Invention Grant
- Patent Title: Enhancement of activity and/or duration of action of soft anti-inflammatory steroids for topical or other local application
- Patent Title (中): 增强软性抗炎类固醇的局部或其他局部应用的活性和/或持续时间
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Application No.: US12480953Application Date: 2009-06-09
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Publication No.: US07923441B2Publication Date: 2011-04-12
- Inventor: Nicholas S. Bodor
- Applicant: Nicholas S. Bodor
- Agency: Buchanan Ingersoll & Rooney PC
- Main IPC: A61K31/56
- IPC: A61K31/56

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 R is H or C1-C4 alkyl; Z1 is carbonyl or β-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is 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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