FIELD: biochemistry. SUBSTANCE: invention provides compounds with general formula 
(I), in which R1 is phenyl, (C1-C4)-alkylphenyl, (C1-C4)-alkoxyphenyl, halogenphenyl; R2 is (C1-C4)-alkyl; R3 is phenyl, biphenyl, naphthyl, thienyl, furyl, tetrazolyl, imidazolyl, pyridyl, quinolinyl, pyridylphenyl, thienylphenyl, furylphenyl, imidazolylphenyl, or isoxazolylphenyl; where above-mentioned aryl or heteroaryl radicals are independent of each other and are unsubstituted or substituted by substituents selected from the group including: (C1-C4)-alkyl, (C1-C4)-alkoxy, phenyl-(C1-C4)- alkoxy, halogen, trifluoroalkyl, hydroxyl, cyano, cyano-(C2-C5)-alkanoyl, and nitro group; 
is hydrogen or phenyl optionally substituted by (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, trifluoroalkyl, hydroxyl, or nitro group; 
is hydrogen; C(=X) is C(=O) or C(=S); Y is NH or methylene; or C(=X) is CHOH and Y is methylene; R4 is -(CH2)5-Ar with s=1 and Ar phenyl, naphthyl, biphenyl, indol-3-yl, 1-(C1-C4)-alkylindol-3-yl, or quinolinyl; where above-mentioned aryl or heteroaryl radicals are independent of each other and are unsubstituted or substituted by substituent selected from the group including: (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, trifluoroalkyl, hydroxyl, and nitro group; R5 is carboxyl. Pharmaceutically acceptable salts of compounds I are also claimed. Effective amount of compound I is used as antagonist in drug inhibiting binding of endothelin. EFFECT: extended choice of endothelin receptor antagonists. 16 cl, 123 ex
