公开(公告)号：US20190337918A1

公开(公告)日：2019-11-07

申请号：US16513417

申请日：2019-07-16

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Michael D. Altman ,  Brandon D. Cash ,  Wonsuk Chang ,  Jared N. Cumming ,  Andrew M. Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Matthew A. Larsen ,  Rui Liang ,  Jongwon Lim ,  Min Lu ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Sriram Tyagarajan

IPC: C07D333/60 ,  C07D498/04 ,  C07D333/62 ,  C07D409/12

Abstract: Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 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 of the disclosure.

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：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。