Patent Evaluation: Novel Quinoline Leukotriene Receptor Antagonists

Summary

Novelty: Unsaturated hydroxyalkylquinoline acids, which are said to be leukotriene antagonists and inhibitors of leukotriene biosynthesis, are disclosed. Quinoline acids may be useful for treating conditions such as angina, cerebral spasm and hepatitis.

Biology: Leukotriene antagonism was evaluated in LTD₄ receptor binding studies undertaken on g.p. lung membranes (in vitro) and in vivo in guinea pigs. A PMN leukocyte LTB₄ assay was also performed. In vivo leukotriene antagonism and leukotriene biosynthesis inhibition were assessed using asthmatic rats and pulmonary mechanics tests. However, no data are provided.

Chemistry: The syntheses of the compounds are described in fifteen reaction schemes. Preparatory details are included for thirty-nine compounds. A further one hundred and sixty-seven examples are given. All compounds were prepared by conventional methods.

Structure: