公开(公告)号：US20150166486A1

公开(公告)日：2015-06-18

申请号：US14409200

申请日：2013-06-17

Applicant: Merck Sharp & Dohme Corp.

Inventor： Andrew M. Haidle ,  Michael D. Altman ,  Solomon D. Kattar ,  Matthew Christopher ,  John Michael Ellis ,  Christian Fischer ,  Alan B. Northrup ,  Kaleen Konrad Childers

IPC: C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D403/04 ,  C07D403/12 ,  A61K31/55 ,  C07D405/12 ,  A61K31/541 ,  C07D401/12 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/506 ,  C07D409/12

CPC classification number: C07D239/42 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D239/47 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t 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.

Abstract translation: 本发明提供了式（I）（I）的某些取代的二嗪和三嗪化合物或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy和t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：US20150148327A1

公开(公告)日：2015-05-28

申请号：US14409151

申请日：2013-06-17

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： Andrew M. Haidle ,  Sandra Lee Knowles ,  Solomon D. Kattar ,  Denis Deschenes ,  Jason Burch ,  Joel Robichaud ,  Matthew Christopher ,  Michael D. Altman ,  James P. Jewell ,  Alan B. Northrup ,  Marc Blouin ,  John Michael Ellis ,  Hua Zhou ,  Christian Fischer ,  Adam J. Schell ,  Michael H. Reutershan ,  Brandon M. Taoka ,  Anthony Donofrio ,  Joel Robichaud

IPC: C07D401/12 ,  A61K31/506 ,  C07D471/04 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/551 ,  C07D405/14 ,  C07D401/14 ,  C07D471/10 ,  C07D491/107 ,  C07D491/113 ,  C07D417/14 ,  C07D413/14 ,  C07D487/04 ,  A61K31/5377

CPC classification number: C07D401/12 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/551 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04 ,  A61K2300/00

Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t 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.

Abstract translation: 本发明提供了式（I）的某些取代的吡啶或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，Rcy，Cy和t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：US20140243336A1

公开(公告)日：2014-08-28

申请号：US14349551

申请日：2012-10-01

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Michael D. Altman ,  Corey E. Bienstock ,  John W. Butcher ,  Kaleen Konrad Childers ,  Maria Emilia Di Francesco ,  Anthony Donofrio ,  John Michael Ellis ,  Christian Fischer ,  Andrew M. Haidle ,  James P. Jewell ,  Sandra Lee Knowles ,  Alan B. Northrup ,  Ryan D. Otte ,  Scott L. Peterson ,  Graham Frank Smith

IPC: C07D401/14 ,  A61K31/444 ,  C07D405/14 ,  C07D487/04 ,  A61K31/506 ,  C07D409/14 ,  A61K31/5377 ,  A61K31/519 ,  A61K31/496 ,  A61K31/4439 ,  C07D213/81 ,  A61K31/5025

CPC classification number: A61K31/4439 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04

Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B 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.

Abstract translation: 本发明提供了具有式（I）的某些含2-吡啶甲酰胺的化合物或其药学上可接受的盐，其中A和B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：US11453697B1

公开(公告)日：2022-09-27

申请号：US16904888

申请日：2020-06-18

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Brian Andresen ,  Wonsuk Chang ,  Jared N. Cumming ,  Ryan D. Otte ,  Benjamin Wesley Trotter

IPC: A01N43/04 ,  A61K31/70 ,  C07H21/04 ,  C07H21/02 ,  A61K39/39 ,  C07H19/20 ,  C07H19/23 ,  A61P35/00 ,  C07H21/00 ,  A61K31/7076 ,  A61K31/7064 ,  A61K31/7084 ,  A61K31/708 ,  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：US20220033435A1

公开(公告)日：2022-02-03

申请号：US17299355

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: C07H21/04

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, R2, R2a, 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：US20220033431A1

公开(公告)日：2022-02-03

申请号：US17299359

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, 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. (I)

公开(公告)号：US10759825B2

公开(公告)日：2020-09-01

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 ,  James P. Jewell ,  Jongwon Lim ,  Alan B. Northrup ,  Ryan D. Otte ,  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.

公开(公告)号：US10738074B2

公开(公告)日：2020-08-11

申请号：US15752144

申请日：2016-08-11

Applicant: 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

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: 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 (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

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：US09943516B2

公开(公告)日：2018-04-17

申请号：US15515388

申请日：2015-09-25

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Michael D. Altman ,  Brian M. Andresen ,  Jason D. Brubaker ,  Anthony Donofrio ,  Thierry Fischmann ,  Craig R. Gibeau ,  Charles A. Lesburg ,  Jongwon Lim ,  John K. F. Maclean ,  Umar F. Mansoor ,  Alan B. Northrup ,  John M. Sanders ,  Graham F. Smith ,  Luis Torres

IPC: A61K31/517 ,  C07D405/04 ,  A61K45/06 ,  C07D239/94

CPC classification number: A61K31/517 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  C07D239/94 ,  C07D405/04 ,  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.