首页> 外国专利> CORTICOID -17,21-DICARBOXYLIC ESTERS AND CORTICOSTEROID 17-CABOXYLIC ESTERS 21-CARBONIC ESTERS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICALS CONTAINING THESE COMPOUNDS

CORTICOID -17,21-DICARBOXYLIC ESTERS AND CORTICOSTEROID 17-CABOXYLIC ESTERS 21-CARBONIC ESTERS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICALS CONTAINING THESE COMPOUNDS

机译:皮质类固醇-17,21-羧基酯和皮质类固醇17-羧基酯,21-羧基酯,其制备方法和包含这些化合物的药物

摘要

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(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.
机译:皮质类固醇17,21-二羧酸酯和皮质类固醇17-羧酸酯21-碳酸酯,其制备方法和含有这些化合物的药物描述了式I的皮质类固醇17,21-二羧酸酯和皮质类固醇17-羧酸酯21-碳酸酯,其中A是CHOH和CHCl,CH 2,C = O或9(11)双键; Y为H,F或Cl; Z为H,F或甲基; R(1)为芳基或杂芳基; R(2)是烷基,R(3)是H或甲基。它们尤其通过使其中R(S)为OH的式II化合物与式III的活化羧酸R(6)-CO-(O)n(C1​​-C4)反应而获得。 )-烷基] mR(1)III。它们具有非常强的局部和局部抗炎作用,并且表现出非常好的局部与全身抗炎作用比例。它们尤其用作治疗炎性皮肤病的试剂。

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