16-Methyl-11-oxygenated-pregnadiene or pregnatriene derivs. - useful as antiinflammatories and antiallergics with reduced side effects

摘要

Corticoids of formula (I) are new (..... indicates a single or double bond; X is beta-hydroxymethylene or CO; R1 is H or physiologically tolerable acid residue. R2 is F, Cl or CH3). They are prepd. e.g. by hydroxylation of 11-unsubstd. cpds. e.g. by fermentation. (I) are antiinflammatories with minimal thymolytic catabolic or mineral-corticoid side effects. They are useful for treating e.b. eczema, polyarthritis, hay fever, respiratory allergies etc. Typical oral doses contain 0.1-50 mg. (I) and typical aerosols for inhalation 0.01-2% (I). In an example, 11beta,-21-dihydroxy-6,16alpha-dimethyl-4,6-pregnadiene-3,20-dion- e was prepd. from the 21-hydroxy by fermentation with Curvularia lunata NRRL 2380.