| 摘要 |
21489-6938 4-15361/+/CGC 1135 Phosphono- and phosphonoalkyl-azacycloal(en)yl carboxylic acid compounds The present invention is concerned with the compounds of formula I, (I) wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be etherified, lower alkyl, benzyl, benzyl substituted on phenyl by halogen, lower alkyl or lower alkoxy; lower alkanoyloxymethyl or lower alkanoyloxymethyl substituted on oxymethyl by lower alkyl or cycloalkyl, m represents one or zero, R1 is carboxy, carbamoyl or lower alkoxycarbonyl, lower alkanoyloxymethoxycarbonyl, di-lower alkylamino straight chain C2-C4-alkoxycarbonyl or pyridylmethoxycarbonyl, wherein the five- or six-membered heterocyclic ring may be additionally substituted on carbon by lower alkyl and/or on nitrogen, by lower alkyl, lower alkanoyl, phenyl-lower alkanoyl or benzoyl, may have present a carboncarbon double bond or may be fused on adjacent carbon atoms with a six-membered carbocyclic ring. A represents a direct bond or lower alkylene provided that A does not represent a direct bond when the heterocyclic ring together with substituent R1 represents 2-carboxy-pyrrolidinyl; and salts thereof. These compounds are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor. |
