| abstract |
Compounds have the formula (I), in which R<1> is heterocyclyl; R<2> is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkoxy lower alkyl, lower alkylsulfonyl lower alkoxy, phenyl, lower alkoxyphenyl, lower alkylene dioxyphenyl or heterocyclyl; R<3> is lower alkyl, lower alkoxy, formyl, lower alkyl halide, lower hydroxyalkyl, lower aminoalkyl or a residue -CH2O-A-lower alkyl, -(CH2)m-O-(CR<a>R<b>)nOH, -(CH2)m-O-(CR<a>R<b>)nNH2 or -(CH2)m-O-(CR<a>R<b>)n-B-R<9>; R<4> to R<8> are hydrogen, lower alkoxy or halogen; R<9> is heterocyclyl, phenyl or lower alkyl-, lower alkoxy- and/or halogen-substituted phenyl, or lower alkyl; R<a> and R<b> are hydrogen or lower alkyl; A is a cetalised 1,2-dihydroxy-ethylene group; B is -OC(O)O-, -O(C(O)NH-, -NH(C(O)NH- or -NHC(O)O-, n equals 2, 3 or 4; and m equals 0 or 1. These compounds may be used to treat diseases associated to endothelin activity, in particular circulatory diseases such as hypertonicity, ischemia, vasospasms and angina pectoris. |