NOVEL BENZAMIDOALDEHYDES Russian patent published in 2002 - IPC

FIELD: organic chemistry, biochemistry. SUBSTANCE: invention relates to novel derivatives of benzamidoaldehydes of the formula (I) where R¹ means phenyl, naphthalene, quinoline, isoquinoline, tetrahydroquinoline, tetrahydroisoquinoline, pyridine, quinazoline, quinoxaline being aromatic and heteroaromatic rings can be substituted with radicals R⁴; R² means hydrogen atom, chlorine, bromine, fluorine atom, alkyl, - NHCO-naphthyl, -NHSO₂- C_1-4-alkyl, -O-C_1-4-alkyl, -CO-NH-C_1-4-alkyl, NO₂; R³ means hydrocarbon residue with 1- 6 carbon atoms that can carry cycloalkyl, indolyl, phenyl ring or a residue of the group -SCH₃-; R⁴ means alkyl, -O-C_1-4-alkyl, chlorine, fluorine, bromine, iodine atom, CF₃, pyridine; X is a bond, , -CH=CH-, -C≡C-, -CO-CH=CH-, -CH=CH-CO-, -(CH₂)_m-CO-(CH₂)₀-,-(CH₂)_m-NR⁵CO-(CH₂)₀- (R⁵ is H, C_1-4-alkyl), , -NH-CO-CH=CH-, -CH= CH-CO- NH- or unsubstituted phenyl or phenyl substituted with radical R²; n is a number 1 or 2; m is a number from 0 to 4 and o is a number from 0 to 4. Novel benzamidoaldehydes show an inhibitory activity and therefore they can be used as inhibitors of cysteine proteases. EFFECT: new compounds indicated above, valuable biochemical properties.