Warner-lambert Company

Chung Stephen Yi

Christopher Franklin Bigge

Thomas C Malone

Robert Michael Schelkun

Gerald David Nordblom

Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones represented by the formula:

Glutamate (ampa/kainate) receptor antagonists: N-substituted fused azacycloalkylquinoxalinediones

Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones are disclosed represented by the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, alkyl or W-alkyl; X and Y are independently hydrogen, halogen, nitro, cyano, trifluoromethyl, SO.sub.2 CF.sub.3, SO.sub.2 R.sup.4, SO.sub.2 NR.sup.4 R.sup.5, alkyl, alkenyl, (CH.sub.2).sub.z CONR.sup.4 R.sup.5, (CH.sub.2).sub.z COOR.sup.4, or NHCOR.sup.4, wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl having 1 to 6 carbon atoms, cycloalkyl or W-alkyl, and z is an integer from 0 to 4; R.sup.2 is benzoyl, W, W-alkyl, COcycloalkyl, COalkyl-W, CONR.sup.3 alkyl, CONR.sup.3 -W, CONR.sup.3 alkyl-W, CSNR.sup.3 alkyl, CSNR.sup.3 alkyl-W, ##STR2## or a moiety derived from a common amino acid by removal of the --OH from the carboxyl group which is alpha to the amino, wherein --W is aryl, heteroaryl, or the heterocycles piperidinyl, piperazinyl, morpholinyl or pyrrolidinyl, wherein R.sup.3 is hydrogen, alkyl or W-alkyl; and m and n are independently 0, 1 or 2 provided that m+n is &gt;1; provided that when R.sup.2 is benzoyl, ##STR3## or X is nitro, Y and R.sup.1 are H, m is 2 and n is 1; when R.sup.2 is ##STR4## X is nitro, Y and R.sup.1 are H and m is 2 and n is 1; or when R.sup.2 is ##STR5## X is bromo, Y and R.sup.1 are H, m is 1 and n is 2. The novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones may be used, for example, as neuroprotective agents, for treatment of chronic neurodegenerative disorders, as anticonvulsants and in the treatment of schizophrenia, epilepsy, anxiety, pain and drug addiction.

Glutamate (ampa/kainate) receptor antagonists: N-substituted fused

The invention discloses novel fused-azacylic quinoxalinediones. These compounds may be employed as excitatory amino acid antagonists and as analogs for use in immunological assays. The invention is also directed to both a radioimmunoassay and enzyme immunoassay for detecting and quantitating 1,4,7,8,9,10,-hexahydro-9-methyl-6-nitropyrido[3,4-f]-quinoxaline-2,3-dion e PNQX and analogs thereof.

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Ann Arbor, MI, United States of America

Chung Stephen Yi