DERIVATIVES OF ARYL- AND HETEROARYLSULFONEAMIDES AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of aryl- and heteroarylsulfoneamides of the general formula (I) where R¹ means substituted phenyl or pyridyl; R² means substituted phenyl; R³ means hydrogen atom, (lower)-alkyl, cyano-, carboxy-, esterified carboxy-group, phenyl, 1H- -tetrazolyl or the group -CON-R⁵R⁶; R⁵ means hydrogen atom or radical R⁷; R⁶ means -(CH₂)_mR⁷ or R⁵ and R⁶ in common with nitrogen atom to which they are bound mean morpholino-, 2,6- -dimethylmorpholino-, piperidino-, 4-(lower)-alkylpiperazino-, 4-(lower)-alkoxypiperazino-, 4-(lower)-alkoxycarbonylpiperazino- or 4-formylpiperazino-group; R⁷ means phenyl, substituted phenyl, substituted phenyl, pyridyl, 1H-tetrazolyl, (lower)- -alkyl, cyano-(lower)-alkyl, hydroxy-(lower)-alkyl, di-(lower)- -alkylamino-(lower)-alkyl, carboxy-(lower)-alkyl, (lower)- -alkoxycarbonyl-(lower)-alkyl, (lower)-alkoxycarbonylamino- -(lower)-alkyl or phenyl-(lower)-alkoxycarbonyl; R^a means hydrogen atom or hydroxy-group; R^b means hydrogen atom; Z means hydroxy-group or the group -OR⁸ or -OC(O)N-R⁸ where R⁸ means pyridyl or pyrimidinyl; X means nitrogen atom or CH; m = 0, 1 or 2; n = 0, 1 or 2 and their pharmaceutically acceptable salts. Derivatives of aryl- and heteroarylsulfone-amides of the formula (I) show the selective inhibitory effect with respect to endothelin A and B receptors and can be used for synthesis of drugs. Invention describes the pharmaceutical composition based on compounds of the formula (I) also. EFFECT: new compounds indicated above, valuable pharmacological properties of compounds. 27 cl, 2 tbl, 146 ex