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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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公开(公告)号：US11566057B2
公开(公告)日：2023-01-31
申请号：US16643881
申请日：2018-09-21
发明人： Anandan Palani , Qiaolin Deng , Chunhui Huang , Yuping Zhu , Elisabetta Bianchi , Federica Orvieto
摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
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公开(公告)号：US11492385B2
公开(公告)日：2022-11-08
申请号：US17003921
申请日：2020-08-26
发明人： Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
IPC分类号： A61K38/00 , A61K38/28 , A61P3/04 , A61P7/12 , A61P3/10 , C07K14/435 , C07K14/605
摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
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![PIPERAZINE-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES](/abs-image/US/2016/07/07/US20160194330A1/abs.jpg.150x150.jpg)
5.发明申请PIPERAZINE-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 有权哌嗪取代[1,2,4]三唑[1,5-C]喹唑啉-5-胺化合物，具有A2A拮抗剂性质公开(公告)号：US20160194330A1
公开(公告)日：2016-07-07
申请号：US14655572
申请日：2013-12-20
申请人： Amjad ALI , Michael Man-Chu LO , Yeon-Hee LIM , Andrew STAMFORD , Rongze KUANG , Paul TEMPEST , Younong YU , Michael BERLIN , Pauline TING , Gang ZHOU , Tao YU , Christopher BOYCE , Joseph Michael KELLY , Jayaram TAGAT , Junying ZHENG , Xianhai HUANG , Wei ZHOU , Jae-Hun KIM , Nicolas ZORN , Dong XIAO , Gioconda V. GALLO , Walter WON , Heping WU , Rajan ANAND , MERCK SHARP & DOHME CORP.
发明人： Amjad Ali , Michael Man-Chu Lo , Yeon-Hee Lim , Andrew Stamford , Rongze Kuang , Paul Tempest , Younong Yu , Michael Berlin , Pauline Ting , Gang Zhou , Tao Yu , Christopher Boyce , Joseph Michael Kelly , Jayaram R. Tagat , Junying Zheng , Xianhai Huang , Wei Zhou , Jae-Hun Kim , Nicolas Zorn , Dong Xiao , Gioconda V. Gallo , Walter Won , Heping Wu , Rajan Anand , Qiaolin Deng
IPC分类号： C07D487/04 , C07D487/18 , C07D487/08 , C07D513/04
CPC分类号： C07D487/04 , C07D487/08 , C07D487/18 , C07D513/04
摘要： Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” 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.
摘要翻译： 公开了式A化合物（结构表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。
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公开(公告)号：US20230054411A1
公开(公告)日：2023-02-23
申请号：US17294836
申请日：2019-11-26
申请人： Yonglian ZHANG , Amjad ALI , Jared CUMMING , Duane DEMONG , Qiaolin DENG , Thomas H. GRAHAM , Elisabeth HENNESSY , Matthew A. LARSEN , Kun LIU , Ping LIU , Umar Faruk MANSOOR , Jianping PAN , Christopher W. PLUMMER , Aaron SATHER , Uma SWAMINATHAN , Huijun WANG , Merck Sharp & Dohme Corp.
发明人： Yonglian Zhang , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Elisabeth Hennessy , Matthew A. Larsen , Kun Liu , Ping Liu , Umar Faruk Mansoor , Jianping Pan , Christopher W. Plummer , Aaron Sather , Uma Swaminathan , Huijun Wang
IPC分类号： A61K31/519 , A61K39/395 , C07D471/04 , C07D519/00 , A61K31/55
摘要： In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
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公开(公告)号：US20200270325A1
公开(公告)日：2020-08-27
申请号：US16643881
申请日：2018-09-21
发明人： Anandan Palani , Qiaolin Deng , Chunhui Huang , Yuping Zhu , Elisabetta Bianchi , Federica Orvieto
IPC分类号： C07K14/605 , C07K14/62 , A61P3/10
摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
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公开(公告)号：US20190338008A1
公开(公告)日：2019-11-07
申请号：US15759911
申请日：2016-10-21
申请人： Anandan PALANI , Ravi NARGUND , Paul E. CARRINGTON , Tomi SAWYER , Qiaolin DENG , Antonello PESSI , Elisabetta BIANCHI , Fe-derica ORYIETO , Merck Sharp & Dohme Corp.
发明人： Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
IPC分类号： C07K14/605 , A61P3/04 , A61K38/28
摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
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公开(公告)号：US20220220117A1
公开(公告)日：2022-07-14
申请号：US17657515
申请日：2022-03-31
发明人： Matthew A. Larsen , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Elisabeth Hennessy , Andrew J. Hoover , Ping Liu , Kun Liu , Umar Faruk Mansoor , Jianping Pan , Christopher W. Plummer , Aaron Sather , Uma Swaminathan , Huijun Wang , Yonglian Zhang
IPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
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公开(公告)号：US20210107904A1
公开(公告)日：2021-04-15
申请号：US16695367
申请日：2019-11-26
发明人： Matthew A. Larsen , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Elisabeth Hennessy , Andrew J. Hoover , Ping Liu , Kun Liu , Umar Faruk Mansoor , Jianping Pan , Christopher W. Plummer , Aaron Sather , Uma Swaminathan , Huijun Wang , Yonglian Zhang
IPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
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