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公开(公告)号：US10370337B2
公开(公告)日：2019-08-06
申请号：US15745850
申请日：2016-07-27
Applicant: Merck Sharp & Dohme Corp. , Antonella Converso , Mildred L. Kaufman , Kevin Rodzinak
Inventor： Antonella Converso , Mildred L. Kaufman , Kevin Rodzinak
IPC: C07D215/22 , A61K31/4704 , C07D215/56 , A61K45/06 , C07D215/54 , C07D405/12
Abstract: The present invention is directed to oxycyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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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：US09663506B2
公开(公告)日：2017-05-30
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: C07D413/14 , C07D417/14 , C07D401/14 , C07D215/48 , C07D401/04 , C07D401/06 , C07D409/04 , C07D413/06 , C07D417/06 , C07D471/04 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , 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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4.发明申请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-负性变构调节剂，组合物及其用途公开(公告)号：US20160158217A1
公开(公告)日：2016-06-09
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 , A61K31/541 , A61K31/506 , A61K31/496 , A61K31/4985 , A61K31/4709 , A61K31/5377
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.
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（优选人）的mGluR2-NAM受体涉及的疾病或病症的方法，包括 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，可能导致阿尔茨海默氏病，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。 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：US20220242847A1
公开(公告)日：2022-08-04
申请号：US17611448
申请日：2020-05-18
Applicant: Antonella CONVERSO , Abdellatif EL MARROUNI , Ashley FORSTER , Jessica L. FRIE , David N. HUNTER , Cheng WANG , Deping WANG , Merck Sharp & Dohme Corp.
Inventor： Antonella Converso , Abdellatif El Marrouni , Ashley Forster , Jessica L. Frie , David N. Hunter , Cheng Wang , Deping Wang
IPC: C07D401/06 , C07D401/14 , A61K45/06 , A61K31/506 , A61P31/18
Abstract: 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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Patent Agency Ranking
6.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：US10370336B2
公开(公告)日：2019-08-06
申请号：US15745845
申请日：2016-07-27
Applicant: Merck Sharp & Dohme Corp.
Inventor： Victoria Cofre , Antonella Converso , Kevin Rodzinak
IPC: C07D215/54 , A61P25/18 , A61P25/14
Abstract: The present invention is directed to phenylcyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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8.发明申请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衍生物作为mGluR2负离子调节剂，组合物及其使用公开(公告)号：US20140309227A1
公开(公告)日：2014-10-16
申请号：US14356080
申请日：2012-10-26
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: C07D413/14 , C07D401/14 , C07D401/06 , C07D401/04
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：US20220064147A1
公开(公告)日：2022-03-03
申请号：US17413882
申请日：2019-12-13
Applicant: Merck Sharp & Dohme Corp.
Inventor： 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: C07D403/06 , A61K45/06
Abstract: 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：US20220062284A1
公开(公告)日：2022-03-03
申请号：US17411341
申请日：2021-08-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： Antonella Converso , Abdellatif El Marrouni , Anthony W. Shaw , David N. Hunter , Ashley Forster , Cheng Wang , Yunlong Zhang
IPC: A61K31/513 , A61K45/06 , C07D403/06 , C07D401/06 , A61P31/18
Abstract: The present disclosure is directed to tetrahydroquinazoline derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve 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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