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

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

发明人： 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分类号： C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00

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

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.

摘要翻译： 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：EP2706852B1

公开(公告)日：2018-08-22

申请号：EP12782391.2

申请日：2012-05-04

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

发明人： DESCHENES, Denis ,  ALTMAN, Michael D. ,  ELLIS, John Michael ,  FISCHER, Christian ,  HAIDLE, Andrew M. ,  KATTAR, Solomon D. ,  NORTHRUP, Alan B. ,  SCHELL, Adam J. ,  SMITH, Graham F. ,  TAOKA, Brandon M. ,  BIENSTOCK, Corey ,  DI FRANCESCO, Maria Emilia ,  DONOFRIO, Anthony ,  PETERSON, Scott ,  SPENCER, Kerrie B. ,  JEWELL, James Patrick ,  ALI, Amjad ,  BENNETT, David Jonathan ,  DANG, Qun ,  WAI, John

IPC分类号： A01N43/40 ,  A61K31/44 ,  C07D213/04

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.

公开(公告)号：EP3148996A1

公开(公告)日：2017-04-05

申请号：EP15803641.8

申请日：2015-05-28

申请人： Merck Sharp & Dohme Corp.

发明人： WALSH, Shawn P. ,  CUMMING, Jared N. ,  HE, Shuwen ,  TAOKA, Brandon M. ,  TRUONG, Quang T. ,  WU, Wen-Lian

IPC分类号： C07D417/14

CPC分类号： C07D487/04 ,  C07D471/04

摘要： In its many embodiments, the present invention provides certain C2-carbocyclic iminothiazine dioxide compounds, including compounds Formula (I); or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, n, ring C, RC and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

摘要翻译： 在其许多实施方案中，本发明提供某些C2-碳环亚氨基噻嗪二氧化物化合物，包括式（I）化合物; 或其互变异构体和所述化合物和所述互变异构体的药学上可接受的盐，其中R1，R2，环A，RA，m，环B，RB，n，环C，RC和p如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。

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

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

发明人： 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分类号： C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00

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

公开(公告)号：EP2706852A1

公开(公告)日：2014-03-19

申请号：EP12782391.2

申请日：2012-05-04

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

发明人： DESCHENES, Denis ,  ALTMAN, Michael D. ,  ELLIS, John Michael ,  FISCHER, Christian ,  HAIDLE, Andrew M. ,  KATTAR, Solomon D. ,  NORTHRUP, Alan B. ,  SCHELL, Adam J. ,  SMITH, Graham F. ,  TAOKA, Brandon M. ,  BIENSTOCK, Corey ,  DI FRANCESCO, Maria Emilia ,  DONOFRIO, Anthony ,  PETERSON, Scott ,  SPENCER, Kerrie B. ,  JEWELL, James Patrick ,  ALI, Amjad ,  BENNETT, David Jonathan ,  DANG, Qun ,  WAL, John

IPC分类号： A01N43/40 ,  A61K31/44 ,  C07D213/04

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.

摘要翻译： 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，或者是其前药，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎和癌症。