| abstract |
FIELD: organic chemistry of heterocyclic compounds, pharmacy. SUBSTANCE: invention describes novel derivatives of benzothiazine dioxide of the general formula (1) where R 2 means the group of the formula (2) or alkyl with 1-7 carbon atoms where each of R a and R c means from 1 to 5 substituents and R b means from 1 to 4 substituents taken independently among the group including hydrogen, chlorine atom, methylenedi- -hydroxy-group, ethylenedihydroxy-group, groups OR and OCH 2 OR where R means hydrogen atom, alkyl with 1-6 carbon atoms or phenyl; R d means groups CO 2 R, SO 3 R, CONRR 1 where R has the above indicated value and R 1 has value given for radical R; n = 0-2; _ _ _ means ordinary or double bond; X means (CH 2 ) n or S(O) n , where n has the above indicated value or their pharmaceutically acceptable salts of acid or base addition. Invention relates to also pharmaceutical composition based on given compounds showing inhibitory activity of endothelin and method of inhibition of endothelin receptors. Proposed heterocyclic compounds can be used as active components in pharmaceutical compositions. EFFECT: broadened arsenal of heterocyclic compounds, valuable properties of compounds. 7 cl, 1 tbl, 56 ex |