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US 4,472,393 AGranted
3,20-Dioxo-1,4-pregnadiene-17.alpha.-ol 17-aromatic heterocycle carboxylates
AssigneeSchering Corporation
InventorElliot L. Shapiro
Life of this patent
Estimating the term…
Abstract
This invention relates to novel 3,20-dioxo-1,4-pregnadiene-17.alpha.-ol 17-aromatic heterocyclic carboxylates, to pharmaceutical formulations thereof, and their use in the treatment and control of inflammatory conditions.
Claims31
A 3,20-dioxo-1,4-pregnadiene of the following formula:
- ##STR3## X is a member selected from the group consisting of hydrogen and halogen having an atomic weight less than 100;
- Y is a member selected from the group consisting of (H,H) provided X is hydrogen, oxygen, (H,.beta.OH), and (H,.beta.-halogen) provided X is chlorine or bromine, said .beta.-halogen having an atomic weight of less than 100 and being at least as electronegative as X;
- Z is hydrogen, CH.sub.3, chlorine, or fluorine;
- V is an acyl radical of an aromatic heterocyclic carboxylic acid selected from the group consisting of thiophenecarboxylic acid, pyrrolecarboxylic acid and furancarboxylic acid, and methyl and halogen-substituted derivatives thereof;
- W is a member selected from the group consisting of (H,H);
- (H, lower alkyl);
- (H, OV.sub.1) wherein V.sub.1 is a member selected from the group consisting of hydrogen and an acyl radical of an acid selected from the group consisting of a hydrocarboncarboxylic acid having up to 12 carbon atoms, benzoic acid substituted by a halogen or methoxy group, retinoic acid, and isonicotinic acid;
- .dbd.CHT wherein T is a member selected from the group consisting of hydrogen, lower alkyl, fluorine, and chlorine;
- G is hydrogen, a halogen having an atomic weight less than 100, or OV.sub.2 wherein V.sub.2 is a member selected from the group consisting of hydrogen, an acyl radical of a hydrocarboncarboxylic acid having up to 12 carbon atoms, benzoic acid substituted by a halogen or methoxy group, retinoic acid, isonicotinic acid, and the acid radical of phosphoric acid and mono- and dialkali and alkaline earth metal salts thereof;
- and the 6-dehydro and 1,2-dihydro analogs of the foregoing.
7 more elements
Dependencies are inferred from the claim text.