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公开(公告)号：US20210361662A1
公开(公告)日：2021-11-25
申请号：US16966961
申请日：2019-02-11
IPC分类号： A61K31/53 , C07D471/18 , C07D498/18 , A61K31/513 , A61K31/7068 , A61K31/427 , A61K31/635 , A61K31/4418 , A61K31/675 , A61K31/505 , A61K31/52 , A61K31/5365
摘要： The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, Z, R1 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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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
发明人： 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分类号： 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分类号： 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
摘要： 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：US11413292B2
公开(公告)日：2022-08-16
申请号：US16966961
申请日：2019-02-11
IPC分类号： A61K31/53 , A61K31/427 , A61K31/4418 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/5365 , A61K31/635 , A61K31/675 , A61K31/7068 , C07D471/18 , C07D498/18
摘要： The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, Z, R1 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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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
发明人： 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分类号： C07D215/48 , C07D409/04 , C07D401/06 , C07D417/14 , C07D417/06 , C07D401/14 , C07D471/04 , C07D401/04 , C07D413/06
CPC分类号： 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
摘要： 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：US20220259227A1
公开(公告)日：2022-08-18
申请号：US17670689
申请日：2022-02-14
IPC分类号： C07D498/22 , A61K45/06
摘要： The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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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
发明人： Christopher James Bungard , Antonella Converso , Barbara Hanney , Timothy John Hartingh , Peter J. Manley , Robert S. Meissner , James J. Perkins , Michael T. Rudd
IPC分类号： C07D413/14 , C07D401/06 , C07D401/14 , C07D215/48 , C07D401/04 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
CPC分类号： 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
摘要： 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.
摘要翻译： 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：US09822138B2
公开(公告)日：2017-11-21
申请号：US15231365
申请日：2016-08-08
发明人： Petr Vachal , Izzat Raheem , Zhiqiang Guo , Timothy John Hartingh
IPC分类号： C07F9/6561 , A61K45/06 , A61K31/675 , C07F9/16
CPC分类号： C07F9/65616 , A61K31/675 , A61K45/06 , C07F9/16
摘要： Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
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公开(公告)号：US20170044192A1
公开(公告)日：2017-02-16
申请号：US15231365
申请日：2016-08-08
发明人： Petr Vachal , Izzat Raheem , Zhiqiang Guo , Timothy John Hartingh
IPC分类号： C07F9/6561 , A61K31/675 , A61K45/06
CPC分类号： C07F9/65616 , A61K31/675 , A61K45/06 , C07F9/16
摘要： Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
摘要翻译： 及其药学上可接受的盐可用于抑制HIV逆转录酶。 该化合物还可用于预防或治疗HIV的感染以及预防，延缓发作或进展以及AIDS的治疗。 化合物及其盐可以用作药物组合物中的成分，任选地与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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9.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
发明人： 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分类号： C07D413/14 , C07D401/14 , C07D401/06 , C07D401/04
CPC分类号： 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
摘要： 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.
摘要翻译： 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：US20180065999A1
公开(公告)日：2018-03-08
申请号：US15714786
申请日：2017-09-25
发明人： Petr Vachal , Izzat Raheem , Zhiqiang Guo , Timothy John Hartingh
IPC分类号： C07F9/6561 , A61K31/675 , A61K45/06 , C07F9/16
CPC分类号： C07F9/65616 , A61K31/675 , A61K45/06 , C07F9/16
摘要： Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
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