| 摘要 |
The invention concerns substituted 3-amino-1-arylalkylbenzazepin-2-ones of general formula (I), in which Ar is aryl; X is -O- or -S(O)n- and n is 0, 1 or 2; X1 is C1-C2 alkylene or a single bond; R1 is hydrogen, lower alkyl, aryl(lower alkyl) or acyl; R2 is lower alkyl, hydroxy(lower alkyl), (lower alkoxy)(lower alkyl), aryl(lower alkoxy)(lower alkyl), aryl(lower alkyl) or (C3-C7 cycloalkyl)(lower alkyl); R3 is a carboxylic group, (lower alkoxy)carbonyl, (lower alkoxy)(lower alkoxy)carbonyl, aryl(lower alkoxy)carbonyl, aryloxycarbonyl, carbamoyl, carbamoyl which is (i) mono-substituted by hydroxy, (lower alkyl)sulphonyl, halo(lower alkyl)sulphonyl or arylsulphonyl, (ii) mono-substituted or independently disubstituted by lower alkyl, lower alkenyl, lower alkinyl or phenyl(lower alkyl) or (iii) disubstituted by lower alkylene or (lower alkylene)-Z1-(lower alkylene), Z1 being O, S or NH; 5-tetrazolyl; PO2H2; PO3H2 or SO3H2; the ring A or aromatic groups, independently of each other, are unsubstituted or singly or multiply substituted by substituents selected from the group comprising lower alkyl, aryl(lower alkyl), (lower alkoxy)(lower alkyl), lower alkoxy, (lower alkoxy)(lower alkoxy), aryl(lower alkoxy), C3-C7 cycloalkyl, (C3-C7 cycloalkyl)(lower alkyl), nitro, halogen, trifluoromethyl, amino or amino which is mono-substituted or independently disubstituted by lower alkyl, aryl(lower alkyl) or aryl or disubstituted by lower alkylene or (lower alkylene)-oxy-(lower alkylene); or a salt thereof. The invention also concerns methods of preparing these compounds, their use, and pharmaceutical preparations containing compounds of formula (I) or pharmaceutically usable salts thereof. |
