公开(公告)号：EP3083559A1

公开(公告)日：2016-10-26

申请号：EP14872226.7

申请日：2014-12-18

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

Inventor： ANDRESEN, Brian M. ,  ARRINGTON, Kenneth L. ,  OTTE, Ryan D. ,  ELLIS, John Michael ,  BUTCHER, John W. ,  NORTHRUP, Alan B. ,  ROBICHAUD, Joel S. ,  GAUTHIER, Jacques Yves ,  FOURNIER, Jean-Francois

IPC: C07D213/72

CPC classification number: C07D417/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  C07D417/12

Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R
1 , R
2 , R
3 , R
4 , ring B, and the subscript r 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: 本发明提供式（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中R1，R2，R3，R4，环B和下标r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：EP2513098A1

公开(公告)日：2012-10-24

申请号：EP10801736.9

申请日：2010-12-15

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

Inventor： ALTMANN, Michael D. ,  ANDRESEN, Brian M. ,  ARRINGTON, Kenneth L. ,  CHILDERS, Kaleen Konrad ,  DI FRANCESCO, Maria Emilia ,  DONOFRIO, Anthony ,  ELLIS, John Michael ,  FISCHER, Christian ,  GUERIN, David Joseph ,  HAIDLE, Andrew M. ,  KATTAR, Solomon ,  KNOWLES, Sandra Lee ,  LI, Chaomin ,  LIM, Jongwon ,  MACHACEK, Michelle ,  NORTHRUP, Alan B. ,  O'BOYLE, Brendan M. ,  OTTE, Ryan D. ,  PETROCCHI, Alessia ,  REUTERSHAN, Michael H. ,  ROMEO, Eric ,  SIU, Tony ,  TAOKA, Brandon M. ,  TROTTER, B. Wesley ,  ZHOU, Hua ,  BURCH, Jason ,  COTE, Bernard ,  DUPONT-GAUDET, Kristina ,  FOURNIER, Jean-Francois ,  GAUTHIER, Jacques Yves ,  GUAY, Daniel ,  ROBICHAUD, Joel S. ,  GRIMM, Jonathan ,  MADDESS, Matthew L. ,  SCHELL, Adam J. ,  SPENCER, Kerrie B. ,  WOO, Hyun Chong ,  BHAT, Sathesh

IPC: C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/08 ,  C07D495/04 ,  C07F9/65583

Abstract: The present invention provides novel pyrimidine amines 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 and rheumatoid arthritis.

Abstract translation: 本发明提供了式（I）的新型嘧啶胺，它们是脾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和类风湿性关节炎。

公开(公告)号：EP2512246A1

公开(公告)日：2012-10-24

申请号：EP10838241.7

申请日：2010-12-16

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

Inventor： ALTMAN, Michael, D. ,  ARRINGTON, Kenneth, L. ,  BURCH, Jason ,  COTE, Bernard ,  FOURNIER, Jean-Francois ,  GAUTHIER, Jacques, Yves ,  KATTAR, Solomon ,  KNOWLES, Sandra Lee ,  LIM, Jongwon ,  MACHACEK, Michelle, R. ,  NORTHRUP, Alan, B. ,  REUTERSHAN, Michael, H. ,  ROBICHAUD, Joel, S. ,  SCHELL, Adam, J. ,  SPENCER, Kerrie, B.

IPC: A01N43/54 ,  A61K31/505

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10

Abstract: The present invention provides novel pyrimidine amines 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 and rheumatoid arthritis.

公开(公告)号：EP2513098B1

公开(公告)日：2016-11-09

申请号：EP10801736.9

申请日：2010-12-15

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

Inventor： ALTMANN, Michael D. ,  ANDRESEN, Brian M. ,  ARRINGTON, Kenneth L. ,  CHILDERS, Kaleen Konrad ,  DI FRANCESCO, Maria Emilia ,  DONOFRIO, Anthony ,  ELLIS, John Michael ,  FISCHER, Christian ,  GUERIN, David Joseph ,  HAIDLE, Andrew M. ,  KATTAR, Solomon ,  KNOWLES, Sandra Lee ,  LI, Chaomin ,  LIM, Jongwon ,  MACHACEK, Michelle ,  NORTHRUP, Alan B. ,  O'BOYLE, Brendan M. ,  OTTE, Ryan D. ,  PETROCCHI, Alessia ,  REUTERSHAN, Michael H. ,  ROMEO, Eric ,  SIU, Tony ,  TAOKA, Brandon M. ,  TROTTER, B. Wesley ,  ZHOU, Hua ,  BURCH, Jason ,  COTE, Bernard ,  DUPONT-GAUDET, Kristina ,  FOURNIER, Jean-Francois ,  GAUTHIER, Jacques Yves ,  GUAY, Daniel ,  ROBICHAUD, Joel S. ,  GRIMM, Jonathan ,  MADDESS, Matthew L. ,  SCHELL, Adam J. ,  SPENCER, Kerrie B. ,  WOO, Hyun Chong ,  BHAT, Sathesh

IPC: C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/08 ,  C07D495/04 ,  C07F9/65583

公开(公告)号：EP2512246B1

公开(公告)日：2015-09-30

申请号：EP10838241.7

申请日：2010-12-16

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

Inventor： ALTMAN, Michael, D. ,  ARRINGTON, Kenneth, L. ,  BURCH, Jason ,  COTE, Bernard ,  FOURNIER, Jean-Francois ,  GAUTHIER, Jacques, Yves ,  KATTAR, Solomon ,  KNOWLES, Sandra Lee ,  LIM, Jongwon ,  MACHACEK, Michelle, R. ,  NORTHRUP, Alan, B. ,  REUTERSHAN, Michael, H. ,  ROBICHAUD, Joel, S. ,  SCHELL, Adam, J. ,  SPENCER, Kerrie, B.

IPC: C07D417/14 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  A61K31/505 ,  A61P11/06

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10