公开(公告)号：US11098059B2

公开(公告)日：2021-08-24

申请号：US16762114

申请日：2018-11-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michelle R. Machacek ,  David J. Witter ,  Michael Hale Reutershan ,  David L. Sloman ,  Michael D. Altman

IPC: A61K31/438 ,  A61K31/439 ,  A61K31/4704 ,  C07D498/08 ,  C07D401/06 ,  C07D401/14 ,  C07D453/06

Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

公开(公告)号：US20170360800A1

公开(公告)日：2017-12-21

申请号：US15532548

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew Lloyd Childers ,  Francesc Xavier Fradera Llinas ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Nunzio Sciammetta ,  Patrick Pengcheng Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla

IPC: A61K31/5513 ,  C07D471/14 ,  C07D471/04 ,  A61K45/06 ,  C07D519/00 ,  A01N43/00

CPC classification number: A61K31/5513 ,  A01N43/00 ,  A61K31/551 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00 ,  A61K2300/00

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N═; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). 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：US09624210B2

公开(公告)日：2017-04-18

申请号：US14651558

申请日：2013-12-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michelle R. Machacek

IPC: C07D417/12

CPC classification number: C07D417/12

Abstract: The invention provides certain amino-pyrimidine-containing compounds. 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.

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：US20150329531A1

公开(公告)日：2015-11-19

申请号：US14651558

申请日：2013-12-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michelle R. Machacek

IPC: C07D417/12

CPC classification number: C07D417/12

Abstract: The invention provides certain amino-pyrimidine-containing compounds. 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: 本发明提供某些含氨基嘧啶的化合物。 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。