公开(公告)号：US20150191495A1

公开(公告)日：2015-07-09

申请号：US14418147

申请日：2013-07-31

申请人： Merck Sharp & Dohme Corp.

发明人： William K. Hagmann ,  Ravi P. Nargund ,  Timothy A. Blizzard ,  Hubert Josien ,  Purakkattle Biju ,  Christopher W. Plummer ,  Qun Dang ,  Bing Li ,  Derun Li ,  Linus S. Lin ,  Mingxiang Cui ,  Bin Hu ,  Jinglai Hao ,  Zhengxia Chen

IPC分类号： C07F9/58 ,  A61K31/4427 ,  C07D221/16 ,  A61K31/4412 ,  C07D401/12 ,  A61K31/444 ,  A61K31/4433 ,  C07D409/14 ,  A61K31/513 ,  C07D417/12 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/675 ,  A61K45/06 ,  C07D405/12

CPC分类号： C07F9/58 ,  A61K31/435 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/675 ,  A61K45/06 ,  C07D221/16 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D417/12

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

公开(公告)号：US09527875B2

公开(公告)日：2016-12-27

申请号：US14418147

申请日：2013-07-31

申请人： Merck Sharp & Dohme Corp.

发明人： William K. Hagmann ,  Ravi P. Nargund ,  Timothy A. Blizzard ,  Hubert Josien ,  Purakkattle Biju ,  Christopher W. Plummer ,  Qun Dang ,  Bing Li ,  Derun Li ,  Linus S. Lin ,  Mingxiang Cui ,  Bin Hu ,  Jinglai Hao ,  Zhengxia Chen

IPC分类号： C07D417/12 ,  A61K31/4353 ,  C07F9/58 ,  C07D401/14 ,  C07D221/16 ,  C07D401/12 ,  A61K31/435 ,  A61K31/444 ,  A61K45/06 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/675 ,  C07D405/12 ,  C07D409/14

CPC分类号： C07F9/58 ,  A61K31/435 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/675 ,  A61K45/06 ,  C07D221/16 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D417/12

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

公开(公告)号：US09834563B2

公开(公告)日：2017-12-05

申请号：US15039607

申请日：2014-12-17

申请人： Merck Sharp & Dohme Corp.

发明人： William K. Hagmann ,  Bing Li ,  Jason W. Szewczyk ,  Bowei Wang ,  Dann Parker ,  Timothy Blizzard ,  Hubert Josien ,  Purakkattle Biju ,  Harry Chobanian ,  Candido Gude ,  Ravi P. Nargund ,  Barbara Pio ,  Qun Dang ,  Linus S. Lin ,  Bin Hu ,  Mingxiang Cui ,  Zhengxia Chen ,  Meibi Dai ,  Zaihong Zhang ,  Ying Lv ,  Lili Tian

IPC分类号： A61K31/506 ,  C07D493/04 ,  A61K45/06 ,  C07D213/64 ,  A61K31/44 ,  C07D409/12 ,  A61K31/4436 ,  C07D401/04 ,  A61K31/4545 ,  C07D471/04 ,  A61K31/437 ,  C07D405/12 ,  A61K31/4433 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/443 ,  C07D239/34 ,  A61K31/505 ,  C07D451/06 ,  A61K31/46 ,  C07D221/20 ,  A61K31/438 ,  C07D213/74 ,  C07D417/04

CPC分类号： C07D493/04 ,  A61K31/437 ,  A61K31/438 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/505 ,  A61K31/506 ,  A61K45/06 ,  C07D213/64 ,  C07D213/74 ,  C07D221/20 ,  C07D239/34 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/04 ,  C07D451/06 ,  C07D471/04

摘要： The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I 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.

公开(公告)号：US10000454B2

公开(公告)日：2018-06-19

申请号：US15310488

申请日：2015-05-19

申请人： 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 ,  A61K31/435 ,  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.

公开(公告)号：US09932311B2

公开(公告)日：2018-04-03

申请号：US15023124

申请日：2014-09-30

申请人： Merck Sharp & Dohme Corp.

