| 摘要 |
<p>The invention comprises amides of 18a - and 18b -glycyrrhetinic and oleanolic acids, 3-acylates thereof wherein the acyl group may contain a carboxyl group in the free or salt form, and 3-keto derivatives thereof, wherein the amide group is of formula -CONR1R11 in which R1 and R11 are hydrogen atoms or optionally substituted alkyl, cycloalkyl, aryl or aralkyl radicals or the group -NR1R11 is a heterocycle, and their preparation by reaction of a 3-acyloxy or 3-keto acid halide with an appropriate amine, followed if desired by (a) hydrolysis of the 3-acyl group or of an ester substituent in the amide group, (b) re-acylation of a 3-ol with a dicarboxylic acid, and (c) conversion of any free carboxylic group into a salt. The compounds of the invention have anti-inflammatory activity and may be used in pharmaceutical compositions in combination with a carrier, for example in forms suitable for oral or parenteral administration.</p> |
