Invention Application
US20050165093A1 Supermolecular carboplatinum derivatives, their preparation and pharmaceutical composition containing tem as active ingredient and applications of the compositions 失效
超分子卡铂衍生物,其制备方法和药物组合物含有作为活性成分的组合物和组合物的应用

Supermolecular carboplatinum derivatives, their preparation and pharmaceutical composition containing tem as active ingredient and applications of the compositions
Abstract:
The present invention relates to a novel class of supermolecular carboplatin derivatives represented by general formula (I), wherein B is a polycarboxylic acid represented by general formula (II), wherein R1, R2 and n are defined as in the description. The present invention also relates to a process for preparing the same, pharmaceutical compositions containing the same as active ingredient and the use of the derivatives in the preparation of pharmaceutical compositions which are useful in treating various cellular cancers including hepatoma, stomach cancer, lung cancer and the like. The derivatives have stable cage-like chemical structures and constitutions in solid and in aqueous solution. The derivatives can not only kill cancer cells at a rate significantly higher than that by carboplatin, in particular, in the case of hepatoma cells, at a rate one to two times higher than that by carboplatin, but also produce little side effects such as vomit, baldness, decreases of leucocytes and platelets, and the like, which can be induced by administration of other chemotherapeutics. In the acute toxicity tests on mice, the lethal dose (LD50) of the present derivatives is about 300 mg/kg and 260 mg/kg body weight for a subcutaneous(sc) and an intraperitoneal(ip) administration, respectively. Therefore, the present derivatives are a novel class of cis-platium which can be widely used as anticancer agents.
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