Patent Evaluation: Novel Piperidines as Leukotriene Antagonists

Summary

Novelty: 4-Diarylmethoxypiperidines which bear an N-linked alkoxyaryl moiety and are potentially useful for the treatment of allergic conditions, such as urticaria, eczema and asthma, are disclosed.

Biology: Histamine (10^–5 M)- and leukotriene (10-⁸ M)-induced contractions in guinea pig ileum were antagonized at a concentration of 10^–7 M of test compound.

Chemistry: Five schemes are presented for preparation of the compounds which employ standard techniques and are exemplified in seventy cases. Several compounds are specifically claimed, including 1-[3-(4-acetyl-3-hydroxy-2-n-propyl-phenoxy)propyl]-4-[(4-chloro)-phen-yl-2-pyridylmethoxy]piperidine.

Structure: