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Claims for Patent: 5,482,934

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Claims for Patent: 5,482,934

Title: Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions
Abstract:The present invention relates to compounds of the formula: ##STR1## in which X.sub.1 and X.sub.2 correspond to H or F without distinction; R.sub.1 represents the following radicals: ##STR2## and R.sub.2 represents the radicals ##STR3## in the form of an R epimer, an S epimer, or a stereoisomeric mixture of the R and S epimers in terms of the orientation of the substituents on the carbon atom at position 22, novel intermediates and a method of their preparation by hydrolysis-ketalization, and use of such compounds as drugs and/or therapeutic agents.
Inventor(s): Calatayud; Jose (Madrid, ES), Conde; Jose R. (Madrid, ES), Luna; Manuel (Madrid, ES)
Assignee: Especialidades Latinas Medicamentos Universales, S.A. (Elmu, S.A.) (Madrid, ES)
Application Number:08/278,112
Patent Claims: 1. A compound of the formula ##STR20## in the form of an R epimer, an S epimer, or a stereoisomeric mixture of the R and S epimers in terms of the orientation of the substituents on the carbon atom at position 22, wherein:

R.sub.1 is cyclohexyl,

R.sub.2 is a member selected from the group consisting of ##STR21## and wherein X.sub.1 and X.sub.2 may be the same or different and each is a member selected from the group consisting of hydrogen and fluorine.

2. A compound according to claim 1 in the form of the (22S)- epimer.

3. A compound according to claim 1 in the form of the (22R)- epimer.

4. An anti-inflammatory drug containing a compound according to claim 1.

5. A method of treating inflammatory conditions which comprises administering to a patient an anti-inflammatory effective amount of a compound according to claim 1.

6. A pharmaceutical composition having anti-inflammatory properties comprising as the active ingredient an effective amount of a compound according to claim 1 together with a pharmaceutically acceptable carrier.

7. A method for the treatment and control of inflammatory conditions characterized by the topical administration to a patient of an effective dose of a compound according to claim 1.

8. The compound of claim 1 which is [11.beta.,16.alpha.(R,S)]-16,17-[cyclohexylmethylene)bis (oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)pregna-1,4-diene-3,20-dione.

9. The R-epimer of the compound of claim 8.

10. The S-epimer of the compound of claim 8.

11. A compound of claim 1 wherein each of is X.sub.1 and X.sub.2 is hydrogen.

12. A compound of claim 1 wherein each of X.sub.1 and X.sub.2 is fluorine.
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