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公开(公告)号：US20210403457A1
公开(公告)日：2021-12-30
申请号：US17347639
申请日：2021-06-15
Applicant: Merck Sharp & Dohme Corp.
Inventor： Ashok Arasappan , Ian M. Bell , Christopher James Bungard , Christopher S. Burgey , Jason M. Cox , Michael J. Kelly, III , Mark E. Layton , Hong Liu , Jian Liu , James J. Perkins , Akshay A. Shah , Michael David VanHeyst , Zhe Wu
IPC: C07D403/12 , C07D233/32 , C07D401/14 , C07D401/12 , C07D405/12 , C07D417/12 , C07D417/14 , C07D413/12 , C07D513/04 , C07D471/08 , C07D471/04
Abstract: 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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2.发明申请公开(公告)号：US20170305902A1
公开(公告)日：2017-10-26
申请号：US15506269
申请日：2015-08-24
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Ashok Arasappan , Christopher James Bungard , Jessica L. Frie , Yongxin Han , Scott B. Hoyt , Peter J. Manley , Robert S. Meissner , James J. Perkins , Iyassu K. Sebhat , Robert R. Wilkening , Kenneth J. Leavitt
IPC: C07D471/04
CPC classification number: C07D471/04 , A61K31/4375
Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
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公开(公告)号：US09636337B2
公开(公告)日：2017-05-02
申请号：US15047224
申请日：2016-02-18
Applicant: Merck Sharp & Dohme Corp
Inventor： Christopher James Bungard , Antonella Converso , Pablo De Leon , Barbara Hanney , Timothy John Hartingh , Jesse Josef Manikowski , Peter J. Manley , Robert Meissner , Zhaoyang Meng , James J. Perkins , Michael T. Rudd , Youheng Shu
IPC: A61K31/47 , A61K31/506 , A61K31/4985 , A61K31/496 , A61K31/4709 , A61K31/541 , A61K31/5377 , C07D401/14 , C07D413/14 , C07D215/48 , C07D401/04 , C07D401/06 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
CPC classification number: C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
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公开(公告)号：US11802122B2
公开(公告)日：2023-10-31
申请号：US17347639
申请日：2021-06-15
Applicant: Merck Sharp & Dohme Corp.
Inventor： Ashok Arasappan , Ian M. Bell , Christopher James Bungard , Christopher S. Burgey , Jason M. Cox , Michael J. Kelly, III , Mark E. Layton , Hong Liu , Jian Liu , James J. Perkins , Akshay A. Shah , Michael David VanHeyst , Zhe Wu
IPC: C07D403/12 , C07D233/32 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D513/04 , A61K31/4166 , A61P25/00 , A61P25/04 , A61P29/00
CPC classification number: C07D403/12 , C07D233/32 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D513/04
Abstract: 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：US20210387966A1
公开(公告)日：2021-12-16
申请号：US17289123
申请日：2019-10-31
Applicant: Merck Sharp & Dohme Corp.
Inventor： 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: C07D401/14 , C07D471/04 , C07D413/14 , C07D471/08 , C07D495/04 , C07D401/12 , C07D487/04 , C07D491/048
Abstract: 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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Patent Agency Ranking
公开(公告)号：US10072003B2
公开(公告)日：2018-09-11
申请号：US15506269
申请日：2015-08-24
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Ashok Arasappan , Christopher James Bungard , Jessica L. Frie , Yongxin Han , Scott B. Hoyt , Peter J. Manley , Robert S. Meissner , James J. Perkins , Iyassu K. Sebhat , Robert R. Wilkening , Kenneth J. Leavitt
IPC: C07D471/04
CPC classification number: C07D471/04 , A61K31/4375
Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
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公开(公告)号：US20160159744A1
公开(公告)日：2016-06-09
申请号：US15047213
申请日：2016-02-18
Applicant: Merck Sharp & Dohme Corp
Inventor： Christopher James Bungard , Antonella Converso , Pablo De Leon , Barbara Hanney , Timothy John Hartingh , Jesse Josef Manikowski , Peter J. Manley , Robert Meissner , Zhaoyang Meng , James J. Perkins , Michael T. Rudd , Youheng Shu
IPC: C07D215/48 , C07D409/04 , C07D401/06 , C07D417/14 , C07D417/06 , C07D401/14 , C07D471/04 , C07D401/04 , C07D413/06
CPC classification number: C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
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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
Applicant: Merck Sharp & Dohme Corp.
Inventor： 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: C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/04 , C07D471/08 , C07D487/04 , C07D491/048 , C07D495/04
Abstract: 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Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use 有权喹啉羧酰胺和喹啉腈衍生物作为mGluR2-负变构调节剂，组合物及其用途公开(公告)号：US09278960B2
公开(公告)日：2016-03-08
申请号：US14356080
申请日：2012-10-26
Applicant: Merck Sharp & Dohme Corp.
Inventor： Christopher James Bungard , Antonella Converso , Barbara Hanney , Timothy John Hartingh , Peter J. Manley , Robert S. Meissner , James J. Perkins , Michael T. Rudd
IPC: C07D413/14 , C07D401/06 , C07D401/14 , C07D215/48 , C07D401/04 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
CPC classification number: C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
Abstract translation: 本发明提供式（I）的喹啉羧酰胺和喹啉腈化合物，其中环A，RQ，-L-，R1，n，R2和R3如本文所定义。 本发明的化合物可用作非竞争性mGluR2拮抗剂或mGluR2负变构调节剂（NAM），以及用于治疗患有（其中涉及mGluR2-NAM受体的疾病或病症）的患者（优选人）的方法，例如 作为阿尔茨海默病，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍，通过向患者施用治疗有效量的本发明化合物或其药学上可接受的盐。 本发明还涉及包含本发明化合物或其药学上可接受的盐（任选与一种或多种另外的活性成分组合）和药学上可接受的载体的药物组合物，以及该化合物和药物组合物的用途 的本发明治疗这些疾病。
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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
Applicant: 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.
Inventor： 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: C07D413/12 , C07D263/24 , C07D417/12
CPC classification number: C07D413/12 , C07D263/24 , C07D417/12
Abstract: 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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