Patent Evaluation: Bis-arylamide and urea antagonists of platelet activating factor

Summary

Novelty: Bis-arylamides and ureas are claimed as PAF antagonists suitable for the treatment of a range of allergic, shock-induced and thrombotic disorders.

Biology: The activities of twenty compounds in an in vitro PAF-induced platelet anti-aggregation model are detailed, as are data from in vivo PAF-induced hypotensive shock and endotoxin induced shock models in mice. The compound shown is effective in all three models.

Chemistry: Synthesis is illustrated in nine flow diagrams and ninety-one examples. The preferred compound is 5-methyl-2[3-[[[3-(tetradecyloxy)phenyl]acetyl]amino]phenyl]-methyl thiazolium bromide.

Structure: