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公开(公告)号:US20170217918A1
公开(公告)日:2017-08-03
申请号:US15328735
申请日:2015-08-06
申请人: Helen CHEN , Steven L. COLLETTI , Duane MONG , Yan GUO , Michael MILLER , Anilkumar NAIR , Christopher W. PLUMMER , Dong XIAO , De-Yi YANG , Merck Sharp & Dohme Corp.
发明人: Helen Chen , Steven L. Colletti , Duane DeMong , Yan Guo , Michael Miller , Anilkumar Nair , Christopher W. Plummer , Dong Xiao , De-Yi Yang
IPC分类号: C07D311/60 , C07D405/14 , C07D471/08 , C07D487/08 , C07D487/04 , C07D491/107 , C07D413/12 , C07D491/08 , C07D405/10 , C07D491/048
CPC分类号: C07D311/60 , A61K31/366 , A61K31/397 , A61K31/4985 , A61K45/06 , C07D405/10 , C07D405/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/048 , C07D491/08 , C07D491/107 , A61K2300/00
摘要: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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公开(公告)号:US20160002255A1
公开(公告)日:2016-01-07
申请号:US14767815
申请日:2014-02-20
申请人: Linda L. BROCKUNIER , Helen CHEN , Harry R. CHOBANIAN , Matthew J. CLEMENTS , Alejandro CRESPO , Duane E. DEMONG , Yan GUO , William K. HAGMANN , Karen M. MARCANTONIO , Michael MILLER , Barbara PIO , Christopher W. PLUMMER , Dong XIAO , MERCK SHARP & DOHME CORP.
发明人: Linda L. Brockunier , Helen Chen , Harry R. Chobanian , Matthew J. H. Clements , Alejandro Crespo , Duane E. DeMong , Yan Guo , William K. Hagmann , Karen M. Marcantonio , Michael Miller , Barbara Pio , Christopher W. Plummer , Dong Xiao
IPC分类号: C07D493/04 , A61K31/352 , C07D405/04 , A61K31/4433 , C07D311/28 , C07D417/04 , A61K31/427 , C07D491/052 , A61K31/436 , C07D405/14 , A61K31/444 , C07D413/10 , A61K31/422 , C07D405/10 , A61K31/416 , A61K31/497 , A61K31/538 , A61K45/06 , C07D311/04
CPC分类号: C07D493/04 , A61K31/352 , A61K31/416 , A61K31/422 , A61K31/427 , A61K31/436 , A61K31/4433 , A61K31/444 , A61K31/497 , A61K31/538 , A61K45/06 , C07D201/00 , C07D311/04 , C07D311/28 , C07D319/20 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/14 , C07D413/10 , C07D417/04 , C07D491/048 , C07D491/052
摘要: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译: 结构式(I)的新型化合物及其药学上可接受的盐是G蛋白偶联受体40(GPR40)的激动剂,可用于治疗,预防和抑制G蛋白偶联受体 受体40.本发明的化合物可用于治疗2型糖尿病,以及通常与该疾病相关的病症,包括肥胖症和脂质疾病,例如混合或糖尿病性血脂异常,高脂血症,高胆固醇血症和 高甘油三酯血症
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公开(公告)号:US10059667B2
公开(公告)日:2018-08-28
申请号:US15110894
申请日:2015-02-03
申请人: MERCK SHARP & DOHME CORP. , Harry Chobanian , Duane DeMong , Yan Guo , Zhiyong Hu , Michael Miller , Barbara Pio , Christopher W. Plummer , Dong Xiao , Cangming Yang , Rui Zhang
发明人: Harry Chobanian , Duane DeMong , Yan Guo , Zhiyong Hu , Michael Miller , Barbara Pio , Christopher W. Plummer , Dong Xiao , Cangming Yang
IPC分类号: C07D211/42 , A61K45/06 , A61K31/366 , A61K31/397 , A61K31/40 , A61K31/44 , C07D231/20 , A61K31/4985 , C07D401/04 , C07D239/52 , C07C217/52 , C07D205/04 , C07D491/056 , C07D265/30 , C07D207/08 , C07D207/10 , C07D207/12 , C07D209/52 , C07D209/54 , C07D211/22 , C07D213/30 , C07D213/64 , C07D213/65 , C07D213/69 , C07D307/86 , C07D307/88 , C07C59/72 , C07D205/12 , C07D213/647
