Corticosteroid 17-alkyl carbonate 21-[0]-carboxylic and carbonic esters, processes for their preparation, and pharmaceuticals containing these compounds

There are described 17-alkyl carbonate-21-carbonic/carboxylic acid esters of corticosteroids of the formula I where A is CHOH or CHCl, CH2, C = O, a 9(11) double bond; Y is H, F, Cl; Z is H, F, CH3; R(1) is aryl, hetaryl; n and m are zero or 1; R(2) is alkyl, -(CH2)2-OCH3; R(3) is H, methyl. They ar...

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Bibliographic Details
Main Authors H.G. ALPERMANN, W. DUERCKHEIMER, U. STACHE
Format Patent
LanguageEnglish
Published 28.02.2001
Edition7
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
STEROIDS
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Summary:There are described 17-alkyl carbonate-21-carbonic/carboxylic acid esters of corticosteroids of the formula I where A is CHOH or CHCl, CH2, C = O, a 9(11) double bond; Y is H, F, Cl; Z is H, F, CH3; R(1) is aryl, hetaryl; n and m are zero or 1; R(2) is alkyl, -(CH2)2-OCH3; R(3) is H, methyl. They are obtained by reacting a compound of the formula II in which R(5) is OH, with an activated carboxylic acid of the formula III R(6)-CO-(O)n-[(C1-C4)-alkyl]m-R(1) III The compounds I have very potent local and topical anti-inflammatory activity and show a very good ratio of local to systemic anti-inflammatory action, which is often clearly superior compared with analogous corticoid 17-alkyl carbonate 21-esters which do not carry an aryl or hetaryl group in the 21 ester radical.
Bibliography:Application Number: CN19941015711