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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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22.发明申请公开(公告)号：US20200069671A1
公开(公告)日：2020-03-05
申请号：US16674546
申请日：2019-11-05
发明人： John J. Acton, III , Jianming Bao , Melissa Egbertson , Xiaolei Gao , Scott T. Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, JR. , Zhaoyang Meng , Michael T. Rudd , Oleg B. Selyutin , David M. Tellers , Ling Tong , Jenny Miu-Chun Wai
IPC分类号： A61K31/4439 , A61P25/28 , A61P25/18 , A61P25/16 , A61K31/437 , C07D401/14 , C07D405/14 , C07D471/04
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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23.发明授权公开(公告)号：US10512638B2
公开(公告)日：2019-12-24
申请号：US16062500
申请日：2016-12-19
IPC分类号： A61K31/4439 , C07D401/14 , A61P25/28 , A61P25/18 , A61P25/16 , A61K31/437 , C07D405/14 , C07D471/04
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine 5 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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24.发明申请公开(公告)号：US20180354901A1
公开(公告)日：2018-12-13
申请号：US15780289
申请日：2016-11-29
申请人： Michael T. Rudd , David Jonathan Bennett , Jenny Wai , Zhaoyang Meng , Merck Sharp & Dohme Corp.
IPC分类号： C07D211/16 , C07D401/14 , C07D211/44 , C07D409/14 , C07D401/06 , C07D487/08 , C07D413/14 , C07D417/14 , C07D451/02
摘要： In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, 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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25.发明申请公开(公告)号：US20180305332A1
公开(公告)日：2018-10-25
申请号：US15774655
申请日：2016-11-07
发明人： Shawn J. Stachel , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Peter J. Manley , Zhaoyang Meng , Kausik K. Nanda , Michael T. Rudd , Jenny Wai
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D471/10 , C07D417/14 , C07D405/14
CPC分类号： C07D401/04 , A61K31/451 , C07D211/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/10
摘要： In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, 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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26.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：US20230018413A1
公开(公告)日：2023-01-19
申请号：US17632065
申请日：2020-08-03
发明人： Stephane L. Bogen , Ping Chen , Dane James Clausen , Jinsong Hao , Dipannita Kalyani , Michael T. Rudd , Shawn P. Walsh , Lan Wei , Dexi Yang
IPC分类号： C07D403/04 , C07D207/14 , C07D401/04 , C07D471/04 , C07D417/04 , C07D413/10 , C07D417/14 , C07D413/04 , C07D409/04 , C07D405/04 , C07D498/04 , C07D491/048
摘要： The present invention is directed to heteroaryl pyrrolidine and piperidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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公开(公告)号：US20220144771A1
公开(公告)日：2022-05-12
申请号：US17430409
申请日：2020-02-11
发明人： Stephane L. Bogen , Michael J. Breslin , Dane James Clausen , Anthony Ginnetti , Michael T. Rudd , Shawn J. Stachel , Craig A. Stump , Dexi Yang
IPC分类号： C07D207/14
摘要： The present invention is directed to pyrrolidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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29.发明授权公开(公告)号：US10752587B2
公开(公告)日：2020-08-25
申请号：US15780289
申请日：2016-11-29
IPC分类号： C07D211/16 , C07D401/14 , C07D409/14 , C07D401/06 , C07D487/08 , C07D413/14 , C07D451/02 , C07D417/14 , C07D211/46 , C07D211/10 , C07D211/54 , C07D211/44
摘要： In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, 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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30.发明授权公开(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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