Invention Grant
US07687484B2 Transporter enhanced corticosteroid activity 有权
转运蛋白增强皮质类固醇活性

Transporter enhanced corticosteroid activity
Abstract:
Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17α-alkoxycarbonyloxy-11β-hydroxyandrost-4-en-3-one-17β-carboxylate type and the corresponding Δ1,4-compounds are described. The enhancing agents have the formula: wherein Z1 is carbonyl, β-hydroxymethylene or methylene; R2 is H, —OH or —OCOR3 wherein R3 is C1-C5 alkyl; Y is —OH, —SH or —OCOR4 wherein R4 is C1-C5 alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated.
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