ANTAGONISTS OF SPECIFIC EXCITATORY AMINO ACID NEUROTRANSMITTER RECEPTORS

摘要

Abstract of the DisclosureInventors: Waclaw Janusz Rzeszotarski, Robert Lee Hudkins,Maria Elizabeth GuzewskaInvention: Antagonists of Specific Excitatory Amino AcidNeurotransmitter ReceptorsThe invention pertains to novel, potentanticonvulsants, analgesics and cognition enhancers achievingtheir action through the antagonism of specific excitatoryamino acid neurotransmitter receptors. In particular, theinvention is directed to .omega.-[2-phosphonoalkylenyl)phenyl]-2-aminoalkanoic acids having general formula:Wherein R1 and R2 are the same or different and areselected from the group consisting of hydrogen, lower alkyl,halogen, -CH=CH-CH=CH=, amino, nitro, trifluoromethyl orcyano; n and m = 0, 1, 2 or 3; and the pharmaceuticallyacceptable salts and derivatives thereof.Examples of specific preferred compounds of generalformula are selected from the group consisting of: 4-[2-phosphonomethylphenyl]-2-aminobutanoic acid, ethyl 3-[2-(2(2-diethylphosphonoethyl)phenyl]-2-acetamido-2-carboethoxypropanoate, 3-[2-phosphonomethyl)phenyl]-2-aminopropanoic acid, ethyl 3-[2-(3-bromopropyl)phenyl]-2-acetamido-3-carboethoxypropanoate, ethyl 3-[2-(3-diethylphosphonopropyl)phenyl]-2-acetamido-2-carboethoxypropanoate, ethyl 3-[2-(3-phosphonopropyl)phenyl]-2-aminopropanoic acid, ethyl 5-[2-(diethylphosphonomethyl)-phenyl]-2- acetamido-2-carboethoxypentanoate, and 5-[2-phosphonomethylphenyl]-2-aminopentanoic acid.