Patent Evaluation: Novel tricyclic quinoxalinediones as strychnine insensitive glycine antagonists

Summary

Novelty: A novel series of tricyclicquinoxalinediones is claimed. These compounds are described as potent antagonists at strychnine-insensitive glycine modulatory sites of NMDA receptors. They may be useful in the treatment or prevention of a number of CNS disorders including neurodegenerative disorders, pain, depression and schizophrenia.

Biology: No biological data are provided, although the compounds are stated to have been evaluated for both [³H]-MK801 and [³H]-glycine binding.

Chemistry: One hundred and forty-four compounds are given as examples with full experimental and spectral details. No preferred compounds are described or named within the claims. One of the examples is 9-bromo-5-carboxy-6,7-dihydro-lH, 5H-pyrido[1,2,3-de]quinoxaline-2,3-dione.