BENZOXAZOLE DERIVATIVES AS RACEMATES OR INDIVIDIAL ENANTIOMERS AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, AND PHARMACEUTICAL COMPOSITIONS HAVING LEUCOTRIENE BIOSYNTHESIS INHIBITORY ACTIVITY

摘要

FIELD: medicine. SUBSTANCE: claimed invention describes benzoxazole derivatives of general formula (I): wherein R₁ and R₂ are independent from each other and are hydrogen, alkyl having 1-6 carbon atoms, CX₃, in which X is halogen, cycloalkyl with 1-3 carbon atoms, halogen, nitrile, alkoxy with 1-6 carbon atoms, CO₂R₇, is which R₇ is hydrogen or alkyl with 1-6 carbon atoms, -C(O)NR₈R₉, in which R₈ and R₉ are hydrogen, alkyl with 1-3 carbon atoms or methoxy, nitro, NR₁₀R₁₁ in which R₁₀ and R₁₁ are hydrogen or alkyl with 1-3 carbon atoms. Sulfonyl substituted by methyl or phenyl, -C(O)R₁₂, in which R₁₂ is alkyl with 1-6 carbon atoms; R₃ is alkyl with 1-6 carbon atoms, cycloalkyl with 3-6 carbon atoms, phenyl unsubstituted or substituted by halogen or alkoxy with 1-3 carbon atoms or alkyl with 1-4 carbon atoms, NR₁₃N₁₄ in which R₁₃ and R₁₄ are alkyl with 1-3 carbon atoms, 5- or 6-membered heteroaromatic ring containing 1-3 heteroatoms form the group consisting of nitrogen, oxygen and sulfur: R₄ is alkyl with 1-6 carbon atoms, cycloalkyl with 3-6 carbon atoms or phenyl unsubstituted or substituted by halogen, alkoxy with 1-3 carbon atoms or alkyl with 1-4 carbon atoms; R₅ is hydrogen or alkyl with 1-4 carbon atom; R₆ is hydrogen or alkyl with 1-3 carbon atoms, as racemates or as individual enantiomers and pharmaceutically acceptable salts thereof. The claimed invention also describes pharmaceutical composition having leucotriene biosynthesis inhibitory activity, said composition comprises, as active ingredient, benzoxazole derivatives of general formula (I) as racemate or individual isomer or pharmaceutically acceptable salt in effective amount. EFFECT: improved properties of the pharmaceutical composition.