SELECTIVE PROTEIN KINASE INHIBITORS

摘要

The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof:;;wherein R1, R2, R3, A, Q, W and X are as defined in the description.;These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.

主权项

1. A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: A is five or six member heterocycle ring; R1 is hydrogen, halogen, a (C1-C10)alkyl group, a thio(C1-C10)alkyl group or a (C1-C10)alkoxy group; R2 is halogen, an aryl group, an halo(C1-C10)alkyl or (C1-C10)alkyl group optionally substituted with at least one heteroatom optionally substituted with an halo(C1-C10)alkyl or (C1-C10)alkyl optionally substituted with a solubilising group; as well as a (C1-C10)alkoxy group, a thio(C1-C10)alkyl group or an halo(C1-C10)alkoxy group; as well as a —COOR, —NRR′, —NR—CO—R′, —CONRR′, —SO2NRR′ or —NR—SO2—R′ group wherein R and R′ are each independently selected from hydrogen, aryl group, heteroaryl group, (C1-C10)alkyl group optionally substituted with at least one heteroatom optionally substituted with a (C1-C10)alkyl group optionally substituted with a solubilising group; as well as a heterocycle group or a solubilising group; R3 is hydrogen, halogen, cyano, a (C1-C10)alkyl group or a (C1-C10)alkoxy group; as well as CF3, —NRR′, —NR—CO—R′, —CONRR′, —SO2NRR′ group wherein R and R′ are each independently selected from hydrogen, (C1-C10)alkyl group optionally substituted with at least one heteroatom optionally substituted with a (C1-C10)alkyl group optionally substituted with a solubilising group; as well as a heterocycle group or a solubilising group; Q is O or S; W is N or CR4; R4 is hydrogen, cyano, CF3, halogen, a thio(C1-C10)alkyl group, a (C1-C10)alkyl group optionally substituted with at least one heteroatom optionally substituted with a (C1-C10)alkyl group optionally substituted with a solubilising group; as well as a (C1-C10)alkoxy group or an halo(C1-C10)alkoxy group, a solubilising group, an heterocycle, —CO—NRR′, —SO2—NRR′, —NRR′, NR—CO—R′ or —NR—SO2R′ group wherein R and R′ are each independently selected from hydrogen, (C1-C10)alkyl group optionally substituted with at least one heteroatom optionally substituted with a (C1-C10)alkyl group optionally substituted with a solubilising group or heterocycle group; X is N or CR5; R5 is hydrogen, cyano, halogen, a (C1-C10)alkyl group, a (C1-C10)alkoxy group, —CO—OR, —CO—NRR′ group wherein R and R′ are each independently selected from hydrogen, (C1-C10)alkyl group optionally substituted with at least one heteroatom optionally substituted with a (C1-C10)alkyl group optionally substituted with a solubilising group or heterocycle group;