NICOTINAMIDE DERIVATIVES, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND USING Russian patent published in 2007 - IPC C07D213/82 C07D401/12 C07D401/14 C07D405/12 C07D405/14 C07D409/12 C07D417/12 C07D417/14 A61K31/4418 A61K31/4427 A61P11/00 A61P19/00 A61P25/00 A61P29/00 

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to novel derivatives of nicotinamide of the general formula (I): wherein R¹ is chosen from hydrogen atom, unsubstituted or substituted (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₃-C₇)-cycloalkyl, phenyl or heteroaryl; R² is chosen from hydrogen atom, (C₁-C₆)-alkyl and group -(CH₂)_q-(C₃-C₇)-cycloalkyl, or -(CH₂)_mR¹ and R² in common with nitrogen atom to which they are bound form (four-six)-membered heterocyclic ring; R³ represents chlorine atom or methyl group; R⁴ represents group -NH-CO-R⁷ or -CO-NH-(CH₂)_q-R⁸; R⁷ is chosen from hydrogen atom, (C₁-C₆)-alkyl, group -(CH₂)_q-(C₃-C₇)-cycloalkyl and others; R⁸ is chosen from hydrogen atom, (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl and others; each X and Y is chosen independently from hydrogen atom, methyl group and halogen atom; Z represents halogen atom; m is chosen from 0,1, 2, 3 and 4; n and q are chosen from 0, 1 and 2, and to pharmaceutically acceptable salts or their solvates. Indicated compounds possess inhibitory activity with respect to p38 kinase and can be used in medicine.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

15 cl, 127 ex