公开(公告)号：EP3102198B1

公开(公告)日：2020-08-26

申请号：EP15745823.3

申请日：2015-02-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： CHOBANIAN, Harry ,  DEMONG, Duane ,  GUO, Yan ,  HU, Zhiyong ,  MILLER, Michael ,  PIO, Barbara ,  PLUMMER, Christopher, W. ,  XIAO, Dong ,  YANG, Cangming ,  ZHANG, Rui

IPC: A61K31/33 ,  A61K31/34 ,  C07C15/14

公开(公告)号：EP3076959B1

公开(公告)日：2018-07-04

申请号：EP14868525.8

申请日：2014-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： BARA, Thomas ,  CHOBANIAN, Harry ,  GUO, Yan ,  JOSIEN, Hubert ,  MILLER, Michael ,  PIO, Barbara ,  PLUMMER, Christopher W. ,  YANG, Cangming ,  XIAO, Dong

IPC: C07C59/72 ,  C07C255/59 ,  C07D221/04 ,  C07D231/12 ,  C07D333/24 ,  C07D417/04 ,  C07D249/04 ,  C07D471/04 ,  C07D207/333 ,  C07D277/42 ,  C07D209/08 ,  C07D209/12 ,  C07D213/64 ,  A61K31/075 ,  A61K45/06 ,  A61P3/10

CPC classification number: 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

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.

公开(公告)号：EP3974413A1

公开(公告)日：2022-03-30

申请号：EP21202075.4

申请日：2014-12-17

Applicant: MERCK SHARP & DOHME CORP.

Inventor： HAGMANN, William K. ,  LI, Bing ,  SZEWCZYK, Jason, W. ,  WANG, Bowei ,  PARKER, Dann ,  BLIZZARD, Timothy ,  JOSIEN, Hubert ,  BIJU, Purakkattle ,  CHOBANIAN, Harry ,  GUDE, Candido ,  NARGUND, Ravi, P. ,  PIO, Barbara ,  DANG, Qun ,  LIN, Linus, S. ,  HU, Bin ,  CUI, Mingxiang ,  CHEN, Zhengxia ,  DAI, Meibi ,  ZHANG, Zaihong ,  LV, Ying ,  TIAN, Lili

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

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：EP3076959A1

公开(公告)日：2016-10-12

申请号：EP14868525.8

申请日：2014-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： BARA, Thomas ,  CHOBANIAN, Harry ,  GUO, Yan ,  JOSIEN, Hubert ,  MILLER, Michael ,  PIO, Barbara ,  PLUMMER, Christopher W. ,  YANG, Cangming ,  XIAO, Dong

IPC: A61K31/075

CPC classification number: 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

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.

公开(公告)号：EP2822557A1

公开(公告)日：2015-01-14

申请号：EP13757283.0

申请日：2013-02-27

Applicant: Merck Sharp & Dohme Corp.

Inventor： MANDAL, Mihir ,  BLIZZARD, Timothy, A. ,  CHEN, Helen ,  CHOBANIAN, Harry ,  GUO, Yan ,  PIO, Barbara ,  WU, Zhicai ,  BIFTU, Tesfaye ,  GREENLEE, William, J. ,  ZHU, Johnny Zhaoning

IPC: A61K31/44

CPC classification number: C07D405/06 ,  A61K31/365 ,  A61K31/4365 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/616 ,  A61K45/06 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61K2300/00

Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is -O-, -N(R), -C(R
8 )(R
9 ) or -C(O)-; and Y is -O-, -N(R), -C(R
8 )(R
9 ) or -C(O)- and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.

公开(公告)号：EP3027625B1

公开(公告)日：2018-05-30

申请号：EP14831878.5

申请日：2014-07-28

Applicant: Merck Sharp & Dohme Corp.

Inventor： TANG, Haifeng ,  PIO, Barbara ,  JIANG, Jinlong ,  PASTERNAK, Alexander ,  DONG, Shuzhi ,  FERGUSON, Ronald Dale, II ,  GUO, Zack Zhiqiang ,  CHOBANIAN, Harry ,  FRIE, Jessica ,  GUO, Yan ,  WU, Zhicai ,  YU, Yang ,  WANG, Ming

IPC: C07D498/12

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/444 ,  A61K31/46 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5386 ,  A61K45/06 ,  C07D451/00 ,  C07D493/04 ,  C07D498/10

Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

公开(公告)号：EP2822557B1

公开(公告)日：2017-08-23

申请号：EP13757283.0

申请日：2013-02-27

Applicant: Merck Sharp & Dohme Corp.

Inventor： MANDAL, Mihir ,  BLIZZARD, Timothy, A. ,  CHEN, Helen ,  CHOBANIAN, Harry ,  GUO, Yan ,  PIO, Barbara ,  WU, Zhicai ,  BIFTU, Tesfaye ,  GREENLEE, William, J. ,  ZHU, Johnny Zhaoning

IPC: C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4427 ,  A61P9/00

CPC classification number: C07D405/06 ,  A61K31/365 ,  A61K31/4365 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/616 ,  A61K45/06 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61K2300/00

公开(公告)号：EP3102198A1

公开(公告)日：2016-12-14

申请号：EP15745823.3

申请日：2015-02-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： CHOBANIAN, Harry ,  DEMONG, Duane ,  GUO, Yan ,  HU, Zhiyong ,  MILLER, Michael ,  PIO, Barbara ,  PLUMMER, Christopher, W. ,  XIAO, Dong ,  YANG, Cangming ,  ZHANG, Rui

IPC: A61K31/33 ,  A61K31/34 ,  C07C15/14

CPC classification number: 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

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：EP2528603A1

公开(公告)日：2012-12-05

申请号：EP11737514.7

申请日：2011-01-25

Applicant: Merck Sharp & Dohme Corp.

Inventor： CHOBANIAN, Harry ,  LIN, Linus, S. ,  LIU, Ping ,  CHOIDA, Marc, D. ,  DEVITA, Robert, J. ,  NARGRUND, Ravi, P. ,  GUO, Yan ,  HAMILL, Terence ,  LI, Wenping ,  HENZE, Darrell, A.

IPC: A61K31/42

CPC classification number: A61K31/422 ,  A61K31/4178

Abstract: The present invention is directed to a composition useful for the treatment of a FAAH mediated disease, disorder or conditions comprising a FAAH inhibitor and a second activation, comprising a selected imidazole or oxazole FAAH inhibitor and a second active agent. The compositions will be useful in the treatment of a wide range of disease, disorder, or conditions 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. In another aspect the invention discloses herein is directed to compositions useful in the treatment of neuropathic and nociceptive pain, said compositions comprising etoricoxib.

公开(公告)号：EP3177282A1

公开(公告)日：2017-06-14

申请号：EP15829663.2

申请日：2015-08-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： CHOBANIAN, Harry ,  DEMONG, Duane ,  GUO, Yan ,  PIO, Barbara ,  PLUMMER, Christopher, W.

IPC: A61K31/192 ,  A61K31/353 ,  C07D311/20

CPC classification number: C07D335/06 ,  A61K31/192 ,  A61K31/352 ,  A61K31/353 ,  A61K31/366 ,  A61K31/382 ,  A61K31/44 ,  A61K31/444 ,  A61K31/453 ,  A61K45/06 ,  C07D213/64 ,  C07D311/04 ,  C07D311/20 ,  C07D405/04 ,  C07D405/10 ,  A61K2300/00

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.