ARYL-S(O)N-SUBSTITUTED CARBOXYLIC-HYDROXAMIC ACIDS AND METHOD OF THEIR SYNTHESIS Russian patent published in 2001 - IPC

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to novel aryl-S(O)n-substituted carboxylic/hydroxamic acids of the formula (I) where Y means hydroxy-group, XONH- where X means H, C₁-C₆-alkyl; R¹ means H, C₁-C₆-alkyl; R² means H, C₁-C₆-alkyl, C₃-C₈-cycloalkyl; C₃-C₈-cycloalkyl-C₂-C₈-alkyl, tetrahydropyranyl, piperidinyl, -NR⁶R⁷ where R⁶ means H, C₁-C₆-alkyl, aryl; R⁷ means H, C₁-C₆-alkyl, aryl, aryl-C₁-C₈-alkyl, -SO₂NR⁸R⁹, arylhydroxycarbonyl, C₁-C₈-alkoxycarbonyl, -C(O)-O-CH₂R^d where R^d means phenyl; or group NR⁶R⁷ means valineamido-group; R⁸ and R⁹ mean independently H, C₁-C₆-alkyl; or R¹ and R² in common with carbon atom to which they are bound form C₃-C₈-cycloalkyl or possibly piperidinyl or tetrahydropyranyl substituted with lower alkyl; R³ means H, C₁-C₆-alkyl, C₃-C₈-cycloalkyl, C₃-C₈-cycloalkyl-C₁-C₈-alkyl, aryl, aryl-C₁-C₈-alkyl, piperidinyl, tetrahydropyranyl; R⁴ means H, C₁-C_6/ -alkyl, C₃-C₈-cycloalkyl, C₃-C₈-cycloalkyl-C₁-C₈-alkyl; R² and R³ in common mean C₃-C₈-cycloalkyl; R³ and R⁴ in common mean C₃-C₈-cycloalkyl; R⁵ means possibly substituted aryl. Compounds of the formula (I) inhibit activity of matrix proteases that ensures to use their in pharmaceutical composition in effective doses. EFFECT: improved synthesis. 28 cl, 2 tbl, 48 ex