Patent Evaluation: Novel Pyridines as TXA₂ Synthase Inhibitors

Summary

Novelty: Novel phenylsulphonamide substituted pyridine alkene and aminooxyalkane carboxylic acid derivatives are disclosed. These compounds are said to be thromboxane synthetase inhibitors which are potentially useful for treating asthma, atherosclerosis and allergic diseases.

Biology: TXA₂ inhibition was evaluated in vitro (IC₅₀ = 0.5–1 nM). Thromboxane receptor binding studies are also reported.

Chemistry: (EZ)-5-[[[3-pyridinyl-3(4-chlorophenylsulphonamido)phenyl]methylen]iminooxy]-pentane carboxylic acid is one of twenty-six exemplified compounds.

Structure: