| 摘要 |
The invention comprises D 4-3,20-dioxo-6a -fluoro-16a -methyl-11b , 14a , 17a 21-tetrahydroxypregnene and 21-esters thereof. They may be prepared by enzymatic hydroxylation of the corresponding 11-unsubstituted-pregnenes, with, for example, enzymes of the fungus Cunninghamella elegans or enzymes obtained from suprarenal glands. Esters and the free 21-ol may be interconverted by standard esterification and hydrolysis procedures. Examples are given and an extensive list of esterifying organic and inorganic acids is provided. D 4-3, 20-dioxo-6a -fluoro-16a -methyl-14a , 17a , 21-trihydroxypregnene and esters thereof are prepared by enzymatic hydroxylation, e.g. using Curvularia lunata, of the corresponding 14-unsubstituted pregnenes. They may be separated from the concomitantly formed D 4-3,20-dioxo-6a -fluoro-16a -methyl-11b , 17a , 21-trihydroxypregnene or esters thereof by, for example, chromatography on silica gel. The steroids of the invention, which are stated to have anti-inflammatory properties, may be formulated as pharmaceutical compositions with suitable excipients. These may take the form of oily or aqueous solutions, suspensions, emulsions, implants, tablets, dragees, ointments or creams, and may contain preserving, stabilizing, wetting or emulsifying agents, salts for regulating the osmotic pressure or buffers.
|
