| abstract |
Compounds of the formula, (see formula I) wherein R1 signifies heterocyclyl; R2 signifies hydrogen, lower-alkyl, lower-alkoxy, lower-alkylthio, lower-alkoxy-lower-alkyl, lower-alkylsulphonyl-lower-alkoxy, phenyl, lower alkylphenyl, lower-alkoxy-phenyl, lower-alkylene-dioxyphenyl, phenyl-lower alkyl, lower alkyl-phenyl-lower alkyl, lower alkoxy-phenyl-lower alkyl, lower alkylenedioxyphenyl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; R3 signifies lower-alkyl, lower-alkoxy, formyl, halo-lower-alkyl, hydroxy-lower-alkyl, amino-lower-alkyl or a residue -CH2O-A-lower-alkyl, -(CH2)m-O-(CR a R b)n OH, -(CH2)m-O-(CR a R b)n OR9, -(CH2)m-O-(CR a R b)n NH2 or -(CH2)m-O-(CR a R b)n-B-R9; R4-R8 signify hydrogen, lower-alkoxy or halogen; R9 signifies heterocyclyl; phenyl or phenyl substituted by lower-alkyl, lower-alkoxy and/or halogen, or lower-alkyl; R a and R b signify hydrogen or lower-alkyl; A signifies a ketalized 1,2-dihydroxy-ethylene group; B signifies -OC(O)O-, -O(C(O)NH-, -NH(C(O)NH- or -NHC(O)O-: n signifies 2, 3 or 4; and m signifies 0 or 1 are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris. |