| abstract |
FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to new compounds of the formula (I) and their pharmaceutically acceptable salts and esters eliciting inhibitory activity with regard to endothelin receptors. Compounds can be used for treatment of diseases associated with anomalous vascular tone and endothelial dysfunction. In compounds of the formula (I) R 1 means pyridyl, thiazolyl optionally substituted with halogen atom, lower alkyl, hydroxy-lower alkyl or lower alkenyl; R 2 means R 21 , -Y-R 22 or aromatic monovalent 5-membered carbocyclic radical comprising at least one heteroatom taken among nitrogen and oxygen atom and this carbocyclic radical can be optionally substituted with lower alkyl; R 21 means cyano-group, hydroxy-lower alkyl, carboxy-group, , amidino-, hydroxyamidino-group, lower alkoxycarbonyl or hydroxy-lower alkoxycarbonyl; R 22 means hydrogen atom, lower alkanoyl, carboxy-lower alkyl, lower alkoxycarbonyl, lower alkoxycarbonyl-lower alkyl, carbamoyl-lower alkyl, di-lower alkyl-carbamoyl-lower alkyl, allyl, lower alkyl or hydroxy-lower alkyl; R a means hydrogen atom or lower alkyl optionally substituted with hydroxy-group; R b means hydrogen atom or lower alkyl; R c means hydrogen atom, acetyl or lower alkylsulfonyl; X means -CH- or -N-; Y means -O-, -NH-. Invention relates also to pharmaceutical composition eliciting inhibitory capacity with regard to endothelin receptor and comprising compound of the formula (I) and pharmaceutically acceptable carrier and/or adjuvant. EFFECT: valuable medicinal properties of compounds. 13 cl, 5 tbl, 90 ex |