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Anti-Inflammatory, Anti-Allergic, Respiratory & GI Agents

Patent Evaluation: Substituted tetralins and chromans as LTD4 antagonists

Pages 113-114 | Published online: 02 Mar 2011
 

Summary

Novelty: Chromans and tetralins are claimed as effective 5-lipoxygenase inhibitors and/or leukotriene antagonists.

Biology: The activity of the compounds is assessed using the following assays: RBL-1 5-lipoxygenase, [3H]-LTD4 binding to guinea-pig lung, [3H]-LTB4 binding to human PMN and PAF-induced death in mice. No data are presented.

Chemistry: Some four hundred compounds are exemplified. Together with twenty-eight intermediates. The majority of these are described in full. Thirteen compounds are explicitly claimed including (3R,4S) 3-(3-methoxyphenyl)methyl-6-(quinolin-2-yl)methoxy chromanol.

Structure:

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