DERIVATIVES OF 3-[2-(3-ACYLAMINO-2-OXO-2H-PYRIDIN-1-YL)-ACETYLAMINO]-4-OXO-PENTANE ACID AND THEIR APPLICATION AS CASPASE INHIBITORS Russian patent published in 2011 - IPC C07D213/75 C07D401/06 C07D409/06 A61K31/4412 A61K31/4436 A61P9/10 A61P29/00 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compound of formula I: where: R¹ represents R⁶C(O)-, R⁶SO₂-, (R⁶)₂NC(O)-; R² represents hydrogen, -CF₃ or R⁸; R³ represents -T-R⁹; R⁴ represents -COOH or -COOR⁸; R⁵ represents -CH₂F or -CH₂O-2, 3, 5, 6 - tetrafluorophenyl; R⁶ represents R^6a or R^6b; two R⁶ groups, together with the atom to which they are bound optionally form 3-10-member aromatic or non-aromatic ring; and where each R⁶ is independently substituted with 6 substituents, independently selected from R; R^6a and R^6b each independently represents (C₁-C₃)-aliphatic group, (C₆-C₁₀)-aryl-, (C₆-C₁₀)-aryl-(C₁-C₁₂) aliphatic group; R represents halogen, -OR⁷, -R⁷; each R⁷ is independently selected from: hydrogen, (C₁-C₁₂)-aliphatic group, (C₆-C₁₀)-aryl; R⁸ represents (C₁-C₁₂)-aliphatic group; T represents direct bond or (C₁-C₆)-aliphatic group, where to 2 aliphatic carbon atoms in T can be optionally substituted with O; R⁹ is optionally substituted (C₆-C₁₀)-aryl or (C₅-C₁₀) - heteroaryl, invention also relates to pharmaceutical composition, to methods of treatment, inhibition of caspase-mediated processes, to method of cell preservation with application of formula I compounds application of such compositions for treatment of caspase-mediated diseases and to methods of obtaining formula I compounds.

EFFECT: obtained and described are novel compounds, which can be useful in treatment of caspase-mediated diseases.

38 cl, 22 ex