公开(公告)号：US20210009608A1

公开(公告)日：2021-01-14

申请号：US17040192

申请日：2019-03-28

申请人： Michael D. ALTMAN ,  Brandon D. CASH ,  Jared N. CUMMING ,  Duane E. DEMONG ,  Andrew M. HAIDLE ,  James P. JEWELL ,  Matthew A. LARSEN ,  Min LU ,  Ryan D. OTTE ,  Brandon M. TAOKA ,  Benjamin Wesley TROTTER ,  Quang T, TRUONG ,  Merck Sharp & Dohme Corp.

发明人： Michael D. Altman ,  Brandon D. Cash ,  Jared N. Cumming ,  Duane E. DeMong ,  Andrew M. Haidle ,  James P. Jewell ,  Matthew A. Larsen ,  Min Lu ,  Ryan D. Otte ,  Brandon M. Taoka ,  Benjamin Wesley Trotter ,  Quang T. Truong

IPC分类号： C07D513/04 ,  C07D495/04 ,  A61P37/04

摘要： Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R5, R6, R8, R9, A, 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 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：US20190337918A1

公开(公告)日：2019-11-07

申请号：US16513417

申请日：2019-07-16

申请人： MERCK SHARP & DOHME CORP.

发明人： 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分类号： C07D333/60 ,  C07D498/04 ,  C07D333/62 ,  C07D409/12

摘要： 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

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D409/12 ,  A61P35/00 ,  C07D495/04 ,  C07D498/04 ,  C07D417/10

摘要： 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.