ARYLETHENOSULFONEAMIDE DERIVATIVES AND PHARMACEUTICAL COMPOSITION Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of arylethenosulfone-amide of the formula (I) or its pharmaceutically acceptable salts that show high affinity to endothelin and can be used in medicine. In compound of the general formula (I) Ar means phenyl that can be substituted with 1-3 substituents taken among the group: halogen atom, lower alkyl possibly substituted with 1-3 substituents taken among halogen atom; lower alkoxyl, lower alkoxycarbonyl, carboxy-group, cyano-group; naphthyl, 5-6-membered heteroaryl taken among the group: thienyl, furyl, thiazolyl, pyridyl, pyrimidyl; X is oxygen, sulfur atom or group -NH-; Y is oxygen atom; R₁ is lower alkyl that can be substituted with halogen atoms, cyclo-alkyl, phenyl that can be substututed with 1-3 substituents taken among lower alkyl possibly substituted with 1-3 halogen atoms, lower alkoxyl, nitro-group, C₁-C₃-alkylenedioxy-group, 5-6-membered heterocycle taken among the group including pyridyl, pyrimidyl, thiazolyl, furyl, thienyl being each of that can be substituted with lower alkyl possibly substituted with 1-3 halogen atoms, lower alkoxy; R₂ is lower alkyl, lower alkenyl being each of that can be substituted with 1-3 groups taken among the group including hydroxy-group, lower alkoxy-group, halogen atom, cycloalkyl; R₃ is phenyl that can be substituted with 1-4 substituents taken among the group including lower alkyl, lower alkoxy-group, lower alkoxy-carbonyl; R₄ and R₅ can be similar or distinct and mean hydrogen atom, lower alkyl, or their pharmaceutically acceptable salt. Invention relates to also the pharmaceutical composition showing properties of endothelia antagonist and including derivatives of arylethenosulfoneamide or its pharmaceutically acceptable salt by p. 1 and pharmaceutically acceptable carrier. EFFECT: new compounds indicated above, valuable medicinal properties. 3 cl, 9 tbl, 95 ex