发明名称 |
NOVEL PACLITAXEL PRODRUGS, METHOD FOR PREPARATION AS WELL ASTHEIR USE IN SELECTIVE CHEMOTHERAPY |
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 |
CA2192424(C) |
申请公布日期 |
2002.01.22 |
申请号 |
CA19962192424 |
申请日期 |
1996.12.09 |
申请人 |
|
发明人 |
DE BONT, HENDRICUS BARTHELOMEAS ANDREAS;LEENDERS, RUBEN GERARDUS GEORGE;SCHEEREN, JOHAN WILHELM;HAISMA, HIDDE JACOB;DE VOS, DICK |
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):C07H13/12;C12N9/96 |
主分类号 |
C07D305/14 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|