公开(公告)号：US20190300513A1

公开(公告)日：2019-10-03

申请号：US16372103

申请日：2019-04-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Brandon D. Cash ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Duane E. DeMong ,  Andrew Marc Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Matthew A. Larsen ,  Jongwon Lim ,  Min Lu ,  Ryan D. Otte ,  Benjamin Wesley Trotter

IPC: C07D409/12 ,  A61P35/00 ,  C07D495/04 ,  C07D498/04 ,  C07D417/10

Abstract: Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.

公开(公告)号：US20180037554A1

公开(公告)日：2018-02-08

申请号：US15549242

申请日：2016-02-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Amjad Ali ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Pauline C. Ting ,  Purakkattle Biju ,  Manuel de Lera Ruiz ,  Sylvia J. Degrado ,  Alexander L. Tung ,  Timothy J. Henderson ,  Liwu Hong ,  Jae-Hun Kim ,  Dong Won-Shik Kim ,  Joe Lee ,  Jie Wu ,  Heping Wu ,  Yushi Xiao ,  Tao Yu ,  Gang Zhou ,  Xiaohong Zhu ,  Kevin D. McCormick ,  Jayaram R. Tagat ,  Dong Xiao ,  Tanweer Khan ,  Jianhua Cao ,  Michael Berlin ,  Yonglian Zhang

IPC: C07D239/84 ,  C07D401/14 ,  C07D413/12 ,  C07D417/12 ,  C07D405/12 ,  C07D417/14 ,  C07D413/14 ,  C07D471/04 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D239/84 ,  A61K31/517 ,  A61P25/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.

公开(公告)号：US20170197991A1

公开(公告)日：2017-07-13

申请号：US15423238

申请日：2017-02-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Xianhai Huang ,  Timothy J. Henderson ,  Jae-Hun Kim ,  Christopher Boyce ,  Pauline Ting ,  Junying Zheng ,  Edward Metzger ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Qiaolin Deng

IPC: C07D519/00 ,  C07D487/04

CPC classification number: C07D519/00 ,  C07D487/04

Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

公开(公告)号：US20170044206A1

公开(公告)日：2017-02-16

申请号：US15234182

申请日：2016-08-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Brian Michael Andresen ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Andrew Marc Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Rui Liang ,  Jongwon Lim ,  Hong Liu ,  Min Lu ,  Alan B. Northrup ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Quang T. Truong ,  Shawn P. Walsh ,  Kake Zhao

IPC: C07H21/04 ,  C07H19/23 ,  C07H19/20 ,  C07H21/02 ,  A61K39/39

CPC classification number: C07H21/04 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/7084 ,  A61K39/39 ,  A61P35/00 ,  C07H19/20 ,  C07H19/23 ,  C07H21/00 ,  C07H21/02

Abstract: A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

Abstract translation: 一类通式（I），通式（I'）或通式（I“）的多环化合物，其中基团1，碱基2，Y，亚氨基，Xa，Xa1，Xb，Xb1，Xc，Xc1， Xd，Xd1，R1，R1a，R2，R2a，R3，R4，R4a，R5，R6，R6a，R7，R7a，R8和R8a在本文中定义，其可用作I型干扰素生产的电感器， 提供了STING活性剂，还提供了合成和使用化合物的方法。