Patent Evaluation: Potent dual Acting PAF/Histamine Antagonists

Summary

Novelty: Novel thazolidine carboxylic acid amide derivatives are disclosed. They are PAF antagonists and are potentially useful as anti-allergic and anti-asthmatic agents.

Biology: The compounds are evaluated for PCA inhibition in rats. At a dose of 6.4 mg/kg po, 56% inhibition is observed. The compounds are also evaluated in vitro for inhibition of PAF-induced, blood platelet aggregation (IC₅₀ = 1.8×10-⁶g/ml) and PAF-receptor binding (IC₅₀ = 6.7 × 10–7 g/ml).

Chemistry: 3-[4-(Diphenylmethylene)-1-piperidyl]propylcarbamoyl-2-(3-pyridyl)thiazolidine is one of fourteen specifically claimed compounds.