公开(公告)号：US09815796B2

公开(公告)日：2017-11-14

申请号：US15107233

申请日：2014-12-17

Applicant: Merck Sharp & Dohme Corp. ,  MSD R & D (China) Co. Ltd.

Inventor： Dong Ming Shen ,  Melissa Egbertson ,  Richard Berger ,  XiaoXia Qian ,  Yimin Qian ,  Bart Harper ,  Meng Yang ,  Zack Zhiqiang Guo ,  Vanessa L. Rada ,  Deping Wang ,  Timothy A. Cernak ,  Christopher Sinz ,  Ming Wang ,  Jonathan E. Wilson ,  Shimin Xu

IPC: C07D239/36 ,  C07D401/12 ,  C07D401/06 ,  C07D403/04 ,  C07D403/14 ,  C07D487/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D403/12 ,  C07D403/06

CPC classification number: C07D239/36 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D487/04

Abstract: Disclosed are pyrimidine carboxamide compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2), pharmaceutical compositions and uses thereof.

公开(公告)号：US20210403479A1

公开(公告)日：2021-12-30

申请号：US17288626

申请日：2019-11-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Wensheng Yu ,  Joseph Kozlowski ,  Dane James Clausen ,  Jian Liu ,  Younong Yu ,  Ming Wang ,  Bing Li

IPC: C07D487/10 ,  C07D403/12 ,  C07D413/14 ,  C07D401/14 ,  C07D401/12 ,  C07D471/04 ,  C07D417/14 ,  C07D498/10 ,  C07D405/14 ,  A61K45/06

Abstract: The present invention relates to Compounds of Formula I: and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4 and A are as defined herein. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treating or preventing HIV infection in a subject.

公开(公告)号：US09751881B2

公开(公告)日：2017-09-05

申请号：US14908222

申请日：2014-07-28

Applicant: Merck Sharp & Dohme Corp.

Inventor： Haifeng Tang ,  Barbara Pio ,  Jinlong Jiang ,  Alexander Pasternak ,  Shuzhi Dong ,  Ronald Dale Ferguson, II ,  Zack Zhiqiang Guo ,  Harry Chobanian ,  Jessica Frie ,  Yan Guo ,  Zhicai Wu ,  Yang Yu ,  Ming Wang

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

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：US20170015633A1

公开(公告)日：2017-01-19

申请号：US15107233

申请日：2014-12-17

Applicant: Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co. Ltd.

Inventor： Dong Ming Shen ,  Melissa Egbertson ,  Richard Berger ,  XiaoXia Qian ,  Yimin Qian ,  Bart Harper ,  Meng Yang ,  Zack Zhi Qiang Guo ,  Vanessa L. Rada ,  Deping Wang ,  Timothy A. Cernak ,  Christopher Sinz ,  Ming Wang ,  Jonathan E. Wilson ,  Shimin Xu

IPC: C07D239/36 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D487/04 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D401/06 ,  C07D403/12

CPC classification number: C07D239/36 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D487/04

Abstract: Disclosed are pyrimidine carboxamide compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2), pharmaceutical compositions and uses thereof.

Abstract translation: 公开了式（I）的嘧啶羧酰胺化合物，其可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病，药物组合物及其用途的治疗剂。

公开(公告)号：US20160060256A1

公开(公告)日：2016-03-03

申请号：US14786466

申请日：2014-04-22

Applicant: Kenneth L. ARRINGTON ,  Byron DUBOIS ,  John S. DEBENHAM ,  Ping LIU ,  Alan B. NORTHRUP ,  Jason W. SZEWCZYK ,  Liping WANG ,  Ming WANG ,  MERCK SHARP & DOHME CORP.

Inventor： Kenneth L. Arrington ,  Byron DuBois ,  John S. Debenham ,  Ping Liu ,  Alan B. Northrup ,  Jason W. Szewczyk ,  Liping Wang ,  Ming Wang

IPC: C07D417/14 ,  C07D417/12 ,  A61K31/5377 ,  A61K31/506

CPC classification number: C07D417/14 ,  A61K31/427 ,  A61K31/506 ,  A61K31/5377 ,  C07D417/12

Abstract: The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

Abstract translation: 本发明提供了式（I）（I）的某些噻唑取代的氨基嘧啶化合物或其药学上可接受的盐，其中R1，R2，R3，R5，R6和下标r，s和t如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。