发明名称 PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK
摘要 The present invention relates to a compound of formula (I):;;or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.
申请公布号 US2014155410(A1) 申请公布日期 2014.06.05
申请号 US201414174198 申请日期 2014.02.06
申请人 GlaxoSmithKline LLC 发明人 Adams Jerry Leroy;Faitg Thomas H.;Johnson Neil W.;Kasparec Jiri;Lin Hong;Mellinger Mark;Peng Xin;Xie Ren
分类号 C07D401/14;C07D401/12 主分类号 C07D401/14
代理机构 代理人
主权项 1. A compound of formula (I): or a salt thereof, wherein: R1 is halo, CF3, C1-C6-alkyl, isopropenyl, (C2-C6-alkylene) C3-C6-cycloalkyl, C1-C6-alkoxy, or cyano; in R2, when p is other than 0, each R2 is independently F, Cl, CF3, methyl, methoxy, CH2CF3, —(X)q—C1-C4-alkylene-R4, —(X—C1-C4-alkylene)q-NR5—C(O)—R6, —(X—C1-C4-alkylene)q-(NR5)q—SOx—R7, —(X—C1-C4-alkylene)q-Y—N(R8)2, a 5- to 6-membered heterocycloalkyl-(R9)q group, or a 5- to 6-membered heteroaryl-(R10)r group; each R3 is independently H, C3-C6-cycloalkyl, C1-C6-alkyl, C1-C6alkoxy, C1-C6-alkylene-R4, —N(R)2, O—C1-C6-alkylene-R4, or, the R3 groups, together with Z form a 5- to 6-membered cycloalkyl or cycloheteroalkyl where the hetero atom is N or O and ring is optionally substituted on a carbon or heteroatom by methyl, C1-C4-alkylene-R4, or C3-C6-cycloalkyl; R4 is H, -(Q)q-N(R8)2, OH, SH, C1-C6-alkoxy, C1-C6-thioalkyl, or a 5- to 6-membered heterocycloalkyl-(R9)q group; R5 is H or C1-C6-alkyl; R6 is H, C1-C6-alkyl, C1-C6-alkoxy, N(R8)2, or a 5- to 6-membered heteroaryl-(R10)r group; R7 is C1-C6-alkyl, phenyl-(R9)q, or 5- to 6-membered heteroaryl-(R10)r R8 is independently H, C1-C6-alkyl, —O—C1-C6-alkyl or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group; R9 is H, C1-C6-alkyl, C1-C6-alkoxy, -(Q)q-N(R8)2, -Q-C1-C6-alkyl, —C1-C6alkylR4, or 5- to 6-membered heterocycloalkyl; R10 is H, C1-C6-alkyl, C1-C6-alkoxy, or -Q-C2-C6-alkyl; R11 is C1-C6-alkyl, CF3, —CH2CF3, -(Q)q-C1-C4-alkylene-R4, -Q-N(R8)2, phenyl-(R5)s, a 5- to 6-membered heterocycloalkyl-(R9)q group, or a 5- to 6-membered heteroaryl-(R10)r group; R12 is H, C1-C6-alkyl, F, Cl, CF3, OH, CN, nitro, COOH, —COO—C1-C6-alkyl, —C1-C6-alkylOH, —C1-C6-alkylN(R8)2, —Y—N(R8)2, C3-C6-cycloalkyl-R14, —(X)q—C1-C6-alkylene-R4, —(X—C1-C6-alkylene)q-NR5—C(O)—R6, —(X—C1-C6-alkylene)q-(NR5)q—SOx—R7, —(X—C1-C6-alkylene)q-Y—N(R8)2, heterocycloalkyl-(R9)q, heteroaryl-(R8)r, or phenyl-(R15)s; R13 is H, F, Cl, C1-C6-alkyl, or C3-C6-cycloalkyl; or R12 and R13, together with the carbon atoms to which they are attached, form a fused 5- or 6-membered carbocycloalkyl or heterocycloralkyl group; R14 is independently H, C1-C6-alkyl. —NR5—SO2—R7, —Y—N(R8)2, or —(X)q—C1-C6-alkylene-R4; each R15 is independently F, Cl, CF3, C1-C3-alkyl, or C1-C3-alkoxy; p is 0, 1, 2, or 3; q is 0 or 1; r is 0, 1, or 2; s is 0, 1, 2, or 3; x is 1 or 2; Q is —C(O)—, —S(O)—, or —SO2—; X is NR5, O, S, —S(O)—, or —SO2—; Y is a bond, SO2, or C(O); and Z is N or CR5.
地址 Wilmington DE US