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sugar chemical compound-taxane compound A pharmaceutical composition for preventing or treating cancer comprising sugar chemical compound-taxane compound conjugate and a method for preparation thereof

机译:糖类化合物-紫杉烷类化合物一种用于预防或治疗癌症的药物组合物,其包含糖类化合物-紫杉烷类化合物缀合物及其制备方法

摘要

The present invention relates to a pharmaceutical composition for preventing or treating cancer comprising, as an active ingredient, a drug conjugate of a taxane compound having a carboxy group and a sugar compound having a hydroxy group, Reacting a taxane compound having a hydroxyl group with a sugar compound having a carboxyl group in the presence of 4-dimethylaminopyridine and N, N'-dicyclohexylcarbodiimide, , A method for producing a drug conjugate, and a carboxymethyl dextran-docetaxel polymer conjugate represented by Chemical Formula (1).The drug conjugate of the present invention is capable of releasing a taxane compound by hydrolysis of an ester bond in the conjugate in a mildly acidic environment in a cancer microenvironment. Since no enzymes are required in the above process, it can be used effectively as a cancer treatment agent which minimizes side effects by selectively releasing taxane compounds at cancer lesion sites which are not normal tissues.;
机译:本发明涉及用于预防或治疗癌症的药物组合物,其包含作为活性成分的具有羧基的紫杉烷化合物和具有羟基的糖化合物的药物缀合物,使具有羟基的紫杉烷化合物与药学上可接受的化合物反应。在4-二甲基氨基吡啶和N,N'-二环己基碳二亚胺存在下的具有羧基的糖化合物,制备药物缀合物的方法,以及化学式(1)表示的羧甲基葡聚糖-多西他赛聚合物缀合物。本发明能够在癌症微环境中在弱酸性环境中通过缀合物中酯键的水解来释放紫杉烷化合物。由于在上述过程中不需要酶,因此它可以有效地用作通过在非正常组织的癌病灶部位选择性释放紫杉烷类化合物而使副作用最小化的癌症治疗剂。

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