Quinazoline-4-one AMPA antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514259, 544278, 544284, 544287, 544290, A61K 31505, C07D23972, C07D49502, C07D40104, C07D40300

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active

060604794

ABSTRACT:
The present invention relates to novel quinazolin-4-one derivatives of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

REFERENCES:
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Watkins, Jeff C., et al., Structure-activity relationships in the development of excitatory amino acid receptor agonists and competitive antagonists, TIPS-(vol. 11) pp. 25-33 Jan. 1990.
Schoepp, Darryle, et al., Pharmacological and functional characteristics of metabotropic excitatory amino acid receptors, TIPS-(vol. 11) pp. 508-515 Dec. 1990.
McDonald, John W. and Johnston, Micheal V., Physiological and pathophysiological roles of excitatory amino acids during central nervous system development, Brain Res. Reviews 15, pp. 41-70 (1990).
Sheardown, Malcom J., et al., 2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F) quinoxaline: A Neuroprotectant for Cerebral Ischemia, Science Reports, vol. 247, pp. 571-574 Feb. 2, 1990.
Buchan, Alastair M., et al., Delayed AMPA receptor blockade reduces cerebral infarction induced by focal ischemia, NeuroReport 2, No. 8, pp. 473-476 (1991).
Le Peillet, Elaine, et al., The non-NMDA antagonists, NBQX and GYKI 52466, protect against cortical and striatal cell loss following transient global ischaemia in the rat, Brain Res. 571, pp. 115-120 (1992).
Parks T.N., et al., Modulation of N-methyl-D-aspartate receptor-mediated increases in cytosolic calcium in cultured rat cerebellar granule cells, Brain Res. 552, pp. 13-22 (1991).
Wolfe, James F., et al., Synthesis and Anticonvulsant Activity of Some New 2-Substituted 3-Aryl-4 (3H)-quinazolinones, J. Med. Chem, 33, pp. 161-166, (1990).
Wolfe, James F., et al., Synthesis and Anticonvulsant Activity of Some New 3, 6-Disubstituted-2-[2-oxo-2-(4-pyridyl)ethyl]-4(3H)-pyrimidinones, Journal of Pharmaceutical Sciences, vol. 80, No.7, pp. 705-706 Jul. 1991.
Beal, M. Flint, Aging, Energy, and Oxidative Stress in Neurodegenerative Diseases, Annals of Neurology, vol. 38, No. 3, pp. 357-366, Sep. 1995.

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