Inactive metabolite approach to soft drug design

摘要

The invention provides novel soft steroidal anti-inflammatory agents, pharmaceutical compositions containing said agents, and methods of administering same to mammals in the treatment of inflammation. Preferred compounds of the invention include haloalkyl 17&agr;-alkoxycarbonyloxy-11&bgr;-hydroxyandrost-4-en-3-one-17&bgr;-carboxylates and the corresponding &Dgr;^1,4 compounds, optionally bearing 6&agr;- and/or 9&agr;-fluorine and 16&agr;- or 16&bgr;-methyl substituents. Especially preferred compounds include haloalkyl 17&agr;-alkoxycarbonyloxy-9&agr;-fluoro-11&bgr;-hydroxy-16-methylandrosta-1,4-dien-3-one-17&bgr;-carboxylates.