| abstract |
The new benzoic acid derivatives according to the invention are specific-acting, sufficiently stable 5-lipoxygenase inhibitors and can be used in particular in pharmaceutical preparation forms for the therapy of pathological conditions in which leukotrienes are involved as mediators. They correspond to the general formula wherein A and E are -C≡C- and B and D are -CH₂-CH₂- or A, B and D are each -C≡C- or cis-CH = CH- and E is trans-CH = CH- stand, R₁ is hydrogen, methyl or ethyl, R₂ is hydrogen, optionally a substituted alkyl or phenyl radical or a cycloalkyl radical, R₃ is hydrogen, acetyl or propionyl and R₄ is a carboxyl group or a functional derivative thereof, such as a salt, an ester , an amide or a hy droxamic acid, or represents a nitrile group.n n n The preparation of the compounds of the formula I according to the inventionntakes place in particular by building up the aliphatic chainnbased on suitable acetylene compounds. The rest R₄ cannthen converted into other desired carboxyl group derivativesnbe changed. By partial or complete hydrogenationnA, B, D and E can be varied within the scope of the definition. |