NMDA antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

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Details

562443, 548496, 514419, C07C22940, A61K 31195

Patent

active

054848148

ABSTRACT:
The present invention is directed to a class of 4,6-disubstituted tryptophan derivatives, 4,6-disubstituted kynurenines, their use as NMDA antagonists and to pharmaceutical compositions containing these compounds.

REFERENCES:
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The Journal of Neuroscience, Sep. 1990, 10(9):2965-297: Cerebral Synthesis and Release of Kynurenic Acid: an Endogenous Antagonist of Excitatory Amino Acid Receptors.
Society For Neuroscience Abstracts, vol. 17, 1991; 315.3; Systemic Loading with Kynurenine and Probenecid Markedly increases Striatal Kynurenic Acid Levels as Measured by in Vivo Microialysis, Miller, et al.
Chemical Abstracts 112(7): 52836c; Uptake of kynurenine into rat brain slices, Speciale, et al. (1991).
Chemical Abstracts 76(25): 150339a: Enzymic studies of the biosynthesis of 5-hydroxy-L-kynurenine in the rat small intestine, Konishi. (1972).
Chemial Abstracts 75(3): 17141t; Pyrrole ring cleavaging enzyme of 5-hydroxytryptophan, Konishi , et al., (1971).
Chemical Abstracts 69(9):33829e; Formation of 5-hydroxy-L-kynurenine from L-kynurenine by hen liver microsomes; Kido, et al. (1968).
Chemical Abstracts 73(3)9673r; Influence of androgens on tryptophan metabolism in man, McGinty, et al. (1970).
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Chemical Abstracts 111 (24):219114j; Sunscreens and skin-lightening cosmetics containing kynurenines; Narutomi, et al. (1989).
Chemical Abstracts 92(5):36767u; The mechanism of Kynurenine hydrolysis catalyzed by kynureninase, Tanizawa, et al. (1980).
Chemical Abstracts 97(15): 125986k; Halogenoanthranyloylalanines as sweeteners; Tanabe (1982).
Chemical Abstracts 93(25):239866u; An intensely sweet analog of kynurenine; Kawashima, et al. (1980).
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Chemical Abstracts, 96:115515w (1982).
Kynurenine metabolites of tryptophan: Implications for neurologic diseases; Freese, et al. 40 Neurology 691-695; Apr. 1990.
10-Microbia Biochem, vol. 112, 1990, Abstract No. 135860g.

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