A compound of the formula described suitable for use as prophylactic and therapeutic treatment of pathological conditions which respond to blockage of excitatory amino acid receptors. The compound has a high binding affinity towards amino acid receptors, such as AMPA receptor, NMDA (kainite) receptors and/or glycine binding sites of NMDA receptors. The compound is useful for treating diseases such as neurodegenerative disorders as a result of stroke, hypoglycemia, anoxia or cerebral palsy symptoms, of ischemic brain disorders, such as cerebral ischemia, cerebral ischemia in heart surgery or cardiac arrest, perinatal asphyxia, epileptic attacks, Huntington's chorea, Alzheimer's and Parkinson's disease, amyotropic lateral sclerosis, bone marrow and cerebral trauma and symptoms of poisoning by neurotoxins or addictive drug abuse, and of ischemic disorders of the eye, of vascular and muscle spasms, such as of migraine or of local or general spasticity, of convulsions, such as epilepsy, and of states of anxiety and pain, such as of trigeminal neuralgias. Wherein R1 is hydroxyl or an aliphatic, araliphatic or aromatic radical; X is a divalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical; R2 is hydrogen or an aliphatic or araliphatic radical; alk is lower alkylidene; and R3, R4 and R5 independently of one another are hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, with the proviso that a1) R4 is other than nitro when X is methylene, 3-hydroxybenzylidene, 3-methoxybenzylidene, 3-pyridylmethylene, ethylene, oxoethylene, ethylidene, 1,3-propylene, 1,3-(1-carboxy)propylene, cyclopropylene or 1,4-butylene, R1 is hydroxyl, alk is methylene and R2, R3 and R5 are hydrogen, or when X is methylene, R1 is methyl or benzyl, alk is methylene and R2, R3 and R5 are hydrogen, or when X is butylene, R1 is hydroxyl, alk is methylene, R2 is methyl and R3 and R5 are hydrogen and b1) R4 is other than bromine when X is methylene or ethylidene, R1 is hydroxyl, alk is methylene and R2, R3 and R5 are hydrogen.
Substituted aminoalkane phosphonic acids for treating block excitatory amino acid receptors related diseases