发明名称 SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS
摘要 Provided are substituted pyrimidinyl compounds for inhibition of JAK and/or Syk kinase, pharmaceutical compositions thereof, methods for inhibiting JAK and/or Syk kinase activity, and methods for treating conditions mediated at least in part by JAK and/or Syk kinase activity.
申请公布号 US2015259328(A1) 申请公布日期 2015.09.17
申请号 US201314434075 申请日期 2013.10.08
申请人 PORTOLA PHARMACEUTICALS, INC. 发明人 Bauer Shawn M.;Jia Zhaozhong J.;Song Yonghong;Pandey Anjali
分类号 C07D405/14;C07D403/12;C07D401/14;C07D239/48;C07D401/12 主分类号 C07D405/14
代理机构 代理人
主权项 1. A compound of Formula (I): or a tautomer or a pharmaceutically acceptable salt thereof, wherein R1 is selected from the group consisting of H, halo, C1-4 alkoxy, and cyano; R2 is selected from the group consisting of H, halo, and C1-4 alkyl; Y is selected from the group consisting of ethyl, isopropyl, trifluoromethyl, fluoro, cyclopropyl, 1,2,3,6-tetrahydropyridin-4-yl, 4-(1-ethylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl, N-morpholino, piperidin-4-yl, 4-(vinylsulfonyl)piperazin-1-yl and T and W are independently N or C provided that at least one of T and W is N; R3 is selected from the group consisting of C1-5alkyl, cyanoC1-4 alkylene, C3-6 cycloalkyl, oxetan-3-yl, 1-cyclopropylpiperidin-4-yl, tetrahydropyran-4-yl, phenyl, pyridin-2-yl, 3-fluoropyridin-2-yl, pyridin-3-yl, HC(O), R3aC(O), R3bS(O)2, and R3cS(O)2; R3a is selected from the group consisting of ethyl, cyanoC1-4alkylene, C1-4alkoxy, C1-4 alkoxyC1-4 alkyl, N-morpholino, tetrahydropyran-4-yl, pyridin-3-yl, C3-6 cycloalkyl, 1-cyanocyclopropyl, pyrrolidin-1-yl, and (R3c)2N; R3b is selected from the group consisting of cyclopropyl, pyridin-3-yl, 1-methyl-imidazol-4-yl, 1-methyl-pyrazol-4-yl, ethenyl, and (R3c)2N; R3c is independently C1-4alkyl; the subscript n is 1 or 2; the subscript m is 1 or 2; the wavy line signifies the point of attachment to the remainder of the molecule; the dashed line signifies that the bond between W and (CHp) can be a single or double bond provided that when the dashed line is a double pond, the subscript p is 1 and when the dashed line signifies that the bond between W and (CHp) is a single bond, the subscript p is 2; provided that when T is N and W is C and R3 is R3CS(O)2, then R3c is ethyl or isopropyl; provided that when that when T and W are both N, then R3 is R3CS(O)2 and R1 and R2 are not both H; and provided that when T is C and W is N and n and m are 2, R1 and R2 are not both H.
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