DERIVATIVES OF IMIDAZOLE, METHODS OF THEIR SYNTHESIS, INTERMEDIATE COMPOUNDS AND PHARMACEUTICAL COMPOSITION BASED ON IMIDAZOLE DERIVATIVES Russian patent published in 2002 - IPC

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes novel derivatives of imidazole of the general formula (I) where R₁ means linear or branched alkyl- or alkylthio-radical comprising 12 carbon atoms, not above, possible substituted with 1-2 similar or different radicals taken among hydroxyl, alkyl, alkoxy- or alkylthio-group where alkyl moiety has 6 carbon atoms, not above, phenyl substituted with C₁-C₄-alkoxy- -group; or radical dioxolan or dioxane; R₂ and R₃ can be similar or different and they are taken among halogen atoms, radicals mercaptogroup, acyl-group, carboxy-group that can be free or converted to salt or esterified form, formyl, alkyl substituted with phenyl or cycloalkyl; or it means radical where m1 is a whole number from 0 to 4; m2 is a whole number from 0 to 1; R₁₀ means linear or branched radical alkyl comprising 6 carbon atoms, not above, or phenyl possibly substituted with 1-2 similar or different substitutes taken among hydroxyl, C₁-C₆- alkyl, C₁-C₆-alkoxyl, carboxyl that can be free or converted to salt or esterified form, carboxyethyl, alkyl substituted with phenyl and substituted in turn with C₁-C₆-alkoxyl; radical cycloalkyl comprising 3-7 carbon atoms or benzodioxol; Y means phenyl substituted with two radicals that forms dioxolane ring in common with two adjacent carbon atoms to which they are bound and that can be substituted with 1-2 similar or different substitutes taken among halogen atom, carboxycarbonyl that can be free or converted to salt or esterified form. Novel derivatives of imidazole can be used for preparing pharmaceutical compositions designated for treatment of diseases caused by anomal stimulation or endothelin receptors and, in part, for treatment of hypertension induced by endothelin, vessel spasm, for treatment of states after cerebral hemorrhage, renal insufficiency, myocardium infarction and in prophylaxis of repeated stenosis after angioplasty. Invention describes methods of their synthesis, intermediate compounds and a pharmaceutical composition based on compounds of the formula (I). EFFECT: new compounds indicated above, improved method of synthesis, valuable medicinal properties. 11 cl, 19 tbl