40385-99-7Relevant academic research and scientific papers
CORTICOID-17,21-DICARBOXYLIC ESTERS AND CORTICOSTEROID 17-CARBOXYLIC ESTER 21-CARBONIC ESTERS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICALS CONTAINING THESE COMPOUNDS
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, (2008/06/13)
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 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, 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. They have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses.
Corticosteroid 17-alkyl carbonate 21-[0]-carboxylic and carbonic esters, and pharmaceuticals containing these compounds
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, (2008/06/13)
Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I STR1 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 CH3 ; R(1) is aryl or hetaryl; n and m are zero or 1; R(2) is alkyl or --(CH2)2 --OCH3 ; R(3) is H or methyl. They are obtained by reacting a compound of the formula II, STR2 in which R(5) is OH, with an activated carboxylic acid of the formula III, The compounds I have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects, which ratio is often markedly superior to that of analogous corticoid 17-alkyl carbonate 21-esters which do not carry any aryl or heteraryl group in the 21-ester radical.
