摘要 |
Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17alpha-alkoxy-11beta-hydroxyandrost-4-en-3-one-17beta-carboxylate type and the corresponding Delta<SUP>1,4 </SUP>compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl; Z<SUB>1 </SUB>is carbonyl or beta-hydroxymethylene; X<SUB>1 </SUB>is -O- or -S-; R<SUB>5 </SUB>is -OH, -OR<SUB>6</SUB>, -OCOOR<SUB>6 </SUB>or -OCOR<SUB>7 </SUB>wherein R<SUB>6 </SUB>is C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl and R<SUB>7 </SUB>is C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl, then R<SUB>5 </SUB>is -OH.
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