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US 2014/0155410 A1Published application
Pyrazolylaminopyridines as inhibitors of fak
AssigneeGlaxoSmithKline LLC
InventorsJerry Leroy Adams, Thomas H. Faitg, Neil W. Johnson, Jiri Kasparec, Hong Lin, Mark Mellinger, Xin Peng, Ren Xie
Life of this patent
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Abstract
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.
Claims13
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.
24 more elements
Dependencies are inferred from the claim text.