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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：US20230227405A1
公开(公告)日：2023-07-20
申请号：US18009310
申请日：2021-06-14
申请人： Ashok ARASAPPAN , Ian M. BELL , Jason M. COX , Michael J. KELLY, III , Mark E. LAYTON , Hong LIU , Jian LIU , Akshay A. SHAH , Michael D. VANHEYST , MERCK SHARP & DOHME CORP.
发明人： Ashok Arasappan , Ian M. Bell , Jason Michael Cox , Michael J. Kelly, III , Mark E. Layton , Hong Liu , Jian Liu , Akshay A. Shah , Michael David VanHeyst
IPC分类号： C07D207/277 , C07D401/12 , C07D417/12
CPC分类号： C07D207/277 , C07D401/12 , 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：US20220396571A1
公开(公告)日：2022-12-15
申请号：US17771527
申请日：2020-10-29
IPC分类号： C07D417/08 , A61K31/454 , C07D413/14 , C07D401/14 , A61K31/4545 , A61K31/506
摘要： The present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
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公开(公告)号：US20200262826A1
公开(公告)日：2020-08-20
申请号：US16646616
申请日：2018-09-14
申请人： Ian M. BELL , Brendan M. CROWLEY , Peter J. MANLEY , William D. SHIPE , Merck Sharp & Dohme Corp.
IPC分类号： C07D413/08 , C07D413/14 , C07D417/08 , C07D417/14 , A61P25/28 , A61P25/16 , A61P25/18
摘要： The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I).
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公开(公告)号：US20110021516A1
公开(公告)日：2011-01-27
申请号：US12934208
申请日：2009-03-24
申请人： Harold G. Selnick , Ian M. Bell , Melody McWherter , Donnette D. Staas , Shawn J. Stachel , Thomas Steele , Craig Stump , Michael R. Wood , C. Blair Zartman
发明人： Harold G. Selnick , Ian M. Bell , Melody McWherter , Donnette D. Staas , Shawn J. Stachel , Thomas Steele , Craig Stump , Michael R. Wood , C. Blair Zartman
IPC分类号： A61K31/5365 , C07D471/04 , A61K31/496 , A61P25/06
CPC分类号： C07D471/10 , C07D403/06 , C07D471/20 , C07D519/00
摘要： The present invention is directed to compounds of the formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, G1, G2, G3, G4, J, Q, Ea, Eb, Ec, R6, R7, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译： 本发明涉及式（I）的化合物：（其中变量A1，A2，A3，A4，A5，A6，A7，A8，G1，G2，G3，G4，J，Q，Ea，Eb，Ec ，R6，R7，RPG和Y如本文所述），其是CGRP受体的拮抗剂，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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公开(公告)号：US08765759B2
公开(公告)日：2014-07-01
申请号：US12934208
申请日：2009-03-24
申请人： Harold G. Selnick , Ian M. Bell , Melody McWherter , Donnette D. Staas , Shawn J. Stachel , Thomas Steele , Craig Stump , Michael R. Wood , C. Blair Zartman
发明人： Harold G. Selnick , Ian M. Bell , Melody McWherter , Donnette D. Staas , Shawn J. Stachel , Thomas Steele , Craig Stump , Michael R. Wood , C. Blair Zartman
IPC分类号： A61K31/437 , A61K31/497 , A61K31/4985
CPC分类号： C07D471/10 , C07D403/06 , C07D471/20 , C07D519/00
摘要： The present invention is directed to compounds of the formula: (wherein variables A1, A2, A3, G1, G2, G3, G4, J, Ea, Eb, Ec, R6, R7, and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译： 本发明涉及下式的化合物：其中作为拮抗剂的式（其中变量A1，A2，A3，G1，G2，G3，G4，J，Ea，Eb，Ec，R6，R7和Y如本文所述） 的CGRP受体，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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公开(公告)号：US07390798B2
公开(公告)日：2008-06-24
申请号：US11660798
申请日：2005-02-09
IPC分类号： C07D401/14 , C07D471/10 , A61K31/553 , A61K31/55 , A61K31/438 , A61K31/4166 , A61P25/06
CPC分类号： C07D471/04 , C07D401/12 , C07D413/12 , C07D519/00
摘要： The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved
摘要翻译： 本发明涉及式I的化合物：I（其中变量A 1，A 2，B，J，K，m，n，R 4 R 5c，R 5b和R 5c如本文所定义）可用作CGRP受体的拮抗剂并且可用于治疗 或预防CGRP所涉及的疾病，如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途
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公开(公告)号：US11377438B2
公开(公告)日：2022-07-05
申请号：US16669598
申请日：2019-10-31
发明人： Ashok Arasappan , Ian M. Bell , Michael J. Breslin , Christopher James Bungard , Christopher S. Burgey , Harry R. Chobanian , Jason M. Cox , Anthony T. Ginnetti , Deodial Guy Guiadeen , Kristen L. G. Jones , Mark E. Layton , Hong Liu , Jian Liu , James J. Perkins , Shawn J. Stachel , Linda M. Suen-Lai , Zhe Wu
IPC分类号： C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/04 , C07D471/08 , C07D487/04 , C07D491/048 , C07D495/04
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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9.发明授权公开(公告)号：US11026958B2
公开(公告)日：2021-06-08
申请号：US16345997
申请日：2017-10-30
发明人： Brendan M. Crowley , Ian M. Bell , Andrew John Harvey , Brian T. Campbell , Thomas J. Greshock , Vanessa L. Rada
IPC分类号： A61K31/695 , A61K31/198 , C07D213/34 , C07D413/04 , C07D239/26 , C07D401/04 , C07D271/06 , C07D233/64 , C07D249/08 , A61K31/4418 , A61K31/5377 , A61K31/505 , A61K31/4439 , A61K31/4245 , A61K31/506 , A61K31/50 , A61K31/4965 , C07D237/08 , C07D241/12 , C07F7/08 , A61K31/4196 , A61K31/4164 , A61K45/06
摘要： The present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
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公开(公告)号：US20190275024A1
公开(公告)日：2019-09-12
申请号：US16396056
申请日：2019-04-26
发明人： Ian M. Bell , Mark E. Fraley , Steven N. Gallicchio , Anthony Ginnetti , Helen J. Mitchell , Daniel V. Paone , Donnette D. Staas , Cheng Wang , C. Blair Zartman
IPC分类号： A61K31/4545 , C07D471/20 , A61K31/438 , A61K31/435 , C07D471/10
摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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