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公开(公告)号：US10894775B2
公开(公告)日：2021-01-19
申请号：US16341591
申请日：2017-10-09
申请人： Merck Sharp & Dohme Corp. , Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu , Chuanman Huang
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu , Chuanman Huang
IPC分类号： C07D221/20 , C07D211/16 , C07D211/96
摘要： In its many embodiments, the present invention provides certain piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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2.发明申请公开(公告)号：US20200247754A1
公开(公告)日：2020-08-06
申请号：US16341595
申请日：2017-10-09
申请人： Michael T. RUDD , Zhaoyang MENG , Jenny WAI , David Jonathan BENNETT , Edward J. BRNARDIC , Nigel J. LIVERTON , Shawn J. STACHEL , Yongxin HAN , Paul TEMPEST , Jiuxiang ZHU , Xuewang XU , Bin ZHU , Merck Sharp & Dohme Corp.
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
IPC分类号： C07D221/20 , C07D401/12 , C07D417/12 , C07D405/12 , C07D211/22 , C07D401/14 , C07D417/14
摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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3.发明授权公开(公告)号：US11655216B2
公开(公告)日：2023-05-23
申请号：US16341595
申请日：2017-10-09
申请人： Merck Sharp & Dohme Corp. , Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
IPC分类号： C07D221/20 , C07D401/12 , C07D417/12 , C07D405/12 , C07D211/22 , C07D401/14 , C07D417/14
CPC分类号： C07D221/20 , C07D211/22 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12 , C07D417/14
摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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4.发明申请公开(公告)号：US20180327374A1
公开(公告)日：2018-11-15
申请号：US15774157
申请日：2016-11-07
申请人： Michael T. RUDD , Edward J. BRNARDIC , Yuntae KIM , Robert S. MEISSNER , Vanessa RADA , Shawn J. STACHEL , Celina V. ZERBINATTI , Merck Sharp & Dohme Corp.
发明人： Michael T. Rudd , Edward J. Brnardic , Yuntae Kim , Robert S. Meissner , Vanessa L. Rada , Shawn J. Stachel , Celina V. Zerbinatti
IPC分类号： C07D295/16 , C07D243/08 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D487/08 , C07D513/04 , A61P25/28 , A61P25/18 , A61P25/16 , A61P3/10
CPC分类号： C07D295/16 , A61K31/496 , A61P3/10 , A61P25/16 , A61P25/18 , A61P25/28 , C07D213/74 , C07D213/85 , C07D243/08 , C07D295/192 , C07D295/205 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/08 , C07D487/18 , C07D513/04 , C07D515/04
摘要： In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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公开(公告)号：US10239849B2
公开(公告)日：2019-03-26
申请号：US15774157
申请日：2016-11-07
申请人： Merck Sharp & Dohme Corp. , Michael T. Rudd , Edward J. Brnardic , Yuntae Kim , Robert S. Meissner , Vanessa L. Rada , Shawn J. Stachel , Celina V. Zerbinatti
发明人： Michael T. Rudd , Edward J. Brnardic , Yuntae Kim , Robert S. Meissner , Vanessa L. Rada , Shawn J. Stachel , Celina V. Zerbinatti
IPC分类号： C07D243/08 , C07D295/16 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D487/08 , C07D513/04 , A61P25/18 , A61P25/16 , A61P25/28 , A61P3/10
摘要： In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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公开(公告)号：US20230227441A1
公开(公告)日：2023-07-20
申请号：US18009306
申请日：2021-06-14
申请人： Ashok ARASAPPAN , Ian M. BELL , Christopher James BUNGARD , Christopher S. BURGEY , Jason M. COX , Deodial Guy GUIADEEN , Michael J. KELLY , Mark E. LAYTON , Hong LIU , Jian LIU , James T. OLSEN , James J. PERKINS , Jeffrey W. SCHUBERT , Akshay A. SHAH , Michael D. VANHEYST , Zhe WU , Shawn J. STACHEL , MERCK SHARP & DOHME CORP.
发明人： Ashok Arasappan , Ian M. Bell , Christopher James Bungard , Christopher S. Burgey , Jason Michael Cox , Deodial Guy Guiadeen, III , Michael J. Kelly, III , Mark E. Layton , Hong Liu , Jian Liu , James T. Olsen , James J. Perkins , Jeffrey W. Schubert , Akshay A. Shah , Shawn J. Stachel , Michael David VanHeyst , Zhe Wu
IPC分类号： C07D413/12 , C07D263/24 , C07D417/12
CPC分类号： C07D413/12 , C07D263/24 , C07D417/12
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
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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：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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![Substituted pyrrolo[3,2-c]pyridines as TrkA kinase inhibitors](/abs-image/US/2015/08/11/US09102673B2/abs.jpg.150x150.jpg)
10.发明授权公开(公告)号：US09102673B2
公开(公告)日：2015-08-11
申请号：US14131861
申请日：2012-07-06
申请人： Barbara Hanney , Peter Manley , Michael T. Rudd , John M. Sanders , Shawn J. Stachel , Darrell Henze
发明人： Barbara Hanney , Peter Manley , Michael T. Rudd , John M. Sanders , Shawn J. Stachel , Darrell Henze
IPC分类号： A61K31/437 , C07D471/04 , C07D401/04 , C07D403/04 , C07D405/04 , C07D417/04 , C07D487/04
CPC分类号： C07D471/04 , C07D401/04 , C07D403/04 , C07D405/04 , C07D417/04 , C07D487/04
摘要： The present invention is directed to compounds of formula I and Ia: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
摘要翻译： 本发明涉及式I和Ia的化合物：它们是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成， 与神经生长因子（NGF）受体TrkA的异常活动相关的疾病，失调，损伤或功能障碍，或与脱髓鞘或脱髓鞘相关的疾病或病症。
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