Corticoid -17,21-dicarboxylic esters and corticosteroid...

Details Corticoid -17,21-dicarboxylic esters and corticosteroid... Corticoid -17,21-dicarboxylic esters and corticosteroid...

C - Chemistry, Metallurgy

07

J

C07J 5/00 (2006.01) C07J 17/00 (2006.01) C07J 31/00 (2006.01) C07J 33/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01)

Patent

CA 2133607

Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds Corticoid 17,21-dicarboxylic esters and corticoid 17- carboxylic ester 21-carbonic esters of the formula I Image are described, in which A is CHOH and CHCl, CH2, C=O or 9(11) double bond; Y is H, F or Cl; Z is H, F or methyl; R(1) is aryl or hetaryl; R(2) is alkyl and R(3) is H or methyl. They are obtained, inter alia, by reacting a compound of the formula II, Image in which R(S) is OH, with an activated carboxylic acid of the formula III, R(6)-CO-(O)n(C1-C4)-alkyl]m-R(1) III. They have a very strong local and topical antiinflamma-tory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses.

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