CPC分类号: C07D211/42 , A61K31/366 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/4985 , A61K45/06 , C07C59/72 , C07C217/52 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07D205/04 , C07D205/12 , C07D207/08 , C07D207/10 , C07D207/12 , C07D209/52 , C07D209/54 , C07D211/22 , C07D213/30 , C07D213/64 , C07D213/647 , C07D213/65 , C07D213/69 , C07D231/20 , C07D239/52 , C07D265/30 , C07D307/86 , C07D307/88 , C07D401/04 , C07D491/056 , A61K2300/00
摘要: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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公开(公告)号:US20160332968A1
公开(公告)日:2016-11-17
申请号:US15110894
申请日:2015-02-03
申请人: Harry CHOBANIAN , Duane DEMONG , Yan Guo , Zhiyong Hu , Barbara PIO , Christopher PLUMMER , Dong XIAO , Cangming YANG , Rui ZHANG , Merck Sharp & Dohme Corp. , Michael MILLER
发明人: Harry Chobanian , Duane DeMong , Yan Guo , Zhiyong Hu , Michael Miller , Barbara Pio , Christopher W. Plummer , Dong Xiao , Michael Yang
IPC分类号: C07D211/42 , C07D211/22 , C07D205/04 , C07D209/54 , C07D209/52 , C07D207/12 , C07D205/12 , C07C217/52 , C07D401/04 , C07D265/30 , C07C59/72 , C07D213/64 , C07D213/69 , C07D239/52 , C07D231/20 , C07D307/88 , C07D491/056 , C07D307/86 , C07D213/30 , C07D213/647 , C07D207/08
CPC分类号: C07D211/42 , A61K31/366 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/4985 , A61K45/06 , C07C59/72 , C07C217/52 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07D205/04 , C07D205/12 , C07D207/08 , C07D207/10 , C07D207/12 , C07D209/52 , C07D209/54 , C07D211/22 , C07D213/30 , C07D213/64 , C07D213/647 , C07D213/65 , C07D213/69 , C07D231/20 , C07D239/52 , C07D265/30 , C07D307/86 , C07D307/88 , C07D401/04 , C07D491/056 , A61K2300/00
摘要: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译: 结构式(I)的新型化合物及其药学上可接受的盐是G蛋白偶联受体40(GPR40)的激动剂,可用于治疗,预防和抑制G蛋白偶联受体 受体40.本发明的化合物可用于治疗2型糖尿病,以及通常与该疾病相关的病症,包括肥胖症和脂质疾病,例如混合或糖尿病性血脂异常,高脂血症,高胆固醇血症和 高甘油三酯血症
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公开(公告)号:US20170081287A1
公开(公告)日:2017-03-23
申请号:US15310488
申请日:2015-05-19
申请人: Tesfaye BIFTU , Purakkattle BIJU , Timothy A. BLIZZARD , Zhengxia CHEN , Matthew J. CLEMENTS , Mingxiang CUI , Jessica L. FRIE , William K. HAGMANN , Bin HU , Hubert JOSIEN , Anilkumar G. NAIR , Christopher W. PLUMMER , Cheng ZHU , Merck Sharp & Dohme Corp.
发明人: Tesfaye Biftu , Purakkattle Biju , Timothy A. Blizzard , Zhengxia Chen , Matthew J. Clements , Mingxiang Cui , Jessica L. Frie , William K. Hagmann , Bin Hu , Hubert Josien , Anilkumar G. Nair , Christopher W. Plummer , Cheng Zhu
IPC分类号: C07D221/16 , A61K31/438 , C07D405/12 , C07D401/12 , A61K31/444 , C07C61/39 , A61K31/192 , A61K31/4725 , A61K31/4709 , A61K31/538 , C07D413/12 , A61K31/55 , C07D215/14 , A61K31/47 , C07D401/04 , A61K45/06
CPC分类号: C07D221/16 , A61K31/192 , A61K31/366 , A61K31/397 , A61K31/435 , A61K31/438 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4985 , A61K31/538 , A61K31/55 , A61K45/06 , C07C61/39 , C07C2602/08 , C07C2603/12 , C07D215/14 , C07D401/04 , C07D401/12 , C07D405/12 , C07D413/12 , A61K2300/00
摘要: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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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:US20210395255A1
公开(公告)日:2021-12-23
申请号:US17292511
申请日:2019-11-15
申请人: Zachary G. BRILL , Amjad ALI , Jared CUMMING , Duane DEMONG , Qiaolin DENG , Thomas H. GRAHAM , Rongze KUANG , Yeon-Hee LIM , Christopher W. PLUMMER , Jenny Lorena RICO DUQUE , Huijun WANG , Yonglian ZHANG , Kake ZHAO , Merck Sharp & Dohme Corp.
