| abstract |
FIELD: biochemistry. SUBSTANCE: invention provides compounds with general formula (I), in which R 1 is phenyl, (C 1 -C 4 )-alkylphenyl, (C 1 -C 4 )-alkoxyphenyl, halogenphenyl; R 2 is (C 1 -C 4 )-alkyl; R 3 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: (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy, phenyl-(C 1 -C 4 )- alkoxy, halogen, trifluoroalkyl, hydroxyl, cyano, cyano-(C 2 -C 5 )-alkanoyl, and nitro group; is hydrogen or phenyl optionally substituted by (C 1 -C 4 )-alkyl, (C 1 -C 4 )-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; R 4 is -(CH 2 ) 5 -Ar with s=1 and Ar phenyl, naphthyl, biphenyl, indol-3-yl, 1-(C 1 -C 4 )-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: (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy, halogen, trifluoroalkyl, hydroxyl, and nitro group; R 5 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 |