Patent Evaluation: Novel cholinesterase inhibitors

Summary

Novelty: The use of [[(aminocarbonyloxy)-1-indanon]-2-yl]methylpiperidines and 6-(aminocarbonyloxy)-2-[(pyridin-4-yl)methylenyl]-1-indanones for the treatment of memory dysfunctions is claimed. They are stated to have acetylcholinesterase inhibitory activity and to be useful for the treatment of Alzheimer's disease.

Biology: Acetylcholinesterase inhibition was measured using rat brain preparations. The specified compound gave an IC₅₀ value of 1.34mM.

Chemistry: A process for the preparation of the compounds is claimed and exemplified in five cases. Four compounds are specifically claimed including 1-benzyl-4-[[6-(methylaminocarbonylxoy))-1-indanon]-2-yl]methylpiperidine.