Patent Evaluation: Novel Pyridinyithiazolidine Derivatives as PAF Antagonists

Summary

Novelty: Novel pyridinylthiazolidine compounds, said to have platelet activating factor (PAF) antagonist activity, are disclosed. These compounds may be useful in treating PAF-mediated disorders such as respiratory distress syndrome, shock and acute inflammation.

Biology: The ability of the compounds to inhibit PAF activity was determined in vitro using a standard PAF receptor binding assay. Results are presented as a table of K_i values.

Chemistry: In US5120751, the syntheses of these compounds are outlined in five reaction schemes. Twenty-one compounds are exemplified, and nine specifically claimed, including N-(3-benzoylphenyl)-2-(3-pyridinyl)-4-thiazolidine carboxamide. In US5120749, the syntheses of fifty-three compounds are described. The compounds are prepared by multistep processes. Thirty-nine compounds are specifically claimed including 3-[2-(3-pyridinyl-tazolid-4-ylmethyl]indole.

Structure: