Substituted phenylacetylenes, pharmaceuticals containing them and methods for the preparation of these compounds and pharmaceuticals.

摘要

The substituted phenylacetylenes according to the invention are specifically acting 5-lipoxygenase inhibitors and can be used, in particular, in pharmaceutical preparations for the therapy of pathologic conditions in which leukotrienes are involved as mediators. The phenylacetylenes have the general formula …… in which one of the radicals R1 is a hydrogen atom and the other is the group of the formula …… … …  in which R3 denotes a hydrogen atom, a methyl or ethyl radical, and R4 denotes a methyl radical or an amino group, …  and in which R2 is a monocyclic or dicyclic aromatic or a sulphur-, nitrogen- or oxygen-containing heterocyclic radical which is optionally substituted as defined above. … …These compounds can be prepared according to the invention for example by reacting a compound of the formula …… in which R2 has the same meaning as above and one of the radicals R7 is hydrogen and the other one is the group of the formula -CO-R3, with hydroxylamine to give the oxime, reducing the latter to the correspondingly substituted hydroxylamine compound and finally introducing the group of the formula -COR4. This preparation method and others are described.