公开(公告)号：US11311528B2

公开(公告)日：2022-04-26

申请号：US16980594

申请日：2019-03-15

Applicant: Merck Sharp & Dohme Corp. ,  Michael D. Altman ,  Matthew L. Childers ,  James P. Jewell ,  Charles A. Lesburg ,  Tony Siu

Inventor： Michael D. Altman ,  Matthew L. Childers ,  James P. Jewell ,  Charles A. Lesburg ,  Tony Siu

IPC: C07D405/10 ,  C07D405/14 ,  C07D409/04 ,  C07D411/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/538

Abstract: The instant invention provides compounds of formula I which are STING inhibitors, and as such are useful for the treatment of STING-mediated diseases such as inflammation, asthma, COPD and cancer.

公开(公告)号：US20220024964A1

公开(公告)日：2022-01-27

申请号：US17299350

申请日：2019-12-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Wonsuk Chang ,  Jared N. Cumming ,  Hong Liu ,  Benjamin Wesley Trotter

IPC: C07H19/14 ,  C07H19/16 ,  C07H19/23

Abstract: A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2a, R3, R3a, R4, R5, R5a, R6, R6a, R7, R7a, R8, R8a, and R9 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 (I).

公开(公告)号：US10947234B2

公开(公告)日：2021-03-16

申请号：US16762201

申请日：2018-11-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michelle R. Machacek ,  David J. Witter ,  Michael Hale Reutershan ,  Michael D. Altman ,  Paul Anthony Stupple

IPC: C07D471/04

Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

公开(公告)号：US10730849B2

公开(公告)日：2020-08-04

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 ,  C07D333/62 ,  C07D409/12 ,  C07D498/04

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：US10703738B2

公开(公告)日：2020-07-07

申请号：US16513409

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 ,  C07D333/62 ,  C07D409/12 ,  C07D498/04

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：US20190337917A1

公开(公告)日：2019-11-07

申请号：US16513409

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：US10106574B2

公开(公告)日：2018-10-23

申请号：US15234182

申请日：2016-08-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Wonsuk Chang ,  Jared N. Cumming ,  Rui Liang ,  Jongwon Lim ,  Tony Siu ,  Benjamin Wesley Trotter ,  Quang T. Truong ,  Shawn P. Walsh

IPC: A61K31/70 ,  A01N43/04 ,  C07H21/04 ,  C07H21/02 ,  A61K39/39 ,  C07H19/20 ,  C07H19/23 ,  C07H21/00 ,  A61K31/7064 ,  A61K31/7084 ,  A61K31/708 ,  A61K31/706 ,  A61K31/7076

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.

公开(公告)号：US20180237469A1

公开(公告)日：2018-08-23

申请号：US15886578

申请日：2018-02-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Brian 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 ,  C07H21/00 ,  C07H19/20 ,  A61K39/39 ,  C07H21/02 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/706 ,  A61K31/7084 ,  A61K31/7064

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.

公开(公告)号：US10040802B2

公开(公告)日：2018-08-07

申请号：US15557206

申请日：2016-03-07

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Jongwon Lim ,  Michael D. Altman ,  Craig R. Gibeau

IPC: C07D495/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/551 ,  A61K31/55 ,  A61K31/4985

Abstract: The present invention relates to thienopyrazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

公开(公告)号：US20140357618A1

公开(公告)日：2014-12-04

申请号：US14465577

申请日：2014-08-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： Matthew P. Christopher ,  Francesc Xavier Fradera Llinas ,  Michelle Machacek ,  Michelle Martinez ,  Michael Hale Reutershan ,  Manami Shizuka ,  Binyuan Sun ,  Christopher Francis Thompson ,  B. Wesley Trotter ,  Matthew E. Voss ,  Michael D. Altman ,  Stephane L. Bogen ,  Ronald J. Doll

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D498/04 ,  C07D519/00

Abstract: The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

Abstract translation: 本发明提供如本文所述的取代的咪唑并吡啶或其药学上可接受的盐或溶剂化物。 代表性化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。