AMIDE DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEASES, PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to compounds of the formula (I) where dotted lines mean optional double bonds and if n = 1, 2 or 3 and m = 3 or 4 than A means -CH₂-; R¹ means: a) -CH₂-R⁴ where R⁴ means mercapto-, acetylthio-, carboxy-, hydroxyaminocarbonyl-, N-hydroxyformyl- -amino-, alkoxycarbonyl-, morpholino-(C₁-C₄)-alkoxycarbonyl-, arylhydroxycarbonyl-, benzylhydroxyaminocarbonyl-group or a residue of the formula (i) where R⁶ means quinol-2-yl; b) -CH(R⁷)-R⁸ where R⁷ means alkyl-, hydroxy-, amino-, alkoxy- -carbonyl-, aminocarbonyl- or carboxy-group and R⁸ means carboxy-, hydroxyaminocarbonyl-, alkoxycarbonyl- or aralkoxycarbonyl-group; c) -NH--CH(R⁹)-R¹⁰ where R⁹ means hydrogen atom or alkyl-group and R¹⁰ means carboxy-, aralkoxycarbonyl- -group; R² means alkyl-, cycloalkyl-, cycloalkylalkyl- or aralkyl-group and R³ means hydrogen atom and if n = 2 or 3 and m = 3 or 4 then A means -N(R¹¹)- where R¹¹ means hydrogen atom or alkyl-group; R¹, R² and R³ have the above indicated values. Composition can be prepared as separate stereoisomers or their mixture or their pharmaceutically acceptable salts and can be used for inhibition of activity of matrix metalloprotease in mammals. EFFECT: enhanced effectiveness of compounds as inhibitors. 26 cl, 49 ex