公开(公告)号：US20210040127A1

公开(公告)日：2021-02-11

申请号：US16977253

申请日：2019-03-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Matthew L. Childers ,  Jared N. Cumming ,  Christian A. Fischer ,  Symon Gathiaka ,  Hakan Gunaydin ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Anandan Palani ,  Rachel L. Palte ,  Qinglin Pu ,  David L. Sloman ,  Sung-Sau So ,  Chunrui Sun ,  Hongjun Zhang

IPC: C07F5/02 ,  C07K16/28

Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

公开(公告)号：US20200290996A1

公开(公告)日：2020-09-17

申请号：US16753050

申请日：2018-10-04

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Catherine M. White ,  Abdelghani Achab ,  Indu T. Bharathan ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Meredeth Ann McGowan ,  Nunzio Sciammetta ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou

IPC: C07D401/14 ,  C07D401/12 ,  C07D213/74 ,  C07D405/12 ,  C07D413/14 ,  C07D417/14

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20200216425A1

公开(公告)日：2020-07-09

申请号：US16819325

申请日：2020-03-16

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yongxin Han ,  Abdelghani Achab ,  Yongqi Deng ,  Xavier Fradera ,  Craig Gibeau ,  Brett A. Hopkins ,  Derun Li ,  Kun Liu ,  Meredeth A. McGowan ,  Nunzio Sciammetta ,  David Sloman ,  Catherine White ,  Hongjun Zhang ,  Hua Zhou

IPC: C07D405/10 ,  A61K31/4427 ,  A61K31/4965 ,  C07D241/12 ,  A61K31/501 ,  C07D417/14 ,  A61K31/4418 ,  C07D213/56 ,  C07D401/04 ,  C07D413/04 ,  A61K31/513 ,  A61K31/444 ,  C07D405/14 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/41 ,  A61K31/427 ,  C07D417/10 ,  A61K31/337 ,  C07D305/08 ,  A61K31/4155 ,  A61K31/506 ,  A61K31/437 ,  C07D471/04 ,  A61K45/06 ,  A61K31/4523 ,  C07D413/14 ,  C07D209/46 ,  A61P31/00 ,  C07D405/04 ,  C07D401/12 ,  C07D413/10 ,  A61P35/00 ,  C07D231/12 ,  A61P37/00 ,  C07D263/32

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20190144433A1

公开(公告)日：2019-05-16

申请号：US16186769

申请日：2018-11-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yongxin Han ,  Abdelghani Achab ,  Yongqi Deng ,  Xavier Fradera ,  Craig Gibeau ,  Brett A. Hopkins ,  Derun Li ,  Kun Liu ,  Meredeth A. McGowan ,  Nunzio Sciammetta ,  David Sloman ,  Catherine White ,  Hongjun Zhang ,  Hua Zhou

IPC: C07D405/10 ,  A61K31/4427 ,  A61K45/06 ,  C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/4155 ,  C07D305/08 ,  A61K31/337 ,  C07D417/10 ,  A61K31/427 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/4184 ,  C07D405/14 ,  A61K31/444 ,  A61K31/513 ,  C07D413/04 ,  C07D401/04 ,  C07D213/56 ,  A61K31/4418 ,  C07D417/14 ,  A61K31/501 ,  C07D241/12 ,  A61K31/4965 ,  A61K31/4523

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

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