CORTICOID-17,21-DICARBOXYLIC ESTERS AND CORTICOSTEROID 17-CARBOXYLIC ESTER 21-CARBONIC ESTERS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICALS CONTAINING THESE COMPOUNDS
申请人:——
公开号:US20020103392A1
公开(公告)日:2002-08-01
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
1
are described, in which A is CHOH and CHCl, CH
2
, 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,
2
in which R(5) is OH, with an activated carboxylic acid of the formula III,
R(6)—CO—(O)
n
[(C
1
-C
4
)-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.
糖皮质激素17,21-二羧酸酯和糖皮质激素17-羧酸酯21-羧酸酯的制备方法和含有这些化合物的药物被描述。其中化学式I1中,A为CHOH和CHCl,CH2,C═O或9(11)双键;Y为H,F或Cl;Z为H,F或甲基;R(1)为芳基或杂环基;R(2)为烷基,R(3)为H或甲基。它们可以通过将化学式II中R(5)为OH的化合物与化学式III中的活化羧酸反应而获得。它们具有非常强的局部和局部抗炎作用,并表现出很好的局部和全身抗炎效应比。它们被用于治疗炎症性皮肤病等。