CARBOXAMIDE COMPOUNDS AND USE THEREOF AS CALPAIN INHIBITORS Russian patent published in 2015 - IPC C07D207/28 C07D401/04 C07D401/14 C07D413/14 A61K31/4439 A61K31/4015 A61P25/28 A61P27/08 A61P35/00 A61P13/12 A61P31/00 A61P31/18 A61P25/00 A61P9/00 A61P21/00 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, particularly to novel carboxamide compounds of formula and to pharmaceutically acceptable salts thereof, where R¹ is phenyl-C₁-C₆-alkyl, where the phenyl can be unsubstituted or substituted with 1 radical R^1c; where R^1c is independently selected from halogen, C₁-C₆-alkyl, C₁-C₆-alkoxy, where the C₁-C₆alkyl groups can be partially or completely halogenated or can have 1, 2 or 3 substitutes R^1a, and -(CH₂)_p-NR^c6R^c7, where p=0, 1, where R^1a is independently selected from NR^a6R^a7, R^a6 is C₁-C₆-alkyl, R^a7 is C₁-C₆-alkyl, or two radicals R^a6 and R^a7, or R^c6 and R^c7 together with a N atom form a nitrogen-containing 6-member saturated heterocycle, which can optionally have 1 additional O heteroatom as a ring member, R² is phenyl, pyridyl, where the phenyl can be unsubstituted or can have 1 substitute R^2c; where R^2c has one of the values given for R^1c; R³ is C₁-C₆-alkyl, C₃-C₆-alkenyl, C₃-C₆-cycloalkyl, C₃-C₆-cycloalkyl-C₁-C₂-alkyl, where C₁-C₆alkyl, is unsubstituted or has 1 substitute R^xa, where R^xa has one of the values given for R^1a; R⁵ is a halogen or C₁-C₂-alkyl, where m equals 0 or 1; n equals 0. The invention also relates to specific compounds and a pharmaceutical composition based on the compound of formula (I).

EFFECT: obtaining novel carboxamide compounds which are useful as calpain inhibitors (calcium-dependent cysteine proteases).

27 cl, 4 tbl, 34 ex