公开(公告)号：US20160332968A1

公开(公告)日：2016-11-17

申请号：US15110894

申请日：2015-02-03

Applicant: Harry CHOBANIAN ,  Duane DEMONG ,  Yan Guo ,  Zhiyong Hu ,  Barbara PIO ,  Christopher PLUMMER ,  Dong XIAO ,  Cangming YANG ,  Rui ZHANG ,  Merck Sharp & Dohme Corp. ,  Michael MILLER

Inventor： Harry Chobanian ,  Duane DeMong ,  Yan Guo ,  Zhiyong Hu ,  Michael Miller ,  Barbara Pio ,  Christopher W. Plummer ,  Dong Xiao ,  Michael Yang

IPC: 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 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：US20160024091A1

公开(公告)日：2016-01-28

申请号：US14774390

申请日：2014-03-10

Applicant: Alexander PASTERNAK ,  Fa-Xiang DING ,  Shuzhi DONG ,  Haifeng TANG ,  Jinlong JIANG ,  Cangming YANG ,  Dipshikha BISWAS ,  MERCK SHARP & DOHME CORP.

Inventor： Alexander Pasternak ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Dipshikha Biswas ,  Haifeng Tang ,  Jinlong Jiang ,  Cangming Yang ,  Xin Gu

IPC: C07D471/10 ,  A61K31/444 ,  A61K31/506 ,  A61K31/435 ,  A61K31/5386 ,  A61K31/501 ,  C07D471/20 ,  A61K31/4995 ,  C07D498/20 ,  A61K45/06 ,  A61K31/497

CPC classification number: C07D471/10 ,  A61K31/24 ,  A61K31/401 ,  A61K31/403 ,  A61K31/405 ,  A61K31/407 ,  A61K31/41 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/4422 ,  A61K31/444 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/551 ,  A61K31/554 ,  A61K31/585 ,  A61K31/675 ,  A61K45/06 ,  C07D471/20 ,  C07D498/20 ,  A61K2300/00

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.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。 这些化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭和慢性肾脏疾病以及与过量的盐和水保留有关的病症的医学病症。

公开(公告)号：US20130059830A1

公开(公告)日：2013-03-07

申请号：US13696831

申请日：2011-05-16

Applicant: Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Cangming Yang

Inventor： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Cangming Yang

IPC: A61K31/506 ,  C07D413/14 ,  A61P3/00 ,  A61K31/55 ,  A61P3/04 ,  A61P3/10 ,  C07D401/14 ,  A61K31/5377

CPC classification number: C07D401/14 ,  C07D413/14

Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.