SUBSTITUTED BENZENESULFONYLUREAS AND BENZENE-SULFONYLTHIOUREAS, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION CONTAINING THEREOF AND METHOD OF ITS PREPARING Russian patent published in 2003 - IPC

Abstract RU 2198163 C2

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to novel substituted derivatives of benzenesulfonylurea or benzene-sulfonylthiourea of the formula (I) and to their pharmaceutically acceptable salts also exhibiting antiarrhythmic activity and activity for prevention of sudden death caused by arrhythmia in heart stop, method of their synthesis, pharmaceutical composition containing thereof and method of its preparing. In compounds of the formula (I) R1 means methyl; R2 means C4-10-alkoxyl-group where from one to 6 carbon atoms are substituted for oxygen atom; E means oxygen or sulfur atom; X means hydrogen, halogen atom, C1-6-alkyl; or Y means [C(R3)2]1-4 where R3 means hydrogen atom; Z means C1-4-alkoxyl-group. Invention proposes method of synthesis of compound of the formula (I) where E means sulfur atom that involves interaction of sulfonamide of the formula (II) or its salt of the formula (III) with thiocyanate of the formula (IV) where R1, R2, R3, Z, X and Y have said values and M means cation of alkaline or alkaline-earth metal, ammonium or tetraalkylammonium. Synthesized compound of the formula (I) where E means sulfur atom can be converted in the presence of oxidizing agent to compound of the formula (I) where E means oxygen atom. Pharmaceutical composition comprises effective amount of compound of the formula (I) or its pharmaceutically acceptable salt as active component and pharmaceutically acceptable additions. Composition is prepared by mixing effective amount of compound of the formula (I) or its pharmaceutically acceptable salt with at least one carrier or accessory substance up to useful dosing form preparing. EFFECT: improved method of synthesis and preparing. 12 cl, 4 ex

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RU 2 198 163 C2

Authors

Ehnglert Khajnrikh

Gerlakh Uve

Mania Diter

Gёgelajn Khajnts

Kajzer Joakhim

Dates

2003-02-10Published

1996-02-16Filed