DERIVATIVES OF HYDROXYMETHYLFURAZAN CARBOXYLIC ACID AND PHARMACEUTICAL PREPARATION Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of hydroxymethyl-furazan carboxylic acid of the general formula (I) where one of radicals R¹ and R² means hydroxymethyl and another means -X being X means NR³R⁴ or OH or OR⁷; R³ and R⁴ mean independently each of other hydrogen atom, (C₁-C₂₀)-alkyl, 1-phenyl-(C₂-C₄)-alkyl, 2-phenyl-(C₃-C₄)-alkyl, (C₃-C₆)-alkenyl, (C₃-C₇)-cyclo-alkyl, or , -(CH₂)_n; or both R³ and R⁴ in common with binding nitrogen atom form heterocycle that can be once or multiple substituted with (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, (C₁-C₄)- -alkoxy-group, amino-group, (C₁-C₄)-alkylamino-group, di-((C₁-C₄)-alkyl)-amino-group, hydroxyl group, benzyl, phenethyl or phenyl; R⁵ and R⁶ independently each of other mean hydrogen atom, (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, benzyl, phenethyl or phenyl; R⁷ means (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, benzyl, phenyl that can be once or multiple substituted with -alkyl; ALK means (C₁-C₆)-alkyl; Ar means phenyl that can be once or multiple substituted with (C₁-C₄)-alkyl, (C₁-C₄)-alkoxy-group, sulfamoyl; Het is a heterocyclic radical with 1-3 nitrogen atoms that can be aromatic, partially unsaturated or saturated and can be once or multiple substituted with (C₁-C₄)-alkyl also; n = 0, 1, 2, 3 or 4; m = 1, 2, 3 or 4; p = 1, 2 or 3 and their pharmaceutically acceptable salts also. New compounds of the formula (I) show valuable pharmacological properties associated with nitrogen oxide formation and its effect for treatment and prophylaxis of cardiovascular system disease. Invention describes a pharmaceutical preparation based on the above indicated compounds showing dilating effect on ocular muscles. EFFECT: improved method of synthesis, valuable pharmacological properties of compounds. 10 cl, 40 ex