Enhancement of activity and/or duration of action of...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

Reexamination Certificate

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C514S179000, C514S944000, C514S945000, C514S951000, C514S960000, C514S966000

Reexamination Certificate

active

10868955

ABSTRACT:
Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17α-alkoxy-11β-hydroxyandrost-4-en-3-one-17β-carboxylate type and the corresponding Δ1,4compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula:wherein R is H or C1-C4alkyl; Z1is carbonyl or β-hydroxymethylene; X1is —O— or —S—; R5is —OH, —OR6, —OCOOR6or —OCOR7wherein R6is C1-C4alkyl and R7is C1-C4alkyl, 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-C4alkyl, then R5is —OH.

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Druzgala et al.,J. Steroid Biochem. Molec. Biol., vol. 38, No. 2, pp. 149-154, published by Pergamon Press Kidlington, Oxford, UK (1991).
Little et al,Pharmaceutical Research, vol. 16, No. 6, pp. 961-967, published by Plenum Publishing Corporation, New York, New York (1999).

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