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：US20220259188A1

公开(公告)日：2022-08-18

申请号：US17614732

申请日：2020-06-01

申请人： Hua ZHOU ,  John J. ACTON, III ,  Michael J. ARDOLINO ,  Yi-Heng CHEN ,  Peter H. FULLER ,  Anmol GULATI ,  Rebecca Elizabeth JOHNSON ,  William P. KAPLAN ,  Solomon D. KATTAR ,  Mitchell H. KEYLOR ,  Derun LI ,  Kaitlyn Marie LOGAN ,  Min LU ,  Gregori J. MORRIELLO ,  Santhosh F. NEELAMKAVIL ,  Barbara PIO ,  Nunzio SCIAMMETTA ,  Vladimir SIMOV ,  Jing SU ,  Luis TORRES ,  Xin YAN ,  Merck Sharp & Dohme Corp.

发明人： Hua Zhou ,  John J. Acton, III ,  Michael J. Ardolino ,  Yi-Heng Chen ,  Peter H. Fuller ,  Anmol Gulati ,  Rebecca Elizabeth Johnson ,  William P. Kaplan ,  Solomon D. Kattar ,  Mitchell H. Keylor ,  Derun Li ,  Kaitlyn Marie Logan ,  Min Lu ,  Gregori J. Morriello ,  Santhosh F. Neelamkavil ,  Barbara Pio ,  Nunzio Sciammetta ,  Vladimir Simov ,  Jing Su ,  Luis Torres ,  Xin Yan

IPC分类号： C07D405/14 ,  C07D487/08 ,  C07D409/14 ,  C07D403/04 ,  C07D403/14 ,  C07D498/04 ,  C07D498/08 ,  C07D487/10 ,  C07D401/14 ,  C07D471/10 ,  C07D491/107 ,  C07D471/04 ,  C07D487/04 ,  A61P25/16

摘要： The present invention is directed to substituted certain 1-pyrazolyl, 5-, 6-disubstituted indazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and ring A are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.

公开(公告)号：US11274111B2

公开(公告)日：2022-03-15

申请号：US16973623

申请日：2019-06-14

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07F5/02 ,  C07K16/28

摘要： 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：US20180244712A1

公开(公告)日：2018-08-30

申请号：US15886568

申请日：2018-02-01

申请人： 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 ,  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分类号： C07H21/04 ,  C07H21/02 ,  C07H21/00 ,  C07H19/23 ,  C07H19/20 ,  A61K39/39 ,  A61K31/7084 ,  A61K31/708 ,  A61K31/7076 ,  A61K31/7064 ,  A61K31/706

摘要： 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：US20180093964A1

公开(公告)日：2018-04-05

申请号：US15722093

申请日：2017-10-02

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

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

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：US10738074B2

公开(公告)日：2020-08-11

申请号：US15752144

申请日：2016-08-11

申请人： Merck Sharp & Dohme Corp. ,  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

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： 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

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：US10414747B2

公开(公告)日：2019-09-17

申请号：US15722093

申请日：2017-10-02

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

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：US10730849B2

公开(公告)日：2020-08-04

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

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：US10703738B2

公开(公告)日：2020-07-07

申请号：US16513409

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

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：US20190337917A1

公开(公告)日：2019-11-07

申请号：US16513409

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.