Patent Evaluation: Novel Benzylpiperidines as Potent AChE Inhibitors

Summary

Novelty: Novel benzylpiperidine derivatives are claimed and are said to have AChE inhibitory activity, without associated side-effects. Such compounds are claimed to be potentially useful for the prevention and treatment of senile dementia and other memory disturbances.

Biology: In vivo rodent studies involving scopolamine-induced (0.5 mg/kg ip) amnesia, are described. Preferred compounds gave > 90% memory improvement at doses of 0.1–0.3 mg/kg (po). Toxicity studies showed no fatalities at 300 mg/kg (po).

Chemistry: 2-(4-(1-Benzylpiperidyl)ethyl)-2,3-dihydropyrrolo[3,4-b]quinoline-1-one is one of seventy-eight exemplified compounds. Preparative details using standard techniques are presented.

Structure: