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1. 发明申请

US20160002255A1 ANTIDIABETIC BICYCLIC COMPOUNDS 有权
标题翻译：抗生素双胶体化合物
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

2. 发明授权

US07091211B2 Cyclopentyl modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的环戊基调节剂
公开(公告)号：US07091211B2
公开(公告)日：2006-08-15
申请号：US10901414
申请日：2004-07-28
申请人： Paul E. Finke , Jennifer L. Loebach , Kerry A. Parker , Christopher W. Plummer , Sander G. Mills
发明人： Paul E. Finke , Jennifer L. Loebach , Kerry A. Parker , Christopher W. Plummer , Sander G. Mills
IPC分类号： A61K31/438 , C07D401/04
CPC分类号： C07D471/10 , C07D471/20 , C07D491/10 , C07D491/20 , C07D498/10
摘要： Cyclopentyl compounds of Formula (I) are modulators of chemokine receptor activity: wherein D, G, R2, R3 and R8 in Formula (I) are defined herein. The compounds, and pharmaceutically acceptable salts and individual diastereomers thereof, are useful in the treatment and prevention of HIV infection, in delaying the onset of AIDS, and in the treatment of AIDS. The compounds are also useful for treating other diseases and conditions mediated by chemokine receptors.
摘要翻译：式（I）的环戊基化合物是趋化因子受体活性的调节剂：其中式（I）中的D，G，R 2，R 3和R 8 （I）在本文中定义。化合物及其药学上可接受的盐和单独的非对映异构体可用于治疗和预防艾滋病毒感染，延缓艾滋病的发病和艾滋病的治疗。该化合物也可用于治疗趋化因子受体介导的其它疾病和病症。

3. 发明申请

US20170081287A1 ANTIDIABETIC TRICYCLIC COMPOUNDS 有权
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.

4. 发明申请

US20210395255A1 SUBSTITUTED AMINO TRIAZOLOPYRIMIDINE AND AMINO TRIAZOLOPYRAZINE ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE 有权
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.

5. 发明授权

US10059667B2 Antidiabetic compounds 有权
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.

6. 发明申请

US20170217918A1 ANTIDIABETIC BICYCLIC COMPOUNDS 审中-公开
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.

7. 发明申请

US20230054411A1 7-, 8-, and 10-SUBSTITUTED AMINO TRIAZOLO QUINAZOLINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE 有权
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.

8. 发明授权

US07572785B2 Substituted imidazoles as cannabinoid receptor modulators 失效
标题翻译：取代的咪唑作为大麻素受体调节剂
公开(公告)号：US07572785B2
公开(公告)日：2009-08-11
申请号：US11265850
申请日：2005-11-03
申请人： Paul E. Finke , Sander G. Mills , Christopher W. Plummer , Shrenik K. Shah , Quang T. Truong
发明人： Paul E. Finke , Sander G. Mills , Christopher W. Plummer , Shrenik K. Shah , Quang T. Truong
IPC分类号： A61K31/55 , C07D405/00 , C07D413/00
CPC分类号： C07D405/12 , C07D233/90
摘要： The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith. Novel compounds of structural formula (I) are also claimed.
摘要翻译：使用本发明的化合物作为大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，特别是用于治疗，预防和抑制由大麻素-1（CB1）受体介导的疾病。本发明涉及这些新化合物选择性拮抗大麻素-1（CB1）受体的用途。因此，本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症的精神药物。血管意外和头部创伤，焦虑障碍，压力，癫痫，帕金森病和精神分裂症。这些化合物也可用于治疗药物滥用障碍，特别是鸦片剂，酒精和尼古丁。所述化合物还可用于治疗与过量食物摄入和与其相关的并发症相关的肥胖或进食障碍。还要求新的结构式（I）化合物。

9. 发明授权

US07057051B2 Substituted imidazoles as cannabinoid receptor modulators 失效
公开(公告)号：US07057051B2
公开(公告)日：2006-06-06
申请号：US10198442
申请日：2002-07-17
申请人： Paul E. Finke , Sander G. Mills , Christopher W. Plummer , Shrenik K. Shah , Quang T. Truong
发明人： Paul E. Finke , Sander G. Mills , Christopher W. Plummer , Shrenik K. Shah , Quang T. Truong
IPC分类号： C07D233/28
CPC分类号： C07D405/12 , C07D233/90
摘要： The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith. Novel compounds of structural formula (I) are also claimed.

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