07D239/36 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/04 , C07D487/04
摘要： Disclosed are 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), pharmaceutical compositions and uses thereof.
摘要翻译： 公开了式（I）的嘧啶羧酰胺化合物，其可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病，药物组合物及其用途的治疗剂。
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