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Generated: December 17, 2017

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Title: Inactive metabolite approach to soft drug design
Abstract: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.alpha.-alkoxycarbonyloxy-11.beta.-hydroxyandrost-4-en-3-one-17.beta.-ca rboxylates and the corresponding .DELTA..sup.1,4 compounds, optionally bearing 6.alpha.- and/or 9.alpha.-fluorine and 16.alpha.- or 16.beta.-methyl substituents. Especially preferred compounds include haloalkyl 17.alpha.-alkoxycarbonyloxy-9.alpha.-fluoro-11.beta.-hydroxy-16-methylandr osta-1,4-dien-3-one-17.beta.-carboxylates.
Inventor(s): Bodor; Nicholas S. (Gainesville, FL)
Assignee: Bodor; Nicholas S. (Gainesville, FL)
Filing Date:May 01, 1995
Application Number:08/431,727
Claims:1. A method for the design of a soft drug entity, the in vivo metabolic disposition of which proceeds in predictable manner into an inactive metabolite moiety and nontoxic moieties thereof after eliciting its desired therapeutic response, comprising (a) identifying a nontoxic, therapeutically inactive candidate metabolite of a given drug entity known to elicit a particular therapeutic response, and (b) structurally converting such therapeutically inactive metabolite into an activated, structurally-related drug species that also elicits such particular therapeutic response, but which activated drug species will in vivo metabolically cleave into said identified inactive metabolite moiety and other nontoxic moieties thereof.

2. A method for eliciting the therapeutic response of a known drug entity in a warm-blooded animal in need of such treatment, comprising administering to such warm-blooded animal a therapeutically effective amount of a corresponding soft drug, entity designed by the method as defined by claim 1.

3. The method according to claim 1, wherein the inactive metabolite is activated by modifying it so that it resembles the known drug isosterically.

4. The method according to claim 1, wherein the inactive metabolite is activated by modifying it so that it resembles the known drug isoelectronically.

5. The method according to claim 1, wherein the inactive metabolite is activated by modifying it so that it resembles the known drug isosterically and isoelectronically.

6. The method according to claim 1, wherein a known inactive metabolite of said known drug is selected.

7. The method according to claim 1, wherein an inactive metabolite of said known drug is designed by the introduction of transporting group in noncritical structural parts.

8. The method according to claim 1, wherein the soft drug is designed to cleave in vivo, after achieving its therapeutic effect, to the starting inactive metabolite and other nontoxic moieties.
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