Patent Evaluation: AChE Inhibitors for the Treatment of Dementia

Summary

Novelty: Novel quinoline 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: