Patent Evaluation: Heterocyclic Cholinesterase Inhibitors

Summary

Novelty: Novel condensed heterocyclic compounds are disclosed, which are potentially useful as cholinesterase inhibitors and hence as therapeutic and prophylactic agents for senile dementia and Alzheimer's disease.

Biology: In an in vitro rat cerebral cortex assay for AChE inhibition, the most effective compound had an IC₅₀ = 6.5 nM.

Chemistry: Syntheses of the compounds are described in thirty-three examples. 3-Methyl-7-[1-oxo-3-[1-(phenylmethyl)piperidin-4-yl]propyl]-2,3,4,5-tetrahydro-1H-3-benzazepine is one of ten specifically claimed examples.

Structure: