| abstract |
Compounds of the formula I <IMAGE> (I) wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R1, R2 and R3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R1, R2 and R3 is hydrogen or, in the case of R1 and R2, is hydroxy, and the remaining one of R1, R2 and R3 is hydrogen, or wherein R denotes methyl, R1 denotes hydrogen or hydroxy, R2 denotes an aromatic radical and R3 represents hydrogen, and their salts have GABAB-antagonistic properties and can be used as GABAB-antagonists. They are obtained when in a compound of formula II <IMAGE> (II) in which R, R1, R2 and R3 have their previous significances, Z represents -NH2 and R4 denotes a hydroxy-protective group R5 or, when R1 and R3 denote hydrogen and R2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R6, or Z represents a protected or latent amino group Zo and R4 denotes hydrogen or a hydroxy-protective group R5, any group R5 or R6 is replaced by hydrogen, and/or any group Zo is converted into -NH2. |