Patent Evaluation: Phenoxyalkanoic Acids as Cholesterol Lowering Agents

Summary

Novelty: Novel phenoxyalkanoic acids are disclosed and are said to be hyperlipidaemic agents. They are potentially useful in the treatment of hypercholesterolaemia, hyperlipidaemia and arteriosclerosis.

Biology: The effect of the compounds on serum total cholesterol (STC) levels in male Sprague-Dawley rats was demonstrated. The total cholesterol level in the serum was measured enzymatically according to a previously established method (Clinical Chemistry (1974) 20:470). The percentage decrease in STC was recorded for five compounds and was in the range 49-73%.

Chemistry: Three compounds are specifically claimed. A total of twenty-eight compounds are disclosed and are exemplified by synthesis. Yields, mps, IR, MS and ¹H nmr are detailed. One of the specifically claimed compounds is 2-[4-(2-(p-chlorobenzene sulphonylamino)propyl)phenoxy]-2-methylpropionic acid.

Structure: