Invention Grant
US07691811B2 Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye 有权
转运蛋白增强的皮质类固醇活性以及用于治疗干眼症的方法和组合物

Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye
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-cn-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 C1-5 alkyl; Y is —OH, —SH or —OCOR4 wherein R4 is C1-5 alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated. Ophthalmic administration in the treatment of dry eye is specifically targeted.
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