公开(公告)号：US20180230178A1

公开(公告)日：2018-08-16

申请号：US15752144

申请日：2016-08-11

申请人： 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.

发明人： 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分类号： C07H21/04 ,  C07H21/02 ,  C07H19/23 ,  C07H19/20 ,  A61P35/00

摘要： 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：US11702430B2

公开(公告)日：2023-07-18

申请号：US17040192

申请日：2019-03-28

申请人： Merck Sharp & Dohme LLC ,  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

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 ,  C07D277/64 ,  A61P37/04 ,  A61P35/00

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

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：US20210206796A1

公开(公告)日：2021-07-08

申请号：US16771814

申请日：2018-12-17

申请人： 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.

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

IPC分类号： C07H21/00 ,  A61P37/04

摘要： 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：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：US11685761B2

公开(公告)日：2023-06-27

申请号：US16771814

申请日：2018-12-17

申请人： 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

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

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

CPC分类号： C07H21/00 ,  A61K31/7084 ,  A61P37/04 ,  C07H21/02 ,  C07H21/04 ,  C07B2200/07

摘要： 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：US20130090309A1

公开(公告)日：2013-04-11

申请号：US13704484

申请日：2012-04-30

申请人： Eric Thomas Romeo ,  Michelle R. Machacek ,  Benjamin Wesley Trotter ,  Thomas Allen Miller ,  Brian Michael Andresen ,  Neville John Anthony ,  Brandon M. Taoka ,  Yuan Liu

发明人： Eric Thomas Romeo ,  Michelle R. Machacek ,  Benjamin Wesley Trotter ,  Thomas Allen Miller ,  Brian Michael Andresen ,  Neville John Anthony ,  Brandon M. Taoka ,  Yuan Liu

IPC分类号： A61K31/444 ,  A61K31/496 ,  A61K45/06 ,  A61K31/675 ,  C07F5/02 ,  A61K31/69 ,  C07D417/14 ,  C07F9/6558

CPC分类号： A61K31/444 ,  A61K31/496 ,  A61K31/675 ,  A61K31/69 ,  A61K45/06 ,  C07D277/04 ,  C07D417/14 ,  C07F5/025 ,  C07F9/65583

摘要： The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

摘要翻译： 本发明提供某些含有氨基 - 吡啶的式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和n如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。

公开(公告)号：US20200062798A1

公开(公告)日：2020-02-27

申请号：US16611624

申请日：2018-05-07

申请人： Wen-Lian WU ,  Jongwon LIM ,  Jared N. CUMMING ,  Benjamin Wesley TROTTER ,  Wonsuk CHANG ,  Merck Sharp & Dohme Corp.

发明人： Wen-Lian WU ,  Jongwon LIM ,  Jared N. Cumming ,  Benjamin Wesley TROTTER ,  Wonsuk CHANG

IPC分类号： C07H21/00

摘要： A class of polycyclic compounds 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, 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：US11466047B2

公开(公告)日：2022-10-11

申请号：US16611624

申请日：2018-05-07

申请人： Merck Sharp & Dohme Corp. ,  Wen-Lian Wu ,  Jongwon Lim ,  Jared N. Cumming ,  Benjamin Wesley Trotter ,  Wonsuk Chang

发明人： Wen-Lian Wu ,  Jongwon Lim ,  Jared N. Cumming ,  Benjamin Wesley Trotter ,  Wonsuk Chang

IPC分类号： C07H21/00 ,  C07H21/04 ,  A61P35/00 ,  A61P37/02 ,  C07H21/02

摘要： A class of polycyclic compounds 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, 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：US11312772B2

公开(公告)日：2022-04-26

申请号：US16635059

申请日：2018-07-30

申请人： Merck Sharp & Dohme Corp. ,  Saso Cemerski ,  Jared N. Cumming ,  Johnny E. Kopinja ,  Samanthi A. Perera ,  Benjamin Wesley Trotter ,  Archie Ngai-Chiu Tse

发明人： Saso Cemerski ,  Jared N. Cumming ,  Johnny E. Kopinja ,  Samanthi A. Perera ,  Benjamin Wesley Trotter ,  Archie Ngai-Chiu Tse

IPC分类号： A61P35/00 ,  A61K31/381 ,  A61K39/00 ,  C07K16/28

摘要： Therapeutic combinations that comprise at least one antagonist of the Programmed Death 1 receptor (PD-1) and at least one benzo[b]thiophene compound that activates the Stimulator of Interferon Genes (STING) pathway are disclosed herein. Also disclosed is the use of such therapeutic combinations for the treatment of cancers.

公开(公告)号：US20210130466A1

公开(公告)日：2021-05-06

申请号：US16635059

申请日：2018-07-30

申请人： Saso CEMERSKI ,  Jared N. CUMMING ,  Johnny E. KOPINJA ,  Samanthi A. PERERA ,  Benjamin Wesley TROTTER ,  Archie Ngai-Chiu TSE ,  Merck Sharp & Dohme Corp.

发明人： Saso CEMERSKI ,  Jared N. CUMMING ,  Johnny E. KOPINJA ,  Samanthi A. PERERA ,  Benjamin Wesley TROTTER ,  Archie Ngai-Chiu TSE

IPC分类号： C07K16/28 ,  A61P35/00 ,  A61K31/381

摘要： Therapeutic combinations that comprise at least one antagonist of the Programmed Death 1 receptor (PD-1) and at least one benzo[b]thiophene compound that activates the Stimulator of Interferon Genes (STING) pathway are disclosed herein. Also disclosed is the use of such therapeutic combinations for the treatment of cancers.