发明名称 CORTICOID-17,21-DICARBOXYLIC ESTERS AND CORTICOSTEROID 17-CARBOXYLIC ESTER 21-CARBONIC ESTERS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICALS CONTAINING THESE COMPOUNDS
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(5) is OH, with an activated carboxylic acid of the formula III, <paragraph lvl="0"><in-line-formula>R(6)-CO-(O)n[(C1-C4)-alkyl]m-R(1) III.</in-line-formula>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.
申请公布号 US2002103392(A1) 申请公布日期 2002.08.01
申请号 US19970897455 申请日期 1997.07.22
申请人 STACHE ULRICH;ALPERMANN HANS-GEORG;DURCKHEIMER WALTER;BOHN MANFRED 发明人 STACHE ULRICH;ALPERMANN HANS-GEORG;DURCKHEIMER WALTER;BOHN MANFRED
分类号 A61K31/57;A61K31/56;A61K31/573;A61K31/58;A61P17/00;A61P29/00;C07J5/00;C07J17/00;C07J31/00;C07J33/00;C07J41/00;C07J43/00;C07J75/00;(IPC1-7):C07J53/00;C07J7/00;A61K31/585 主分类号 A61K31/57
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