发明名称 NOVOS PRO-FARMACOS DE PACLITAXEL METODO PARA A SUA PREPARACAO BEM COMO A SUA UTILIZACAO EM QUIMIOTERAPIA SELECTIVA
摘要 The invention relates to novel, water-soluble paclitaxel prodrugs wherein paclitaxel is, through its 2'-hydroxyl functionality, connected to a cleavable spacer group, which is in turn attached to a preferably enzymatically cleavable sugar group. Such prodrugs are relatively non-toxic and can be used in cancer treatment. They can be selectively activated at the tumor site by the action of endogeneous enzymes or targeted enzymes, or via a non-enzymatic process. The enzyme is preferably beta -glucuronidase, beta -glucosidase or beta -galactosidase. The invention also relates to a process for preparing a pharmaceutical composition containing a paclitaxel prodrug as defined herein, which comprises said prodrug with a pharmaceutically acceptable carrier to provide a solid or liquid formulation for administration.
申请公布号 PT781778(E) 申请公布日期 2002.08.30
申请号 PT19960203571T 申请日期 1996.12.17
申请人 PHARMACHEMIE B.V. 发明人 JOHAN WILHELM SCHEEREN;DICK DE VOS;HENDRICUS BARTHELOMEAS ANDREAS DE BONT;HIDDE JACOB HAISMA;RUBEN GERADUS GEORGE LEENDERS
分类号 C07D305/14;A61K31/335;A61K31/337;A61K31/70;A61K31/7024;A61K38/46;A61K39/395;A61K47/48;A61P35/00;A61P43/00;C07C263/12;C07H13/12;(IPC1-7):C07H13/10;C07C265/12;C07C265/04 主分类号 C07D305/14
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