CORTICOSTEROID 17-ALKYL CARBONATE 21-[O]-CARBOXYLIC AND CARBONIC ESTERS, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICALS CONTAININGTHESE COMPOUNDS

摘要

Corticosteroid 17-alkyl carbonate 21-[O]-carboxylic and carbonic esters, processes for their preparation, and pharmaceuticals containing these compounds Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I (see formula I) are described in which A is CHOH and CHC1, 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, (see 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]n-R(1) 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.