首页> 外国专利> paclitaxel prodrogen, method for the production and their use for the selective chemotherapy

paclitaxel prodrogen, method for the production and their use for the selective chemotherapy

机译:紫杉醇前驱素,制备方法及其在选择性化疗中的应用

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.
机译:本发明涉及新颖的水溶性紫杉醇前药,其中紫杉醇通过其2'-羟基官能团与可裂解的间隔基团相连,该间隔基团又与优选的可酶裂解的糖基团相连。此类前药相对无毒,可用于癌症治疗。它们可通过内源酶或靶向酶的作用,或通过非酶促过程在肿瘤部位被选择性激活。该酶优选是β-葡糖醛酸糖苷酶,β-葡糖苷酶或β-半乳糖苷酶。本发明还涉及制备包含如本文所定义的紫杉醇前药的药物组合物的方法,所述药物组合物包含所述前药和药学上可接受的载体以提供用于给药的固体或液体制剂。

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号