发明人： Tesfaye Biftu ,  Purakkattle Biju ,  Steven L. Colletti ,  Mingxiang Cui ,  William K. Hagmann ,  Bin Hu ,  Hubert Josien ,  Nam Fung Kar ,  Anilkumar Nair ,  Ravi Nargund ,  Donald M. Sperbeck ,  Cheng Zhu

IPC分类号： C07D221/16 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  A61K31/435 ,  A61K31/444 ,  A61K45/06

CPC分类号： C07D221/16 ,  A61K31/435 ,  A61K31/444 ,  A61K45/06 ,  C07D401/12 ,  C07D405/12

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.

公开(公告)号：US20170166578A1

公开(公告)日：2017-06-15

申请号：US15039607

申请日：2014-12-17

申请人： Merck Sharp & Dohme Corp.

发明人： William K. Hagmann ,  Bing Li ,  Jason W. Szewczyk ,  Bowei Wang ,  Dann Parker ,  Timothy Blizzard ,  Hubert Josien ,  Purakkattle Biju ,  Harry Chobanian ,  Candido Gude ,  Ravi P. Nargund ,  Barbara Pio ,  Qun Dang ,  Linus S. Lin ,  Bin Hu ,  Mingxiang Cui ,  Zhengxia Chen ,  Meibi Dai ,  Zaihong Zhang ,  Ying Lv ,  Lili Tian

IPC分类号： C07D493/04 ,  C07D213/64 ,  A61K31/44 ,  C07D409/12 ,  A61K31/4436 ,  C07D401/04 ,  A61K31/4545 ,  C07D471/04 ,  A61K31/437 ,  C07D405/12 ,  A61K31/4433 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/443 ,  C07D239/34 ,  A61K31/505 ,  C07D451/06 ,  A61K31/46 ,  C07D221/20 ,  A61K31/438 ,  A61K31/506 ,  C07D213/74 ,  C07D417/04 ,  A61K45/06

CPC分类号： C07D493/04 ,  A61K31/437 ,  A61K31/438 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/505 ,  A61K31/506 ,  A61K45/06 ,  C07D213/64 ,  C07D213/74 ,  C07D221/20 ,  C07D239/34 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/04 ,  C07D451/06 ,  C07D471/04

摘要： The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I 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.

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.

公开(公告)号：US20160207887A1

公开(公告)日：2016-07-21

申请号：US15023124

申请日：2014-09-30

申请人： MERCK SHARP & DOHME CORP.

发明人： Tesfaye Biftu ,  Purakkattle Biju ,  Steven L. Colletti ,  Mingxiang Cui ,  William K. Hagmann ,  Bin Hu ,  Hubert Josien ,  Nam Fung Kar ,  Anilkumar Nair ,  Ravi Nargund ,  Donald M. Sperbeck ,  Cheng Zhu

IPC分类号： C07D221/16 ,  A61K45/06 ,  C07D405/12 ,  A61K31/444 ,  A61K31/435 ,  C07D401/12

CPC分类号： C07D221/16 ,  A61K31/435 ,  A61K31/444 ,  A61K45/06 ,  C07D401/12 ,  C07D405/12

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 dyslip idemia, 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，例如混合型或糖尿病型血脂异常，高脂血症，高胆固醇血症， 和高甘油三酯血症。

公开(公告)号：US20140045746A1

公开(公告)日：2014-02-13

申请号：US13955282

申请日：2013-07-31

申请人： Merck Sharp & Dohme Corp.

发明人： William K. Hagmann ,  Ravi P. Nargund ,  Timothy A. Blizzard ,  Hubert Josien ,  Purakkattle Biju ,  Christopher W. Plummer ,  Qun Dang ,  Bing Li ,  Linus S. Lin ,  Mingxiang Cui ,  Bin Hu ,  Jinglai Hao ,  Zhengxia Chen

IPC分类号： C07D221/16 ,  A61K31/444 ,  A61K45/06 ,  C07D401/12 ,  A61K31/435

CPC分类号： C07F9/58 ,  A61K31/435 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/675 ,  A61K45/06 ,  C07D221/16 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D417/12

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