Generated: April 25, 2017
|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)|
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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