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1.发明授权公开(公告)号：US11339156B2
公开(公告)日：2022-05-24
申请号：US16621953
申请日：2018-06-22
发明人： John J. Acton, III , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Timothy J. Henderson , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Meng Na , Michael T. Rudd , Oleg B. Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang , Takao Suzuki
IPC分类号： C07D471/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D417/14
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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2.发明授权公开(公告)号：US11149036B2
公开(公告)日：2021-10-19
申请号：US16621959
申请日：2018-06-22
申请人： John J. Acton, III , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd. , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
发明人： John J. Acton, III , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
IPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D491/048 , C07D498/04
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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3.发明授权公开(公告)号：US10933056B2
公开(公告)日：2021-03-02
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： C07D401/14 , C07D405/14 , C07D471/04 , A61K31/4439 , A61P25/28 , A61P25/18 , A61P25/16 , A61K31/437
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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4.发明授权公开(公告)号：US10981902B2
公开(公告)日：2021-04-20
申请号：US16621943
申请日：2018-06-22
发明人： Jianming Bao , Timothy J. Henderson , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Meng Na , Michael T. Rudd , David M. Tellers , Ling Tong
IPC分类号： C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention is directed to 5-(pyridine-3-yl)oxaxole 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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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：US20140296136A1
公开(公告)日：2014-10-02
申请号：US14358050
申请日：2012-11-09
申请人： MERCK SHARP & DOHME CORP. , MERCK CANADA INC. , ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.R.L.
发明人： Michael T. Rudd , John McCauley , Nigel Liverton , Christiane Grisé-Bard , Marie-Christine Brochu , Sylvie Charron , Virender Aulakh , Benoit Bachand , Patrick Beaulieu , Helmi Zaghdane , Yongxin Han , Marco Ferrara , Steven Harper , Vincenzo Summa , Samuel Chackalamannil , Srikanth Venkatraman , Unmesh Shah , Francisco Velazquez
IPC分类号： C07K5/08 , A61K31/4745 , A61K31/7056 , A61K31/5377 , A61K38/06 , A61K38/00 , A61K31/675
CPC分类号： C07K5/08 , A61K31/4745 , A61K31/5377 , A61K31/675 , A61K31/7056 , A61K38/005 , A61K38/06 , A61K38/12 , A61K38/21 , C07K5/0804 , C07K5/0808 , C07K5/0812 , C07K5/0821 , A61K2300/00
摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。
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公开(公告)号：US20230365533A1
公开(公告)日：2023-11-16
申请号：US18040896
申请日：2021-08-16
申请人： Stephane L. BOGEN , Dane James CLAUSEN , Deodial Guy GUIADEEN , Jinsong HAO , Shishi LIN , Michael T. RUDD , Lan WEI , Li XIAO , Dexi YANG , MERCK SHARP & DOHME CORP.
发明人： Stephane L. Bogen , Dane James Clausen , Deodial Guy Guiadeen , Jinsong Hao , Shishi Lin , Michael T. Rudd , Lan Wei , Li Xiao , Dexi Yang
IPC分类号： C07D403/12 , C07D403/14 , C07D417/12 , C07D491/048
CPC分类号： C07D403/12 , C07D403/14 , C07D417/12 , C07D491/048
摘要： The present invention is directed to bicyclo[4.1 0]heptane pyrrolidine compounds of formula (I) 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.
where
is
wherein n is 0 or 1;-
公开(公告)号：US20210260082A1
公开(公告)日：2021-08-26
申请号：US17260619
申请日：2019-07-15
IPC分类号： A61K31/675 , C07F9/6561 , A61P31/18 , A61K31/52 , A61K31/7068 , A61K31/7072 , A61K31/341 , A61K31/496 , A61K31/513 , A61K31/427 , A61K31/635 , A61K31/4439 , A61K31/536
摘要： Compounds of Formula I: 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：US11098029B2
公开(公告)日：2021-08-24
申请号：US16787201
申请日：2020-02-11
IPC分类号： C07D401/14 , C07D207/16 , C07D403/12 , C07D409/12
摘要： The present invention is directed to 5-alkyl 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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公开(公告)号：US10961215B2
公开(公告)日：2021-03-30
申请号：US16341602
申请日：2017-10-09
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
IPC分类号： C07D401/04 , C07D211/26 , C07D405/14
摘要： In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be 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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