Patent Evaluation: The use of Pyridols in the Treatment of Alzheimer's Disease

Summary

Novelty: New substituted 4-amino-3-pyridinols, which are said to ameliorate memory dysfunction, are disclosed.

Biology: The compounds were assessed for their ability to reverse scopolamine-induced memory deficit in a variety of animals. A 26.6% reversal was achieved using 0.3 mg/kg (sc) of 4-[[(dimethylamino)-methylene]amino]-3-pyridinol-N,N-diethylcarbamate], compared with 13% at 0.63 mg (sc) for the standard, tacarine. In an in vitro, rat striatum, AChE inhibition assay, the most active compounds had IC₅₀ values approximately 2000 times greater than physostigmine.

Chemistry: The compounds were synthesized using fourteen methods and are described in forty one examples. 4-Amino-3-pyridinol-N,N-dimethylcarbamate is one of several specifically claimed examples.

Structure: