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Corticoid 17,21-dicarboxylic esters and cortiscosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds

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

摘要

Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic esters 21-carbonic esters of the formula I IMAGE with A equal to CHOH and CHClm CH2, C=0, 9(11) double bond; Y equal to H, F, Cl; Z equal to H, F, methyl, R(1) equal to aryl, hetaryl; R(2) equal to alkyl, R(3) equal to H, methyl are described. They are obtained, inter alia, by reacting a compound of the formula II IMAGE in which R(5) is equal to OH, with an activated carboxylic acid of the formula III IMAGE They have very high local and topical antiinflammatory activity and show a very good ratio of local to systemic antiinflammatory effect. They are used inter alia as agents for treating inflammatory dermatoses.
机译:具有A等于CHOH和CH 2,C = 0、9(11)双键的式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; Y等于H,F,Cl; Z等于H,F,甲基,R(1)等于芳基,杂芳基;描述了等于烷基的R(2),等于H的R(3),甲基。它们尤其是通过使其中R(5)等于OH的式II 的化合物与式III 的活化的羧酸反应而获得。它们具有非常高的局部和局部抗炎活性并显示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药剂。

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