Alkyl, azido, alkoxy, and fluoro-substituted and fused quinoxalinediones
AssigneesState of Oregon, acting by and through The Oregon State Board of Higher Education, acting for and on behalf of The Oregon Health Sciences University and The University of Oregon, Eugene Oregon, Acea Pharmaceuticals, Inc., The Regents of the University of California
InventorsSui X. Cai, Eckard Weber, John F.W. Keana, Sunil Kher
Life of this patent
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Abstract
Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, and inducing anesthesia are disclosed by administering to an animal in need of such treatment an alkyl or azido-substituted 1,4-dihydroquinoxaline-2,3-dione or pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.
Claims10
A compound having the Formula ##STR46## or a tautomer or a pharmaceutically acceptable salt thereof;
- wherein R.sup.1 is nitro, cyano, CF.sub.3, carboxy, or alkanoyl;
- R.sup.2 is alkoxy, aralkoxy, thioalkyl, hydroxy, mercaptoalkyl, azido, or NR.sup.5 R.sup.6, wherein R.sup.5 and R.sup.6 are independently hydrogen, alkyl, or aryl groups;
- R.sup.3 is halo, haloalkyl, nitro, alkyl, alkoxy, azido, or cyano;
- and
- R.sup.4 is hydrogen.
A compound having the Formula ##STR47## or a tautomer or a pharmaceutically acceptable salt thereof;
- wherein R.sup.1 is nitro, fluoro, and chloro;
- R.sup.2 is fluoro, chloro, alkyl, azido, or cyano;
- R.sup.3 is fluoro or chloro;
- and
- R.sup.4 is hydrogen;
- with the proviso that at least one of R.sup.1 -R.sup.3 is fluoro and that R.sup.2 is not fluoro, when R.sup.1 is nitro.
A pharmaceutical composition, comprising the compound of any one of claims, 1 and 3 and a pharmaceutically acceptable carrier.
A compound having the Formula:
- ##STR48## or a tautomer or a pharmaceutically acceptable salt thereof;
- wherein R.sup.1 is alkyl, azido, alkoxy, hydroxy, haloalkyl, halo, nitro, cyano or alkanoylamino;
- R.sup.2 is alkyl, azido, alkoxy, aralkoxy, cyano, haloalkyl, halo, hydroxy or nitro;
- R.sup.3 is alkyl, azido, alkoxy, cyano, halo, haloalkyl or hydroxy;
- R.sup.4 is hydrogen or fluoro;
- provided that (a) at least one of R.sup.1, R.sup.2 or R.sup.3 is hydroxy or azido, or (b) at least one of R.sup.2 or R.sup.3 is alkyl or alkoxy, or (c) R.sup.1 is cyano.
Dependencies are inferred from the claim text.