| 摘要 |
Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17alpha- alkoxycarbonyloxy-11beta-hydroxyandrost-4-en-3-one-17beta- carboxylate type and the corresponding Delta1,4-compounds are described. The enhancing agents have the formula: (II) wherein R is H or C1-C4 alkyl; Z1 is carbonyl or beta- hydroxymethylene; X1 is -O- or -S-; R5 is -OH, -OR 6, -OCOOR6 or -OCOR7 wherein R6 is C 1-C4 alkyl and R7is C1-C4 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 C1-C4 alkyl, then R5 is -OH.
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