Substituted aminoalkane phosphonic acids

Abstract

Several substituted 2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-5-ylmethyl)- amino-alkylphosphonic acids are disclosed as excitatory amino acid antagonists. No specific biological data are reported and compounds are claimed to exhibit an especially strong affinity for the α-amino-3- hydroxy-5-methylisoxazole-4-propionic acid (AMPA) and/or kainate binding sites, and a less strong affinity for the glycine binding sites of the N-methyl-D-aspartic (NMDA) receptor. Over 100 compounds are specifically claimed, 77 are characterised and specific synthetic methods for 10 compounds are presented. The compounds can be used in the preparation of medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.

• AMPA
• excitatory amino acid
• glutamate
• glycine co-agonist site of the NMDA receptor
• neurodegenerative diseases
• phosphonic acid
• quinoxalinediones