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).

公开(公告)号：EP2632908B1

公开(公告)日：2016-05-25

申请号：EP11835401.8

申请日：2011-10-27

申请人： Merck Canada Inc.

发明人： MORADEI, Oscar, M. ,  CRANE, Sheldon ,  MCKAY, Daniel, J. ,  LEBRUN, Marie-Eve ,  TRUONG, Vouy Linh

IPC分类号： C07D277/62 ,  A61K31/27 ,  A61K31/415 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/506 ,  A61P31/18 ,  C07C311/29 ,  C07C311/41 ,  C07C317/40 ,  C07C323/49 ,  C07D231/12 ,  C07D261/08 ,  C07D417/12 ,  C07D417/14

CPC分类号： C07C311/18 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/63 ,  A61K31/635 ,  A61K45/06 ,  C07C311/29 ,  C07C311/41 ,  C07C317/40 ,  C07C323/49 ,  C07C2601/02 ,  C07D213/75 ,  C07D231/12 ,  C07D239/26 ,  C07D261/08 ,  C07D277/62 ,  C07D277/64 ,  C07D417/12 ,  C07D417/14

公开(公告)号：EP2632908A1

公开(公告)日：2013-09-04

申请号：EP11835401.8

申请日：2011-10-27

申请人： Merck Canada Inc.

发明人： MORADEI, Oscar, M. ,  CRANE, Sheldon ,  MCKAY, Daniel, J. ,  LEBRUN, Marie-Eve ,  TRUONG, Vouy Linh

IPC分类号： C07D277/62 ,  A61K31/27 ,  A61K31/415 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/506 ,  A61P31/18 ,  C07C311/29 ,  C07C311/41 ,  C07C317/40 ,  C07C323/49 ,  C07D231/12 ,  C07D261/08 ,  C07D417/12 ,  C07D417/14

CPC分类号： C07C311/18 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/63 ,  A61K31/635 ,  A61K45/06 ,  C07C311/29 ,  C07C311/41 ,  C07C317/40 ,  C07C323/49 ,  C07C2601/02 ,  C07D213/75 ,  C07D231/12 ,  C07D239/26 ,  C07D261/08 ,  C07D277/62 ,  C07D277/64 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of Formula I are disclosed: wherein L, A, R
1 , R
2 , R
3A , R
3B , R
4A , R
4B , R
5 , R
6 and R
7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.