Patent Evaluation Central & Peripheral Nervous Systems: Benzoxazolinone and benzothiazolinone derivatives

Abstract

This patent describes a series of new benzoxazolinone and benzothiazolinone derivatives that are claimed to interact selectively with sigma (σ) binding sites in the brain. Their in vitro affinities for these binding sites are not disclosed. In vivo, they are active in animal tests commonly used to predict antipsychotic, anxiolytic and antidepressant activity. Surprisingly, they also appear to be active in an animal model of rheumatoid arthritis.

The compounds are undoubtedly of interest in terms of their in vivo pharmacology, either for use in psychiatry or for the treatment of rheumatoid arthritis. However, it is not clear to what extent the activities described are really due to an interaction with σ binding sites.