Omega-[2-(alkyl)phenyl]-2-aminoalkanoic acids as antagonists of

Details Omega-[2-(alkyl)phenyl]-2-aminoalkanoic acids as antagonists of Omega-[2-(alkyl)phenyl]-2-aminoalkanoic acids as antagonists of

1992-12-02

1994-11-15

Springer, David B.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514538, 514562, 514567, 548253, 560 12, 560 38, 562433, 562 41, C07D25704, A61K 3110, A61K 31195, A61K 31215

Patent

active

053648765

ABSTRACT:
The present invention pertains to antagonists of excitatory amino acid receptors, their method of preparation as well as compositions pertaining to them, which have the general formula: ##STR1## wherein m and n are independently 0,1,2, or 3: R1 and R2 are selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C1 to C6 lower alkyl, C7 to C12 higher alkyl, aryl and aralkyl; Z is a monoacidic radical; R3 is selected from the group consisting of hydrogen, and C1 to C6 lower alkyl; the stereoisomers thereof in their resolved or racemic form, and pharmaceutically acceptable salts thereof. In a preferred embodiment m is 2 or 3 and n is 1.

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patent: 4918064 (1990-04-01), Cordi et al.
patent: 5049555 (1991-09-01), Rzeszotarski et al.
Watkins et al., "Excitatory Amino Acid Transmitters," Amer. Rev. Pharmacol. Toxicol. (1981), vol. 21 pp. 165-204.
Schwarcz et al., "Quinolinic Acid: An Endogenous Metabolite that Produces Axon-Sparing Lesions in Rat Brain," Science, Jan. 1983, vol. 219, pp. 316-318.
Simon et al., "Blockade of N-Methyl-D-Aspartate Receptors May Protect Against Ischemic Damage in the Brain," Science, vol. 226, pp. 850-852, (1984).

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