首页> 外国专利> 10-deacetylbaccatine III and 10-deacetyl 14beta -hydroxybaccatine III derivatives, a process for the preparation thereof and pharmaceutical compositions containing them

10-deacetylbaccatine III and 10-deacetyl 14beta -hydroxybaccatine III derivatives, a process for the preparation thereof and pharmaceutical compositions containing them

机译:10-脱乙酰基卡卡汀III和10-脱乙酰基14β-羟基巴卡汀III衍生物,其制备方法和含有它们的药物组合物

摘要

The present invention relates to novel derivatives of 10-deacetylbaccatine III and of 10-deacetyl-14 beta -hydroxybaccatine III, having cytoxic and anti-tumoral activity. They are prepared starting from the so-called syntons or from other taxanes of natural origin, by selective oxidation of the hydroxyl in position 10 to keto function and subsequent esterification in position 13, if necessary, with isoserine chains variously substituted. The products of the invention can be administered by injection or orally, when suitably formulated.
机译:本发明涉及具有细胞毒性和抗肿瘤活性的10-去乙酰基卡卡汀III和10-去乙酰基14β-羟基卡卡汀III的新型衍生物。它们是从所谓的合成子或天然来源的其他紫杉烷类开始制备的,方法是将10位的羟基选择性氧化成酮官能团,然后在13位进行酯化反应(必要时用异丝氨酸链取代)。当适当地配制时,本发明的产品可以通过注射或口服给药。

著录项

  • 公开/公告号AU705923B2

    专利类型

  • 公开/公告日1999-06-03

    原文格式PDF

  • 申请/专利权人 INDENA S.P.A.;

    申请/专利号AU19960048320

  • 申请日1996-03-04

  • 分类号C07D305/14;C07F7/18;C07D493/10;C07D263/04;A61K31/335;

  • 国家 AU

  • 入库时间 2022-08-22 02:22:49

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