公开(公告)号：US09527875B2

公开(公告)日：2016-12-27

申请号：US14418147

申请日：2013-07-31

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: 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 classification number: 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

Abstract: 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.

Abstract translation: 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：US20150191495A1

公开(公告)日：2015-07-09

申请号：US14418147

申请日：2013-07-31

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: 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 classification number: 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

Abstract: 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.

Abstract translation: 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

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: 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 classification number: 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

Abstract: 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：US20170166578A1

公开(公告)日：2017-06-15

申请号：US15039607

申请日：2014-12-17

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: 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 classification number: 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

Abstract: 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：US09045467B2

公开(公告)日：2015-06-02

申请号：US14099142

申请日：2013-12-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Harry Chobanian ,  Linus S. Lin ,  Ping Liu ,  Marc D. Chioda ,  Robert J. DeVita ,  Ravi P. Nargund ,  Yan Guo

IPC: A01N43/40 ,  A61K31/44 ,  C07D413/14 ,  C07D263/46 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14 ,  C07D271/06 ,  C07D271/10

CPC classification number: C07D413/14 ,  C07D263/46 ,  C07D271/06 ,  C07D271/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.

Abstract translation: 本发明涉及可用作脂肪酸酰胺水解酶（FAAH）抑制剂的某些恶唑衍生物。 本发明还涉及包含这些化合物作为活性成分的药物制剂，以及这些化合物及其制剂在治疗某些疾病，包括骨关节炎，类风湿性关节炎，糖尿病性神经病变，带状疱疹后神经痛，ke肉肌痛和纤维肌痛等方面的用途。 作为急性疼痛，偏头痛，睡眠障碍，阿尔茨海默病和帕金森病。

公开(公告)号：US20140171437A1

公开(公告)日：2014-06-19

申请号：US14099142

申请日：2013-12-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Harry Chobanian ,  Linus S. Lin ,  Ping Liu ,  Marc D. Chioda ,  Robert J. DeVita ,  Ravi P. Nargund ,  Yan Guo

IPC: C07D413/14 ,  C07D271/10 ,  C07D271/06 ,  C07D413/04 ,  C07D263/46

CPC classification number: C07D413/14 ,  C07D263/46 ,  C07D271/06 ,  C07D271/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.

Abstract translation: 本发明涉及可用作脂肪酸酰胺水解酶（FAAH）抑制剂的某些恶唑衍生物。 本发明还涉及包含这些化合物作为活性成分的药物制剂，以及这些化合物及其制剂在治疗某些疾病，包括骨关节炎，类风湿性关节炎，糖尿病性神经病变，带状疱疹后神经痛，ke肉肌痛和纤维肌痛等方面的用途。 作为急性疼痛，偏头痛，睡眠障碍，阿尔茨海默病和帕金森病。

公开(公告)号：US20140045746A1

公开(公告)日：2014-02-13

申请号：US13955282

申请日：2013-07-31

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07D221/16 ,  A61K31/444 ,  A61K45/06 ,  C07D401/12 ,  A61K31/435

CPC classification number: 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

Abstract: 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.

Abstract translation: 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