Patent Evaluation: Bicyclic Bisaryl Compounds as LTB₄ Antagonists

Summary

Novelty: Novel LTB₄ antagonists are claimed; they are potentially useful for the treatment of inflammatory or hypersensitive conditions. The compounds described are (di)substituted aryl or heteroaryl substituted carboxylic acids.

Biology: IC₅₀ data for 150 compounds are tabulated for in vitro receptor binding studies and LTB₄-induced g.p. parenchyma contraction assays. Values given are in the range of 0.5–5000 nM. Details of other tests are provided but no data for the claimed compounds are reported.

Chemistry: There are twenty-one synthetic examples. The compound shown is 6[[4-(3,4-methylenedioxyphenyl)-6-phenyl-2-pyridyl]oxy]hexanoic acid.

Structure: