公开(公告)号：US11685761B2

公开(公告)日：2023-06-27

申请号：US16771814

申请日：2018-12-17

Applicant: Merck Sharp & Dohme Corp. ,  Brian M. Andresen ,  Frank Bennett ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Jongwon Lim ,  Min Lu ,  Benjamin Wesley Trotter ,  Wen-Lian Wu

Inventor： Brian M. Andresen ,  Frank Bennett ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Jongwon Lim ,  Min Lu ,  Benjamin Wesley Trotter ,  Wen-Lian Wu

IPC: C07H21/00 ,  A61P37/04 ,  C07H21/02 ,  A61K31/7084 ,  C07H21/04

CPC classification number: C07H21/00 ,  A61K31/7084 ,  A61P37/04 ,  C07H21/02 ,  C07H21/04 ,  C07B2200/07

Abstract: A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, 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.

公开(公告)号：US20210330676A1

公开(公告)日：2021-10-28

申请号：US17268995

申请日：2019-08-16

Applicant: Merck Sharp & Dohme Corp.

Inventor： Dane Clausen ,  Xavier Fradera ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Xianhai Huang ,  Joseph Kozlowski ,  Guoqing Li ,  Jongwon Lim ,  Theodore A. Martinot ,  Alexander Pasternak ,  Nunzio Sciammetta ,  Andreas Verras ,  Li Xiao ,  Wensheng Yu ,  Rui Zhang

IPC: A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D401/06 ,  C07D413/14 ,  C07D451/06 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/454 ,  A61K31/46

Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20190382363A1

公开(公告)日：2019-12-19

申请号：US15768880

申请日：2016-11-28

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yongxin Han ,  Jongwon Lim ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

IPC: C07D311/22 ,  C07D409/06 ,  C07D405/06 ,  C07D417/06 ,  C07D413/06 ,  C07D405/14

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.

公开(公告)号：US10329295B2

公开(公告)日：2019-06-25

申请号：US15557203

申请日：2016-03-07

Applicant: MERCK SHARP & DOHME CORP. ,  Jongwon Lim ,  Michael D. Altman ,  Jason D. Brubaker ,  Craig R. Gibeau

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

IPC: C07D487/04 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D403/14 ,  A61P29/00

Abstract: The present invention relates to pyrrolotriazine 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：US20180244712A1

公开(公告)日：2018-08-30

申请号：US15886568

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 ,  C07H21/02 ,  C07H21/00 ,  C07H19/23 ,  C07H19/20 ,  A61K39/39 ,  A61K31/7084 ,  A61K31/708 ,  A61K31/7076 ,  A61K31/7064 ,  A61K31/706

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：US09969749B2

公开(公告)日：2018-05-15

申请号：US15515383

申请日：2015-09-25

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Michael D. Altman ,  Brian M. Andresen ,  Jason D. Brubaker ,  Matthew L. Childers ,  Anthony Donofrio ,  Thierry Fischmann ,  Craig R. Gibeau ,  Solomon D. Kattar ,  Charles A. Lesburg ,  Jongwon Lim ,  John K. F. MacLean ,  Umar F. Mansoor ,  Alan B. Northrup ,  John M. Sanders ,  Luis Torres

IPC: C07D498/04 ,  A61K45/06 ,  A61K31/517 ,  C07D403/04 ,  C07D239/94 ,  C07D401/04 ,  A61K31/5377 ,  C07D405/14 ,  C07D401/14 ,  C07D413/04 ,  C07D405/04 ,  C07D471/04 ,  A61K31/5383 ,  C07D491/048 ,  C07D417/04 ,  C07D409/04

CPC classification number: C07D498/04 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  A61P37/00 ,  C07D239/94 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/048 ,  A61K2300/00

Abstract: The present invention relates to 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：US20180093964A1

公开(公告)日：2018-04-05

申请号：US15722093

申请日：2017-10-02

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

CPC classification number: 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：US11111232B2

公开(公告)日：2021-09-07

申请号：US16753050

申请日：2018-10-04

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Catherine M. White ,  Abdelghani Achab ,  Indu T. Bharathan ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Meredeth Ann McGowan ,  Nunzio Sciammetta ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou

IPC: A61K31/4418 ,  C07D401/14 ,  C07D213/74 ,  C07D401/12 ,  C07D405/12 ,  C07D413/14 ,  C07D417/14

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

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.