发明人: Zachary G. Brill , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Rongze Kuang , Yeon-Hee Lim , Christopher W. Plummer , Jenny Lorena Rico Duque , Huijun Wang , Yonglian Zhang , Kake Zhao
IPC分类号: C07D487/04 , C07K16/28
摘要: In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): or and pharmaceutically acceptable salts thereof, wherein, R1, R2, and R3 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 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:US20190161448A1
公开(公告)日:2019-05-30
申请号:US16096710
申请日:2017-05-19
发明人: Gregory L. Adams , Jason M. Cox , John S. Debenham , Scott Edmondson , Eric J. Gilbert , Yan Guo , Yu Jiang , Hubert Josien , Hyunjin M. Kim , Ping Lan , Shouwu Miao , Christopher W. Plummer , Murali Rajagopalan , Unmesh Shah , Zhongxiang Sun , Quang T. Truong , Feroze Ujjainwalla , Francisco Velazquez , Srikanth Venkatraman , Takao Suzuki , Nengxue Wang
IPC分类号: C07D217/04 , C07D401/12 , C07D401/04 , C07D401/06 , C07D417/04 , C07D417/14 , C07D417/12 , C07D413/04 , A61P3/10 , A61P3/06 , A61P3/04 , A61P29/00
摘要: The present invention relates to a compound represented by formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
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公开(公告)号:US10000454B2
公开(公告)日:2018-06-19
申请号:US15310488
申请日:2015-05-19
发明人: Tesfaye Biftu , Purakkattle Biju , Timothy A. Blizzard , Zhengxia Chen , Matthew J. Clements , Mingxiang Cui , Jessica L. Frie , William K. Hagmann , Bin Hu , Hubert Josien , Anilkumar G. Nair , Christopher W. Plummer , Cheng Zhu
IPC分类号: C07D221/16 , A61K31/435 , A61K31/444 , C07D401/12 , C07D405/12 , A61K31/192 , A61K31/438 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/538 , A61K31/55 , A61K45/06 , C07C61/39 , C07D215/14 , C07D401/04 , C07D413/12
CPC分类号: C07D221/16 , A61K31/192 , A61K31/366 , A61K31/397 , A61K31/435 , A61K31/438 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4985 , A61K31/538 , A61K31/55 , A61K45/06 , C07C61/39 , C07C2602/08 , C07C2603/12 , C07D215/14 , C07D401/04 , C07D401/12 , C07D405/12 , C07D413/12 , A61K2300/00
摘要: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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公开(公告)号:US20160280626A1
公开(公告)日:2016-09-29
申请号:US15034189
申请日:2014-12-01
发明人: Thomas Bara , Harry R. Chobanian , Yan Guo , Hubert Josien , Michael Miller , Barbara Pio , Christopher W. Plummer , Cangming Yang , Dong Xiao
IPC分类号: C07C59/72 , C07D213/64 , A61K31/44 , C07D209/08 , A61K31/404 , C07D231/12 , A61K31/415 , C07D417/04 , A61K31/427 , C07D471/04 , A61K31/437 , C07D249/04 , A61K31/4192 , C07D333/24 , A61K31/381 , C07C255/59 , A61K31/277 , C07D221/04 , A61K31/435 , A61K45/06 , A61K31/192
CPC分类号: C07C59/72 , A61K31/192 , A61K31/277 , A61K31/381 , A61K31/404 , A61K31/415 , A61K31/4192 , A61K31/427 , A61K31/435 , A61K31/437 , A61K31/44 , A61K45/06 , C07C255/59 , C07C2601/02 , C07C2601/14 , C07C2602/06 , C07C2602/08 , C07D207/333 , C07D209/08 , C07D209/12 , C07D213/64 , C07D221/04 , C07D231/12 , C07D249/04 , C07D277/42 , C07D333/24 , C07D417/04 , C07D471/04 , A61K2300/00
摘要: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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