CIS-2,4,5-TRIARYLIMIDAZOLINES Russian patent published in 2008 - IPC C07D233/22 C07D233/36 C07D401/06 C07D401/12 C07D401/14 C07D403/06 C07D403/12 C07D405/12 C07D409/12 C07D413/12 C07D417/12 C07D491/10 A61K31/4164 A61K31/4178 A61P35/00 

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula: wherein X₁ and X₂ represent halogen atom; X₃ represents lower alkoxy group; R is chosen from group consisting of the following substances: and wherein R₁ is chosen from group consisting of N-lower alkyl, unsubstituted heterocycle and heterocycle substituted with one or some substitutes chosen from group consisting of -NH₂, -NH-C(O)-lower alkyl, -C(O)-lower alkyl, -C(O)-lower alkoxy group, oxo group, heterocycle and lower alkyl substituted with hydroxy group; R₂ is chosen from hydrogen atom, methyl and lower alkoxy group; R₃ is chosen from group consisting of heteroaryl, heterocycle, lower alkyl substituted with R₇, aryl, lower alkoxy group and lower alkyl; R₄ is chosen from group consisting of -C(O)-lower alkoxy group, lower alkoxy group, CH₂-heterocycle, CH₂-heterocycle substituted with oxo group, aryl, -NH-C(S)-N-lower alkyl, -NH-C(S)-N-aryl, -NH-C(O)-R₈, N-alkyl substituted with -C(O)-R₁₆ and trifluoromethyl; R₅ is chosen from group consisting of oxo group, heteroaryl, aryl substituted with a substitute chosen from lower alkoxy group and fluorine atom, -C(S)-N-lower alkyl, -C(S)-N-aryl, -C(O)-R₁₃, -SO₂-R₁₄ and lower alkyl substituted with a substitute chosen from R₁₅ and -C(O)-R₁₆; R₆ is chosen from group consisting of lower alkyl substituted with N-lower alkyl, lower alkyl substituted with heterocycle, lower alkyl substituted with heterocycle substituted with one or two substitutes chosen from lower alkyl, lower alkyl substituted with hydroxyl and oxo group; R₇ is chosen from group consisting of cyano, hydroxy group, heteroaryl, heterocycle substituted with oxo group and aryl substituted with a substitute chosen from group consisting of -SO₂NH, lower alkoxy and hydroxy group; R is chosen from group consisting of N-lower alkyl, heterocycle, heterocycle substituted with a substitute chosen from group consisting of oxo group, -C(O)-NH₂ and -C(O)-NH-lower alkyl, CH₂-R₉ and CH₂-R₁₀; R₉ is chosen group consisting of -NH₂, N-lower alkyl, N-lower alkyl substituted with a substitute chosen from hydroxy and lower alkoxy group; R₁₀ is chosen from heterocycle and heterocycle substituted with one or some groups chosen from group consisting of -C(O)-NH₂, lower alkyl substituted with hydroxy group, hydroxy group; R₁₃ is chosen from group consisting of heteroaryl, heteroaryl substituted with one or some substitutes chosen from group consisting of lower alkyl, aryl and halogen atom, heterocycle, heterocycle substituted with one or some substitutes chosen from group consisting of lower alkyl, aryl and halogen atom, -C(O)-lower alkyl, -C(O)-NH₂, -C(O)-N-lower alkyl and lower alkyl substituted with -O-C(O)-CH₂; R₁₄ is chosen from group consisting of trifluoromethyl, lower alkyl, aryl substituted with lower alkyl, -NH₂, N-lower alkyl, N-lower alkyl substituted with a substitute chosen from lower alkoxy, cyano, amino group and trifluoromethyl, heteroaryl, heteroaryl substituted with a substitute chosen from group consisting of amino group, halogen atom, -C(O)-lower alkoxy group, lower alkyl and lower alkyl substituted with hydroxyl, heterocycle and heterocycle substituted with a substitute chosen from group consisting of hydroxy, oxo group; R₁₅ is chosen from group consisting of lower alkoxy, cyano group, trifluoromethyl, N-lower alkyl, -SO₂-lower alkyl, -C(O)-lower alkyl, heteroaryl and heterocycle; R₁₆ is chosen from group consisting of lower alkoxy group, -NH₂, N-lower alkyl, N-lower alkoxy group, N-lower alkenyl, N-benzyloxy group, N-lower alkyl, substituted R₁₈, heterocycle and heterocycle substituted with one or two substitutes chosen from group consisting of hydroxy, alkoxy group, trifluoromethyl, -C(O)-lower alkyl, -C(O)-NH₂, -C(O)-N-lower alkyl, lower alkyl substituted with hydroxy and oxo group; R₁₈ is chosen from group consisting of lower alkoxy, cyano group, trifluoromethyl, heterocycle and hydroxyl. Also, invention relates to a pharmaceutical composition possessing anti-proliferative activity based on these compounds. Invention provides synthesis of novel compounds possessing valuable biological properties.

EFFECT: valuable properties of compounds and pharmaceutical composition.

28 cl, 243 ex