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1.
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:US10822338B2
公开(公告)日:2020-11-03
申请号:US15738178
申请日:2016-07-05
发明人: Amjad Ali , Xianhai Huang , Yeon-Hee Lim , Rongze Kuang , Heping Wu , Rajan Anand , Younong Yu , Edward Metzger , Michael Man-Chu Lo , Pauline C. Ting , Andrew W. Stamford , Paul Tempest
IPC分类号: C07D487/04 , C07D491/153
摘要: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, 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:US10351564B2
公开(公告)日:2019-07-16
申请号:US16176608
申请日:2018-10-31
IPC分类号: C07D471/04 , C07D519/00 , C07D491/052 , C07D491/048 , C07D471/08 , C07F9/22 , A61K31/437 , A61P25/00
摘要: The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one 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:US09745282B2
公开(公告)日:2017-08-29
申请号:US15197957
申请日:2016-06-30
发明人: Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Lina Yin , Rolf Hartmann , Qingzhong Hu , Ralf Heim , Christina Zimmer
IPC分类号: C07D401/04 , A61K31/4709 , A61K31/4439 , A61K45/06 , C07D409/14 , A61K31/4725
CPC分类号: C07D401/04 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D409/14 , A61K2300/00
摘要: This invention relates to indoline compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
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公开(公告)号:US20160214997A1
公开(公告)日:2016-07-28
申请号:US14914843
申请日:2014-08-25
申请人: Amjad ALI , Gioconda V. GALLO , Timothy J. HENDERSON , Rongze KUANG , Yeon-Hee LIM , Michael Man-Chu LO , Edward METZGER , Manuel de Lera RUIZ , Andrew STAMFORD , Paul TEMPEST , Brent WHITEHEAD , Heping WU , MERCK SHARP & DOHME CORP.
发明人: Ali Amjad , Gioconda V. Gallo , Timothy J. Henderson , Rongze Kuang , Yeon-Hee Lim , Michael Man-Chu Lo , Edward Metzger , Manuel de Lera Ruiz , Andrew Stamford , Paul Tempest , Brent Whitehead , Heping Wu
IPC分类号: C07D519/00 , C07D491/147
CPC分类号: C07D519/00 , C07D491/147
摘要: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.
摘要翻译: 本发明涉及作为A2A受体拮抗剂的2,2-二氟二氧代己基化合物。 本发明还涉及本文所述的2,2-二氟二氧代环戊基化合物在涉及A2A受体的神经障碍和疾病的潜在治疗或预防中的用途。 本发明还涉及包含这些化合物的药物组合物以及这些药物组合物用于预防或治疗其中涉及A2A受体的疾病的用途。
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6.
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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公开(公告)号:US20180037554A1
公开(公告)日:2018-02-08
申请号:US15549242
申请日:2016-02-01
发明人: Amjad Ali , Rongze Kuang , Yeon-Hee Lim , Michael Man-Chu Lo , Pauline C. Ting , Purakkattle Biju , Manuel de Lera Ruiz , Sylvia J. Degrado , Alexander L. Tung , Timothy J. Henderson , Liwu Hong , Jae-Hun Kim , Dong Won-Shik Kim , Joe Lee , Jie Wu , Heping Wu , Yushi Xiao , Tao Yu , Gang Zhou , Xiaohong Zhu , Kevin D. McCormick , Jayaram R. Tagat , Dong Xiao , Tanweer Khan , Jianhua Cao , Michael Berlin , Yonglian Zhang
IPC分类号: C07D239/84 , C07D401/14 , C07D413/12 , C07D417/12 , C07D405/12 , C07D417/14 , C07D413/14 , C07D471/04 , C07D401/12 , C07D403/12
CPC分类号: C07D239/84 , A61K31/517 , A61P25/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要: The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.
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8.
公开(公告)号:US20170197991A1
公开(公告)日:2017-07-13
申请号:US15423238
申请日:2017-02-02
发明人: Amjad Ali , Michael Man-Chu Lo , Yeon-Hee Lim , Andrew Stamford , Rongze Kuang , Paul Tempest , Younong Yu , Xianhai Huang , Timothy J. Henderson , Jae-Hun Kim , Christopher Boyce , Pauline Ting , Junying Zheng , Edward Metzger , Nicolas Zorn , Dong Xiao , Gioconda V. Gallo , Walter Won , Heping Wu , Qiaolin Deng
IPC分类号: C07D519/00 , C07D487/04
CPC分类号: C07D519/00 , C07D487/04
摘要: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
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公开(公告)号:US11230556B2
公开(公告)日:2022-01-25
申请号:US16471672
申请日:2017-12-18
发明人: Xiaolei Gao , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Debra L. Ondeyka
IPC分类号: C07D498/04 , C07D471/04 , C07D487/04 , C07D491/048 , C07D513/04 , C07D471/14 , C07D498/14 , C07D401/14
摘要: The present invention is directed to 6,5-fused heteroarylpiperidine ether 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:US11046714B2
公开(公告)日:2021-06-29
申请号:US14914843
申请日:2014-08-25
申请人: Merck Sharp & Dohme Corp. , Ali Amjad , Gioconda V. Gallo , Timothy J. Henderson , Rongze Kuang , Yeon-Hee Lim , Michael Man-Chu Lo , Edward Metzger , Manuel de Lera Ruiz , Andrew Stamford , Paul Tempest , Brent Whitehead , Heping Wu
发明人: Ali Amjad , Gioconda V. Gallo , Timothy J. Henderson , Rongze Kuang , Yeon-Hee Lim , Michael Man-Chu Lo , Edward Metzger , Manuel de Lera Ruiz , Andrew Stamford , Paul Tempest , Brent Whitehead , Heping Wu
IPC分类号: C07D519/00 , C07D491/147
摘要: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.
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