| abstract |
(57) [Summary]nThe present invention provides a compound of formula (I):nEmbedded imagen Wherein the substituents have the following meaning: R 1 = Tetrazole or group (1):nEmbedded imagen Then, in the formula, R = group OR 7 , (2):nEmbedded imagen , (3):nEmbedded imagen A 5-membered heteroaromatic linked by a nitrogen atom, such as pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R Two , R Three = Hydrogen, hydroxy, NH Two , NH (C 1 ~ C Four -Alkyl), N (C 1 ~ C Four -Alkyl) Two , Halogen, C 1 ~ C Four -Alkyl, C Two ~ C Four -Alkenyl, C Two ~ C Four -Alkynyl, C 1 ~ C Four -Hydroxyalkyl, C 1 ~ C Four -Alkoxy, C 1 ~ C Four -Halogenalkyl, C 1 ~ C Four -Alkoxy, C 1 ~ C Four -Halogenalkoxy or C 1 ~ C Four -Alkylthio; X = halogen, C 1 ~ C Four -Halogenalkyl, hydroxy; R Four And R Five = Phenyl or naphthyl, C Three ~ C 7 -Cycloalkyl, direct bond, methylene, ethylene or ethenylene group, oxygen or sulfur atom or SO Two Phenyl or naphthyl linked at the ortho position by an -NH or N-alkyl group or a 5- or 6-membered heteroaromatic; 6 = Hydrogen, phenyl or naphthyl, 5- or 6-membered heteroaromatic, C 1 ~ C 8 -Alkyl, C Three ~ C 6 -Alkenyl, C Three ~ C 6 Alkynyl or C Three ~ C 8 -Cycloalkyl, wherein these groups may be mono- or polysubstituted, provided that when Z is not a single bond, R 6 May represent only hydrogen; Z = sulfur, oxygen or single bond], as well as physiologically acceptable salts and enantiomerically pure or diastereomerically pure forms. The novel compounds are suitable for disease control, especially as endothelin antagonists. |