| 摘要 |
Compounds of the formula (see Figure I) in which R1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X1 is CO, SO2 or -O-C(=O)- with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula (I); X2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R2 is carboxyl which, if required, is esterified or amidated, substituted or unsubstituted amino, formyl which, if required, is acetalised, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if required, is etherified, S(O)m-R where m is 0, 1 or 2 and R is hydrogen or an aliphatic hydrocarbon radical, alkanoyl, unsubstituted or N-substituted sulfamoyl or POnH2 where n is 2 or 3; X3 is a divalent aliphatic hydrocarbon; R3 is carboxyl, 5-tetrazolyl, SO3H, PO2H2, PO3H2 or haloalkyl-sulfamoyl; and the rings A and B independently of one another are substituted or unsubstituted; in free form or in salt form with the proviso that when R1 is C1-C5 alkyl, X1 is CO, X2 is a group of formula (Ib) (see figure Ib) in which p and r are 0 and q is 1 and X4 is C1-C4 alkyl, X5 is hydrogen, R2 is carboxy or C2-C5 alkoxycarbonyl then R3 is other than 5-tetrazolyl attached at the 2' position. These compounds have pronounced angiotensin II antagonist properties.
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