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：US20210403469A1

公开(公告)日：2021-12-30

申请号：US17289062

申请日：2019-11-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yongxin Han ,  David Jonathan Bennett ,  Indu Bharathan ,  Liangqin Guo ,  Brett A. Hopkins ,  Xianhai Huang ,  Derun Li ,  Min Lu ,  Alexander Pasternak ,  David L. Sloman ,  Hongjun Zhang ,  Hua Zhou

IPC: C07D471/04 ,  C07D401/04 ,  C07D215/14 ,  C07D209/94 ,  C07D403/04

Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Formula (I). 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：US10793557B2

公开(公告)日：2020-10-06

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 ,  C07D417/10 ,  C07D498/04 ,  C07D495/04 ,  C07D277/64 ,  C07D417/12 ,  C07D333/56 ,  A61P35/00

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：US20180230178A1

公开(公告)日：2018-08-16

申请号：US15752144

申请日：2016-08-11

Applicant: Michael D. ALTMAN ,  Brian ANDRESEN ,  Wonsuk CHANG ,  Matthew Lloyd CHILDERS ,  Jared N. CUMMING ,  Andrew Marc HAIDLE ,  Timothy J. HENDERSON ,  James P. JEWELL ,  Min LU ,  Alan B. NORTHRUP ,  Ryan D. OTTE ,  Tony SIU ,  Benjamin Wesley TROTTER ,  Quang T TRUONG ,  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 ,  Min Lu ,  Alan B. Northrup ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Quang T. Truong

IPC: C07H21/04 ,  C07H21/02 ,  C07H19/23 ,  C07H19/20 ,  A61P35/00

Abstract: A class of polycyclic compounds of general formula (II), of general formula (II′), or of general formula (II″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, 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：US20220056051A1

公开(公告)日：2022-02-24

申请号：US17312480

申请日：2019-12-13

Applicant: Abdelghani Abe ACHAB ,  Matthew L. CHILDERS ,  Jared N. CUMMING ,  Symon GATHIAKA ,  Charles A. LESBURG ,  Derun LI ,  Min LU ,  Matthew J. MITCHELTREE ,  Anandan PALANI ,  Rachel L. PALTE ,  Hongjun ZHANG ,  Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Matthew L. Childers ,  Jared N. Cumming ,  Symon Gathiaka ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Matthew J. Mitcheltree ,  Anandan Palani ,  Rachel L. Palte ,  Hongjun Zhang

IPC: C07F5/02

Abstract: Described herein are compounds of Formula (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

公开(公告)号：US20210206796A1

公开(公告)日：2021-07-08

申请号：US16771814

申请日：2018-12-17

Applicant: Brian M. ANDRESEN ,  Frank BENNETT ,  Wonsuk CHANG ,  Matthew Lloyd CHILDERS ,  Jared N. CUMMING ,  Jongwon LIM ,  Min LU ,  Benjamin Wesley TROTTER ,  Wen-Lian WU ,  Merck Sharp & Dohme Corp.

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

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：US20210163505A1

公开(公告)日：2021-06-03

申请号：US16973623

申请日：2019-06-14

Applicant: Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Jared N. Cumming ,  Christian Fischer ,  Symon Gathiaka ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Matthew J. Mitcheltree ,  Anandan Palani ,  Rachel L. Palte ,  David L. Sloman ,  Hongjun Zhang

IPC: C07F5/02 ,  C07K16/28

Abstract: Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

公开(公告)号：US20210040127A1

公开(公告)日：2021-02-11

申请号：US16977253

申请日：2019-03-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Matthew L. Childers ,  Jared N. Cumming ,  Christian A. Fischer ,  Symon Gathiaka ,  Hakan Gunaydin ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Anandan Palani ,  Rachel L. Palte ,  Qinglin Pu ,  David L. Sloman ,  Sung-Sau So ,  Chunrui Sun ,  Hongjun Zhang

IPC: C07F5/02 ,  C07K16/28

Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

公开(公告)号：US20210009608A1

公开(公告)日：2021-01-14

申请号：US17040192

申请日：2019-03-28

Applicant: 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.

Inventor： 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: C07D513/04 ,  C07D495/04 ,  A61P37/04

Abstract: 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：US10766919B2

公开(公告)日：2020-09-08

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: A01N43/04 ,  A61K31/70 ,  C07H21/04 ,  C07H21/02 ,  A61K39/39 ,  C07H19/20 ,  C07H19/23 ,  C07H21/00 ,  A61P35/00 ,  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.