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

申请人： Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

发明人： 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分类号： A01N43/54 ,  A61K31/505

CPC分类号： C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10

摘要： 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：EP2512246B1

公开(公告)日：2015-09-30

申请号：EP10838241.7

申请日：2010-12-16

申请人： Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

发明人： 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分类号： C07D417/14 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  A61K31/505 ,  A61P11/06

CPC分类号： C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10

公开(公告)号：EP2988744A1

公开(公告)日：2016-03-02

申请号：EP14788026.4

申请日：2014-04-22

申请人： Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

发明人： ANTHONY, Neville, J. ,  ANDRESEN, Brian, M. ,  NORTHRUP, Alan, B. ,  CHILDERS, Kaleen, K. ,  DONOFRIO, Anthony ,  MILLER, Thomas, A. ,  LIU, Yuan ,  MACHACEK, Michelle, R. ,  WOO, Hyun Chong ,  SPENCER, Kerrie, B. ,  ELLIS, John Michael ,  ALTMAN, Michael, D. ,  ROMEO, Eric, T. ,  GUAY, Daniel ,  GRIMM, Jonathan ,  LEBRUN, Marie-Eve ,  ROBICHAUD, Joel, S. ,  WANG, Liping ,  DUBOIS, Byron ,  DENG, Qiaolin

IPC分类号： A61K31/44 ,  A61K31/53 ,  A61K31/426

CPC分类号： C07D417/14 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  C07D417/12

摘要： 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).