公开(公告)号：US20150191461A1

公开(公告)日：2015-07-09

申请号：US14409133

申请日：2013-06-18

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

Inventor： Michelle R. Machacek ,  Michael D. Altman ,  Eric T. Romeo ,  Dilrukshi Vitharana ,  Brandon Cash ,  Tony Siu ,  Matthew Christopher ,  Solomon D. Kattar ,  Andrew M. Haidle ,  Kaleen Konrad Childers ,  Matthew L. Maddess ,  Michael H. Reutershan ,  Yves Ducharme ,  David J. Guerin ,  Kerrie Spencer ,  Christian Beaulieu ,  Vouy Linh Truong ,  Daniel Guay ,  Alan B. Northrup ,  Brandon M. Taoka ,  Jongwon Lim ,  Christian Fischer ,  John W. Butcher ,  Ryan D. Otte ,  Binyuan Sun ,  John Michael Ellis

IPC: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D409/14 ,  C07D403/14 ,  C07D403/12

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Abstract translation: 本发明提供了式I的新型吡唑衍生物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。

公开(公告)号：US09242984B2

公开(公告)日：2016-01-26

申请号：US14409133

申请日：2013-06-18

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

Inventor： Michelle R. Machacek ,  Michael D. Altman ,  Eric T. Romeo ,  Dilrukshi Vitharana ,  Brandon Cash ,  Tony Siu ,  Hua Zhou ,  Matthew Christopher ,  Solomon D. Kattar ,  Andrew M. Haidle ,  Kaleen Konrad Childers ,  Matthew L. Maddess ,  Michael H. Reutershan ,  Yves Ducharme ,  David J. Guerin ,  Kerrie Spencer ,  Christian Beaulieu ,  Vouy Linh Truong ,  Daniel Guay ,  Alan B. Northrup ,  Brandon M. Taoka ,  Jongwon Lim ,  Christian Fischer ,  John W. Butcher ,  Ryan D. Otte ,  Binyuan Sun ,  John Michael Ellis

IPC: C07D401/00 ,  A61K31/00 ,  C07D471/04 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Abstract translation: 本发明提供了式I的新型吡唑衍生物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。

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：US20170369507A1

公开(公告)日：2017-12-28

申请号：US15532549

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Fischer Christian ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  Michael J. Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael H. Reutershan ,  Nunzio Sciammetta ,  Patrick Pengcheng Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig R. Gibeau

IPC: C07D498/08 ,  C07D471/04 ,  C07D498/10 ,  C07D471/08 ,  A01N43/00

CPC classification number: C07D498/08 ,  A01N43/00 ,  A61K31/551 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D498/04 ,  C07D498/10

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：US20170071935A1

公开(公告)日：2017-03-16

申请号：US15125373

申请日：2015-03-09

Applicant: Michael D. ALTMAN ,  Brandon CASH ,  John Michael ELLIS ,  Matthew L. MADDESS ,  Alan B. NORTHRUP ,  Ryan D. OTTE ,  Binyuan SUN ,  Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Brandon Cash ,  John Michael Ellis ,  Matthew L. Maddess ,  Alan B. Northrup ,  Ryan D. Otte ,  Binyuan Sun

IPC: A61K31/497 ,  C07D405/04 ,  C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D491/056 ,  A61K45/06 ,  C07D409/14

CPC classification number: A61K31/497 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D491/056 ,  A61K2300/00

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

Abstract translation: 本发明提供了一些式（I）的吡嗪-2-甲酰胺化合物或其药学上可接受的盐，其中A，B和X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）介导的疾病或病症的方法。

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：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：US20150353535A1

公开(公告)日：2015-12-10

申请号：US14653488

申请日：2013-12-19

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Michael D. Altman ,  Brian M. Andresen ,  Kenneth L. Arrington ,  Kaleen Konrad Childers ,  Maria Emilia Di Francesco ,  John Michael Ellis ,  Andrew M. Haidle ,  Yuan Liu ,  Alan B. Northrup ,  Brendan O'Boyle ,  Ryan D. Otte ,  Michael H. Reutershan ,  Dilrukshi Vitharana ,  Hyun Chong Woo

IPC: C07D417/14 ,  A61K31/444

CPC classification number: C07D417/14 ,  A61K31/444 ,  A61K45/06

Abstract: The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript 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).

Abstract translation: 本发明提供了式（I）（I）的某些噻唑取代的氨基吡啶化合物或其药学上可接受的盐，其中R1，R2，R3，R4，R5，R6，Cy和下标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）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。