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公开(公告)号：US11225471B2
公开(公告)日：2022-01-18
申请号：US15733056
申请日：2018-11-12
申请人： Steven L. Colletti , Duane DeMong , Kevin D. Dykstra , Zhiyong Hu , Michael Miller , Merck Sharp & Dohme Corp.
IPC分类号： C07D405/14 , A61P3/10
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 Formula (I).
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公开(公告)号：US20210094938A1
公开(公告)日：2021-04-01
申请号：US15733056
申请日：2018-11-12
申请人： Steven L. COLLETTI , Duane DEMONG , Kevin D. DYKSTRA , Zhiyong HU , Michael MILLER , Merck Sharp & Dohme Corp.
IPC分类号： C07D405/14 , A61P3/10
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 Formula (I).
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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：US09718818B2
公开(公告)日：2017-08-01
申请号：US14912761
申请日：2014-08-18
申请人： MERCK SHARP & DOHME CORP. , Duane DeMong , Thomas J. Greshock , Ronald K. Chang , Xing Dai , Hong Liu , John A. McCauley , Wei Li , Kallol Basu , Jack D. Scott , Michael Miller
发明人： Duane DeMong , Thomas J. Greshock , Ronald K. Chang , Xing Dai , Hong Liu , John A. McCauley , Wei Li , Kallol Basu , Jack D. Scott , Michael Miller
IPC分类号： A61K31/44 , C07D471/04 , C07D498/04 , C07D519/00 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00
摘要： The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
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公开(公告)号：US20160200722A1
公开(公告)日：2016-07-14
申请号：US14912761
申请日：2014-08-18
申请人： Duane DEMONG , Thomas J. GRESHOCK , Ronald K. CHANG , Xing DAI , Hong LIU , John A. MCCAULEY , Wei LI , Kallol BASU , Jack D. SCOTT , Michael MILLER , MERCK SHARP & DOHME CORP.
发明人： Duane DeMong , Thomas J. Greshock , Ronald K. Chang , Xing Dai , Hong Liu , John A. McCauley , Wei Li , Kallol Basu , Jack D. Scott , Michael Miller
IPC分类号： C07D471/04 , C07D498/04 , C07D519/00
CPC分类号： C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00
摘要： The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
摘要翻译： 本发明涉及作为LRRK2激酶的有效抑制剂并且可用于治疗或预防涉及LRRK2激酶的疾病（例如帕金森病）的唑烷化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及LRRK-2激酶的疾病中的用途。
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公开(公告)号：US20160009696A1
公开(公告)日：2016-01-14
申请号：US14772290
申请日：2014-02-27
申请人： Michael MILLER , Kallol BASU , Duane DEMONG , Jack SCOTT , Wei LI , Joel HARRIS , Andrew STAMFORD , Marc POIRIER , Paul TEMPEST , MERCK SHARP & DOHME CORP.
发明人： Michael Miller , Kallol Basu , Duane DeMong , Jack Scott , Wei Li , Joel Harris , Andrew Stamford , Marc Poirier , Paul Tempest
IPC分类号： C07D403/14 , C07D401/14 , C07D491/107 , C07D417/14 , C07D471/10 , C07D413/14 , C07D498/08
CPC分类号： C07D403/14 , A61K31/505 , A61K31/506 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10 , C07D491/107 , C07D498/08
摘要： The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
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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：US20160009689A1
公开(公告)日：2016-01-14
申请号：US14772295
申请日：2014-02-27
申请人： Michael MILLER , Kallol BASU , Duane DEMONG , Jack SCOTT , Wei LI , Andrew STAMFORD , Marc POIRIER , Paul TEMPEST , MERCK SHARP & DOHME CORP.
发明人： Michael Miller , Kallol Basu , Duane DeMong , Jack Scott , Wei Li , Andrew Stamford , Marc Poirer , Paul Tempest
IPC分类号： C07D403/04 , C07D413/14 , C07D401/14 , C07D471/10 , C07D491/107 , C07D498/10 , C07D487/10 , C07D405/14 , C07D498/04 , C07D487/04 , C07D409/14 , C07D403/14 , C07D498/08
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107 , C07D498/04 , C07D498/08 , C07D498/10
摘要： The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
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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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