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公开(公告)号：US10968210B2
公开(公告)日：2021-04-06
申请号：US16345913
申请日：2017-11-13
申请人： Merck Sharp & Dohme Corp. , Thomas J. Greshock , James Mulhearn , Anthony J. Roecker , Tianying Jian , Gang Zhou , Liangqin Guo , Walter Won , Ting Zhang , Rajan Anand , John E. Stelmach , Deping Wang , Ronald M. Kim , Mark E. Layton , Christopher S. Burgey , Philippe G. Nantermet
发明人： Thomas J. Greshock , James Mulhearn , Anthony J. Roecker , Tianying Jian , Gang Zhou , Liangqin Guo , Walter Won , Ting Zhang , Rajan Anand , John E. Stelmach , Deping Wang , Ronald M. Kim , Mark E. Layton , Christopher S. Burgey , Philippe G. Nantermet
IPC分类号： C07D417/12 , C07D417/14 , C07D277/52 , C07D471/04 , C07D487/10 , C07D401/12 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08
摘要： Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.
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公开(公告)号：US10519147B2
公开(公告)日：2019-12-31
申请号：US16061815
申请日：2016-12-15
申请人： Merck Sharp & Dohme Corp. , Thomas J. Greshock , James Mulhearn , Liangqin Guo , Ting Zhang , Deping Wang , Ronald M. Kim , Mark E. Layton , Michael J. Kelly, III , Rajan Anand , Philippe Nantermet , Tianying Jian , Anthony J. Roecker , Walter Won , Gang Zhou
发明人： Thomas J. Greshock , James Mulhearn , Liangqin Guo , Ting Zhang , Deping Wang , Ronald M. Kim , Mark E. Layton , Michael J. Kelly, III , Rajan Anand , Philippe Nantermet , Tianying Jian , Anthony J. Roecker , Walter Won , Gang Zhou
IPC分类号： C07D417/12 , A61K45/06 , C07D277/52 , C07D285/135 , A61P25/02 , A61P25/04 , A61P11/14 , A61P17/04
摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.
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3.发明申请公开(公告)号：US20190185462A1
公开(公告)日：2019-06-20
申请号：US16309390
申请日：2017-06-19
发明人： Abbas Walji , Richard Berger , Craig A. Stump , Kelly Ann S. Schlegel , James J. Mulhearn , Thomas J. Greshock , Deping Wang , Mark E. Fraley , Kristen G. Jones
IPC分类号： C07D413/10 , C07D413/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/052 , C07D498/04 , C07D513/04 , C07D271/06 , C07D471/14 , A61P25/28 , A61P25/18 , A61P29/00 , A61P11/06 , A61P3/10 , A61P35/00 , A61P37/02
CPC分类号： C07D413/10 , A61K45/06 , A61P3/10 , A61P9/00 , A61P11/06 , A61P25/18 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , C07D271/06 , C07D271/113 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/048 , C07D491/052 , C07D498/04 , C07D513/04 , C07F7/0807
摘要： The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.
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公开(公告)号：US20220064147A1
公开(公告)日：2022-03-03
申请号：US17413882
申请日：2019-12-13
发明人： Antonella Converso , Abdellatif El Marrouni , Ashley Forster , Jessica L. Frie , David N. Hunter , Scott D. Kuduk , Helen J. Mitchell , Philippe Nantermet , Deyou Sha , William Daniel Shipe , Cheng Wang , Deping Wang
IPC分类号： C07D403/06 , A61K45/06
摘要： The present disclosure is directed to pyrimidone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
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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：US10221167B2
公开(公告)日：2019-03-05
申请号：US15378465
申请日：2016-12-14
发明人： Thomas J. Greshock , James Mulhearn , Junying Zheng , Ronald M. Kim , Ting Zhang , Anthony J. Roecker , Walter Won , Philippe Nantermet , Rajan Anand , Gang Zhou , Deping Wang , Liangqin Guo
IPC分类号： C07D417/12 , C07D285/08 , C07D277/52 , A61K31/4178 , A61K31/4196 , A61K31/4168 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/551 , A61K45/06
摘要： Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.
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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：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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公开(公告)号：US20220242847A1
公开(公告)日：2022-08-04
申请号：US17611448
申请日：2020-05-18
申请人： Antonella CONVERSO , Abdellatif EL MARROUNI , Ashley FORSTER , Jessica L. FRIE , David N. HUNTER , Cheng WANG , Deping WANG , Merck Sharp & Dohme Corp.
发明人： Antonella Converso , Abdellatif El Marrouni , Ashley Forster , Jessica L. Frie , David N. Hunter , Cheng Wang , Deping Wang
IPC分类号： C07D401/06 , C07D401/14 , A61K45/06 , A61K31/506 , A61P31/18
摘要： The present disclosure is directed to pyridinone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
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