摘要 |
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.
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申请人 |
F. HOFFMANN-LA ROCHE AG |
发明人 |
BREU, VOLKER;BURRI, KASPAR;CASSAL, JEAN-MARIE;CLOZEL, MARTINE;HIRTH, GEORGES;LOFFLER, BERND-MICHAEL;MULLER, MARCEL;NEIDHART, WERNER;RAMUZ, HENRI |