ANTAGONISTS OF SPECIFIC EXCITATORY AMINO ACID NEUROTRANSMITTER RECEPTORS

摘要

Inventors: Waclaw Janusz Rzeszotarski, Robert Lee Hudkins, Maria Elizabeth Guzewska Invention: Antagonists of Specific Excitatory Amino Acid Neurotransmitter Receptors The invention pertains to novel, potent anticonvulsants, analgesics and cognition enhancers achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to .omega.-¢2-phosphonoalkylenyl)phenyl!-2-aminoalkanoic acids having general formula: <IMG> Wherein R1 and R2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, halogen, -CH=CH-CH=CH=, amino, nitro, trifluoromethyl or cyano; n and m = 0, 1, 2 or 3; and the pharmaceutically acceptable salts and derivatives thereof. Examples of specific preferred compounds of general formula 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.