公开(公告)号：US10947234B2

公开(公告)日：2021-03-16

申请号：US16762201

申请日：2018-11-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michelle R. Machacek ,  David J. Witter ,  Michael Hale Reutershan ,  Michael D. Altman ,  Paul Anthony Stupple

IPC: C07D471/04

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：US10086000B2

公开(公告)日：2018-10-02

申请号：US15532548

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

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

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

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：US09745295B2

公开(公告)日：2017-08-29

申请号：US14786464

申请日：2014-04-22

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

Inventor： Neville J. Anthony ,  Brian M. Andresen ,  Alan B. Northrup ,  Kaleen K. Childers ,  Anthony Donofrio ,  Thomas A. Miller ,  Yuan Liu ,  Michelle R. Machacek ,  Hyun Chong Woo ,  Kerrie B. Spencer ,  John Michael Ellis ,  Michael D. Altman ,  Eric T. Romeo ,  Daniel Guay ,  Jonathan Grimm ,  Marie-Eve Lebrun ,  Joel S. Robichaud ,  Liping Wang ,  Byron DuBois ,  Qiaolin Deng

IPC: A61K31/4439 ,  A61K31/53 ,  A61K31/501 ,  A61K31/497 ,  A61K31/506 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D417/14 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  C07D417/12

Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 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).

公开(公告)号：US20160311813A1

公开(公告)日：2016-10-27

申请号：US15105411

申请日：2014-12-15

Applicant: Michelle R. MACHACEK ,  Eric T. ROMEO ,  Alan B. NORTHUP ,  Michael D. ALTMAN ,  MERCK SHARP & DOHME CORP.

Inventor： Michelle R. Machacek ,  Eric T. Romeo ,  Alan B.. Nortrup ,  Michael D. Altman

IPC: C07D417/12 ,  A61K31/5377 ,  A61K31/433 ,  A61K31/427 ,  A61K45/06

CPC classification number: C07D417/12 ,  A61K31/427 ,  A61K31/433 ,  A61K31/5377 ,  A61K45/06

Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R3, R5, R6, A, Cy and the subscripts r, s, 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).

公开(公告)号：US10508108B2

公开(公告)日：2019-12-17

申请号：US15532552

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Dawn M. Hoffman ,  Chunhui Huang ,  Solomon D. Kattar ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Michael H. Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla ,  Zhicai Wu ,  Yang Yu ,  Craig R. Gibeau

IPC: C07D471/04 ,  C07D471/14 ,  C07D519/00

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), and (II-ii). 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：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：US20170362220A1

公开(公告)日：2017-12-21

申请号：US15532552

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  Michael J. Ellis ,  Sara Esposite ,  Dawn M. Hoffman ,  Chunhui Huang ,  Solomon D. Kattar ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Michael H. Reutershan ,  Nunzio Sciammetta ,  Patrick Pengcheng Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla ,  Zhicai Wu ,  Yang Yu ,  Craig R. Gibeau

IPC: C07D471/04 ,  C07D519/00 ,  C07D471/14

CPC classification number: C07D471/04 ,  C07D471/14 ,  C07D519/00

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), and (II-ii). 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：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：US09783531B2

公开(公告)日：2017-10-10

申请号：US15105411

申请日：2014-12-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michelle R. Machacek ,  Eric T. Romeo ,  Alan B. Northrup ,  Michael D. Altman

IPC: C07D417/12 ,  A61K45/06 ,  A61K31/427 ,  A61K31/433 ,  A61K31/5377

CPC classification number: C07D417/12 ,  A61K31/427 ,  A61K31/433 ,  A61K31/5377 ,  A61K45/06

Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R3, R5, R6, A, Cy and the subscripts r, s, 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).

公开(公告)号：US20140323440A1

公开(公告)日：2014-10-30

申请号：US14328329

申请日：2014-07-10

Applicant: Merck Sharp & Dohme Corp.

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

IPC: C07F5/02 ,  C07F9/6558 ,  C07D417/14

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

Abstract: 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.

Abstract translation: 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。