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1.发明申请公开(公告)号：US20210395224A1
公开(公告)日：2021-12-23
申请号：US17286591
申请日：2019-10-24
发明人： John J. Acton, III , Melissa Egbertson , Xiaolei Gao , Scott T. Harrison , Timothy J. Henderson , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , James Mulhearn , Vanessa L. Rada , Jeffrey W. Schubert , Oleg B. Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang , Jianming Bao , Chunsing Li
IPC分类号： C07D401/14 , C07D405/14
摘要： The present invention is directed to cinnolinyl and quinolinyl 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：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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3.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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4.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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5.发明授权公开(公告)号：US11970479B2
公开(公告)日：2024-04-30
申请号：US17286591
申请日：2019-10-24
发明人： John J. Acton, III , Melissa Egbertson , Xiaolei Gao , Scott T. Harrison , Timothy J. Henderson , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , James Mulhearn , Vanessa L. Rada , Jeffrey W. Schubert , Oleg B. Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang , Jianming Bao , Chunsing Li
IPC分类号： C07D401/14 , C07D405/14
CPC分类号： C07D401/14 , C07D405/14
摘要： The present invention is directed to cinnolinyl and quinolinyl 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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6.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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7.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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公开(公告)号：US09868727B2
公开(公告)日：2018-01-16
申请号：US15329634
申请日：2015-07-23
发明人： Weiguo Liu , Scott D. Edmondson , Zhuyan Guo , Sung-Sau So , Anthony K. Ogawa , Rongze Kuang , Heping Wu , Amjad Ali , Ying-Duo Gao , Yu Jiang , Chunsing Li , Tingting Yu
IPC分类号： C07D409/14 , C07D417/14 , C07D413/14 , C07D401/14 , C07D401/06 , A61K31/4439 , A61K31/444
CPC分类号： C07D409/14 , A61P7/02 , C07D401/06 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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9.发明申请SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 有权磺酰胺衍生物及其用于改善药物药物动力学的方法公开(公告)号：US20150197531A1
公开(公告)日：2015-07-16
申请号：US14410846
申请日：2013-06-25
发明人： Craig A. Coburn , Milana Maletic , Richard Soll , Chunsing Li , Yunfu Luo , Zhiqi Qi
IPC分类号： C07D498/04 , A61K31/496 , C07D471/10 , C07D417/14 , A61K31/4402 , A61K31/4985 , A61K31/5383 , A61K31/5377 , A61K45/06 , A61K31/513 , C07D417/12 , C07D487/04
CPC分类号： C07D498/04 , A61K31/4402 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5377 , A61K31/5383 , A61K38/05 , A61K45/06 , C07D401/14 , C07D403/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/04
摘要： The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
摘要翻译： 本发明涉及式（I）的磺酰胺衍生物及其药学上可接受的盐，其中A，W，X，R 1，R 2，R 3，R 4和R 5如本文所定义。 本发明还涉及包含至少一种磺酰胺衍生物的组合物，以及使用磺酰胺衍生物来改善药物的药代动力学的方法。
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10.发明申请SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 审中-公开磺酰胺衍生物及其用于改善药物药物动力学的方法公开(公告)号：US20140005103A1
公开(公告)日：2014-01-02
申请号：US13926481
申请日：2013-06-25
发明人： Craig A. Coburn , Milana Maletic , Richard Soll , Chunsing Li , Yunfu Luo , Zhiqi Qi
IPC分类号： A61K31/496 , C07D471/10 , C07D471/04 , A61K31/4985 , A61K38/05 , A61K31/5383 , A61K31/5377 , C07D487/04 , A61K31/513 , C07D417/12 , C07D498/04
CPC分类号： C07D498/04 , A61K31/4402 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5377 , A61K31/5383 , A61K38/05 , A61K45/06 , C07D401/14 , C07D403/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/04
摘要： The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
摘要翻译： 本发明涉及式（I）的磺酰胺衍生物及其药学上可接受的盐，其中A，W，X，R 1，R 2，R 3，R 4和R 5如本文所定义。 本发明还涉及包含至少一种磺酰胺衍生物的组合物，以及使用磺酰胺衍生物来改善药物的药代动力学的方法。
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