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 …<IMAGE>… in which one of the radicals R1 is a hydrogen atom and the other is the group of the formula …<IMAGE>… … … 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 …<IMAGE>… 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. |