发明名称 Bipyridylaminopyridines as Syk inhibitors
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.
申请公布号 US9145391(B2) 申请公布日期 2015.09.29
申请号 US201214116199 申请日期 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
分类号 C07D213/73;C07D401/14;C07D401/12;C07D409/14;C07D417/14;C07D471/04 主分类号 C07D213/73
代理机构 代理人 Meade Eric A.;Fitch Catherine D.
主权项 1. A compound having formula Ia or a pharmaceutically acceptable salt thereof, wherein R1 is C1-4alkyl, C1-4fluoroalkyl, C3-6cycloalkyl or C1-4alkoxy; R2 is H or halogen; R3 is H, halogen, NRbRc, C1-4alkyl, C1-4haloalkyl, C3-6cycloalkyl or C1-4hydroxyalkyl; Y is selected from the group consisting of a bond, —NH—, and —C(R5)(R6)—; R5 is H, OH, C1-4 alkoxy or halogen; R6 is H, C1-4alkyl, C1-4haloalkyl, C3-6cycloalkyl or C1-4hydroxyalkyl; Z is (a) an optionally benzofused C3-6cycloalkyl optionally substituted with 1-5 groups independently selected from C1-4alkyl, ORa, CO2Ra, and CONRbRc; Ra is selected from the group consisting of: (i) H;(ii) C1-8 alkyl;(iii) a group of the formula -M-RCH, wherein M is a bond or —(CH2)1-2-;RCH is aryl or carbocycle optionally substituted with 1-3 groups independently selected from halo, C1-4alkyl, or C1-4alkoxy;(iv) a group of the formula —(CH2)1-2—Re or —(CH2)2—O—(CH2)2—Re wherein Re is CO2Re1, C(O)N(Re2)2, or —O(CO)Re1; Re1 is C1-4alkyl; andRe2 is H or C1-4alkyl;(v) a group of the formula —(CH2)2—Rf, Rf is OH, —OC1-4alkyl, NH2, —N(H)(C1-4alkyl) or N(C1-4alkyl)2;(vi) a group of the formula wherein Rg is H or C1-4alkyl; andRh is C1-4alkyl, C3-6cycloalkyl, or phenyl; and,(vii) a group of the formula wherein Rg and Rh are as set forth above; Rb and Rc are each independently selected from H and C1-4alkyl.
地址 Rahway NJ US