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：US08993756B2

公开(公告)日：2015-03-31

申请号：US14363097

申请日：2012-11-30

Applicant: Merck Sharp & Dohme Corp.

Inventor： Sean P. Ahearn ,  Matthew Christopher ,  Christopher Dinsmore ,  Joon Jung ,  Qinglin Pu ,  Alexey Rivkin ,  Mark E. Scott ,  David J. Witter ,  Hyun Chong Woo ,  Brandon Cash

IPC: C07D487/04 ,  C07D417/04 ,  C07D413/04 ,  A61K31/519 ,  A61P19/02 ,  C07D519/00 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.

Abstract translation: 本发明提供了作为JAK3抑制剂的式I化合物。 具体地，式I化合物是吡咯并[2,3-d]嘧啶衍生物化合物。 本发明还提供了通过给予式I的吡咯并[2,3-d]嘧啶衍生物化合物来治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症的方法。

公开(公告)号：US20140349998A1

公开(公告)日：2014-11-27

申请号：US14363097

申请日：2012-11-30

Applicant: Merck Sharp & Dohme Corp.

Inventor： Sean P Ahearn ,  Matthew Christopher ,  Christopher Dinsmore ,  Joon Jung ,  Qinglin Pu ,  Alexey Rivkin ,  Mark E. Scott ,  David J. Witter ,  Hyun Chong Woo ,  Brandon Cash

IPC: C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.

Abstract translation: 本发明提供了作为JAK3抑制剂的式I化合物。 具体地，式I化合物是吡咯并[2,3-d]嘧啶衍生物化合物。 本发明还提供了通过给予式I的吡咯并[2,3-d]嘧啶衍生物化合物来治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症的方法。

公开(公告)号：US20140228348A1

公开(公告)日：2014-08-14

申请号：US14345978

申请日：2012-09-21

Applicant: MERCK SHARP& DOHME CORP.

Inventor： Jason Brubaker ,  Matthew Lloyd Childers ,  Matthew Christopher ,  Joshua T. Close ,  Jason David Katz ,  Joon Jung ,  Scott Peterson ,  Phieng Siliphaivanh ,  Tony Siu ,  Graham Frank Smith ,  Luis E. Torres ,  Hyun Chong Woo ,  Jonathan R. Young ,  Hongjun Zhang

IPC: C07D231/38 ,  C07D405/04 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04

CPC classification number: C07D405/08 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

Abstract translation: 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。