SUBSTITUTED DERIVATIVES OF BENZENESULFONYLUREA AND BENZENESULFONYLTHIOUREA, METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION COMPRISING THEREOF AND METHOD OF ITS PREPARING Russian patent published in 2003 - IPC

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to novel substituted derivatives of benzenesulfonylurea or benzenesulfonylthiourea of the formula (I) their pharmaceutically acceptable salts, to method of their synthesis, pharmaceutical composition comprising thereof and method of its preparing. The proposed substituted derivatives of benzenesulfonylurea or benzene- -sulfonylthiourea exhibit antiarrhythmic activity similar to that of GLIBENCLAMIDE but they elicit the less effect on blood glucose content in their using in effective doses. In compounds of the formula (I) R₁ means hydrogen atom, C_1-7-alkyl, C_3-7-cycloalkyl; R₂ means hydrogen atom, C_1-6-alkoxyl; among R₃,R₄ each means independently hydrogen atom, C_1-12-alkyl, C_3-10-cycloalkyl; E means oxygen or sulfur atom; X means oxygen atom; Y means C(R₅,R_5′)_m where R₅,R_5′ mean hydrogen atom; m = 1, 2, 3. Invention proposes method of synthesis of compounds of the formula (I) where E means sulfur atom that are synthesized by interaction of benzenesulfonylthiourea of the formula (II) or its salt of the formula (III) with thioisocyanate of the formula (IV) R(1)-N=C=S (IV) where, R₁,R₂,R₃,R₄ X and Y have the above indicated values and M means cation of alkaline or alkaline-earth metal. Pharmaceutical composition comprises effective amount of compound of the formula (I) as active component or its pharmaceutically acceptable salts and pharmaceutically acceptable additions. Composition is prepared by mixing effective amount of compound of the formula (I) or its pharmaceutically acceptable salt in common with at least one carrier or accessory substance up to useful dosing form. EFFECT: improved method of synthesis and preparing. 9 cl, 58 ex