2-PYRIDYL-SUBSTITUTED IMIDAZOLES AS THERAPEUTIC ALK5 AND/OR ALK4 INHIBITORS Russian patent published in 2014 - IPC C07D471/04 A61K31/437 A61P13/12 A61P11/00 A61P19/10 A61P25/28 

FIELD: chemistry.

SUBSTANCE: described are novel 2-pyridyl-substituted imidazoles of general formula (I) , where R^a is C_1-6alkyl; m = 1; A¹ = N; A² = NR¹, where R¹ is hydrogen; X is bond, -NR²-, -O- or -S-, where R² is hydrogen or C_1-3alkyl; R^b independently is H, halogen, C_1-6alkyl, C_2-6alkenyl, C_2-6alkinyl, -(CH₂)_q-OR³, where R³ - C_1-6alkyl or C_1-6halogene alkyl, and q=0,1, -(CH₂)_q-NR³R⁴, where R³ and R⁴ independently are C_1-6alkyl or together with nitrogen atom - pyrrolidinyl or morpholinyl, and q=0-2; -SR³, where R³ - C_1-6alkyl, -(CH₂)_q-CN, where q=0 or 1, -COR³ or -CO₂R³, where R³ is C_1-6alkyl, -CONR³R⁴, where R³ and R⁴ is hydrogen, -NHCOR³ or -NHSO₂R³, where R³ stands for C_1-6alkyl; n equals 0, 1, 2, 3, 4 or 5; or their pharmaceutically acceptable salts, or hydrates and pharmaceutically acceptable compositions for treatment or abatement of metastasis of tumour cells, carcinomas, fibrosis by inhibiting pathways of transmission of signal of TGF-β or activin, or both.

EFFECT: improvement of composition properties.

6 cl, 6 tbl, 7 ex, 33 dwg