发明名称 2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
摘要 The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B 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) kinase.;
申请公布号 US9216173(B2) 申请公布日期 2015.12.22
申请号 US201214349551 申请日期 2012.10.01
申请人 Merck Sharp & Dohme Corp. 发明人 Altman Michael D.;Bienstock Corey E.;Butcher John W.;Childers Kaleen Konrad;Di Francesco Maria Emilia;Donofrio Anthony;Ellis John Michael;Fischer Christian;Haidle Andrew M.;Jewell James P.;Knowles Sandra Lee;Northrup Alan B.;Otte Ryan D.;Peterson Scott L.;Smith Graham Frank
分类号 C07D213/73;A61K31/4439;C07D401/14;C07D405/14;C07D413/14;C07D213/81;C07D401/12;C07D409/14;C07D417/14;C07D487/04;C07D495/04;A61K31/444;A61K31/496;A61K31/5025;A61K31/506;A61K31/519;A61K31/5377 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 of the Formula (I)or a pharmaceutically acceptable salt thereof, whereinB is pyridyl; wherein B is unsubstituted or substituted by 1 to 3 R3 moieties, wherein each R3 moiety is independently selected from the group consisting of C1-C3 alkyl, C1-C3 alkoxy, C1-C3 fluoroalkyl, C1-C3 hydroxyalkyl, halo, hydroxy, amino, (C1-C3 alkyl)amino, di(C1-C3 alkyl)amino, —N(H)SO2—(C1-C3 alkyl), —CO2H, —C(O)NH2, —C(O)N(H)(C1-C3 alkyl), —C(O)N(H)(C1-C3 alkyl)2, —CH2O—(C1-C4 alkylene)-OH, and E; E is (a) -E′,(b) —CH2-E1 or(c) —O—CH2-E1;wherein E1 is: (i) phenyl; or(ii) C3-C6 cycloalkyl;wherein E1 is unsubstituted or substituted by 1 to 2 moieties independently selected from the group consisting of C1-C3 alkyl, C1-C3 alkoxy, halo, hydroxy, nitro, carboxy, C1-C3 hydroxyalkyl, —O—(C1-C3 fluoroalkyl), —C(H)(OH)—(C1-C3 fluoroalkyl), —N(CH3)SO2—(C1-C3 alkyl), and RE1; wherein RE1 is(a) —(CH2)x—RE1a, wherein x is 1, 2, or 3; or(b) —RE1a;wherein RE1a is phenyl; wherein RE1a is unsubstituted or substituted by 1 to 2 moieties independently selected from the group consisting of C1-C3 alkyl, C1-C3 alkoxy and halo;A is selected from the group consisting of (a)  wherein Y is —CH—;R11 and R12 are independently H or F; andn is 1 or 2;n′ is 0 or 1; or (b)  wherein Ra and Rb are independently H, C1-C6 alkyl, or phenyl; or Ra and Rb together with the carbon atom to which they are attached form —C(O)—;Q is  —C(O)—, or —CH2CH2—; wherein Rc is H, C1-C6 alkyl, C1-C3 fluoroalkyl, C3-C6 cycloalkyl, —(CH2)rOR13, —C(O)NH2, —C(O)N(H)(C1-C3 alkyl), —C(O)N(C1-C3 alkyl)2, —(CH2)rS(O)tR14, —(CH2)r-phenyl, or —(CH2)rN(H)C(O)—(C1-C3 alkyl); R13 is H or C1-C3 alkyl; andR14 is C1-C3 alkyl;r is 1 or 2;t is 0, 1, or 2;Rd is H or C1-C6 alkyl, orRc and Rd together with the carbon atom to which they are attached form a group of the formula  wherein q is 1, 2, 3, or 4; or (c)  wherein m is 1 or 2 and m′ is 0 or 1; (e) H; (f) —C(O)N(H)—(C1-C3 alkyl); and (g) —S(O)2CH2CH2NH2.
地址 Rahway NJ US