Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-04-07
1997-10-14
Mullis, Jeffrey C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544353, 544356, 544355, C07D24136, C07D24138, A01N 4360
Patent
active
056773056
ABSTRACT:
An oxopyridinylquinoxaline derivative represented by the following Formula I or pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1 is hydrogen, halogen, nitro, or trihalomethyl; R.sup.2 is hydrogen, halogen, nitro, cyano, trihalomethyl, carbamoyl, carbamoyl substituted with lower alkyl, sulfamoyl, or sulfamoyl substituted with lower alkyl; R.sup.3 is hydrogen, nitro, or halogen; R.sup.4 is hydrogen, lower alkyl, substituted lower alkyl, lower cycloalkyl, or substituted lower cycloalkyl; R.sup.5 's are substituents independently selected from the group consisting of halogen, nitro, cyano, lower alkyl, carbamoyl, and carbamoyl substituted with lower alkyl; and n is an integer of 0 to 4. The derivative works as an antagonistic agent against both the NMDA receptors and the AMPA receptors, so that it is effective as a therapeutic agent for neurological disorders caused by excitatory amino acids binding to the receptors.
REFERENCES:
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J. Mosinger et al., "Blockade of Both NMDA and Non-NMDA Receptors Is Required for Optimal Protection Against Ischemic Neuronal Degeneration in the in Vivo Adult Mammalian Retina", Exp. Neurol., 113, pp. 10-17 (1991).
M. Sheardown et al., "A Potent Antagonist of the Strychnine Insensitive Glycine Receptor Has Anticonvulsant Properties", Eur. J. Pharmacol., 174, pp. 197-204 (1989).
M. Sheardown et al., "2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline: A Neuroprotectant for Cerebral Ischemia", Science, 247, pp. 571-574 (1990).
Adachi Makoto
Chomei Nobuo
Eigyo Masami
Kawasaki Kazuo
Takada Susumu
Haley, Jr. James F.
Mullis Jeffrey C.
Shionogi & Co. Ltd.
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