首页> 外国专利> Method for obtaining conjugate of docetaxel, trastuzumab and dendrimer PAMAM of 4th generation that has 64 amino groups on its surface and the application of docetaxel, trastuzumab and dendrimer PAMAM of 4th generation that has 64 amino groups on its surface for production of a drug intended for treatment of breast cancer

Method for obtaining conjugate of docetaxel, trastuzumab and dendrimer PAMAM of 4th generation that has 64 amino groups on its surface and the application of docetaxel, trastuzumab and dendrimer PAMAM of 4th generation that has 64 amino groups on its surface for production of a drug intended for treatment of breast cancer

机译:获得表面具有64个氨基的第四代多西他赛,曲妥珠单抗和树枝状聚合物PAMAM的缀合物的方法以及其表面具有64个氨基的第四代多西他赛,曲妥珠单抗和树枝状聚合物PAMAM的用途用于制备用于乳腺癌的治疗

摘要

the object of the application is the way to receive docetaxel conjugate, trastuzumab and dendrymeru pamam generation 4 having surface 64 amino group and application of docetaxeltrastuzumab and dendrymeru pamam generation 4 having surface amino groups to produce 64 your medicine for therapy of breast cancer.way to receive trastuzumab and docetaxel conjugate, dendrymeru pamam generation 4 having amino group on the surface 64, is thatin the first stage of succinic acid molecules undergo modification of hydroxyl groups of docetaxel.next, in the presence of edc (ethyl n - (3-dimethylamino) propyl - n '- etylokarbodiimidu) is formed between the surface dendrymeru binding amide linkages, with the previously modified substrate.the reaction results in dmso at room temperature.in the later stage of reaction, in order to connect to dendrymeru trastuzumab pamam uses adapter molecule n - sukcynoimidylo - 4 - (nmaleimidometylo) cykloheksylokarboksylan - (smcc) holding onits end functional group forming reaction with both tiolami and amines.in addition to the surface dendrymeru is tiolowu0105 - sh group, using trauta reagent (ethyl 2 - iminotiolanu).the modified dendrymeru00f3w pamam accompanied by monoclonal antibody previously sprzu0119gniu0119te hyphenated smcc.
机译:本申请的目的是接收具有表面64个氨基的多西他赛偶联物,曲妥珠单抗和dendrymeru pamam第4代的方法以及具有表面氨基的多西他赛曲妥珠单抗和dendrymeru pamam第4代产生64个用于乳腺癌治疗的药物的方法。接收曲妥珠单抗和多西他赛缀合物,在表面64上具有氨基的dendrymeru pamam第4代,是在琥珀酸分子的第一阶段中,在edc(乙基n-(3-二甲基氨基)存在下,对多西他赛的羟基进行修饰。在表面dendrymeru结合酰胺键与先前修饰的底物之间形成丙基-n'-etylokarbodiimidu),反应在室温下产生dmso。在反应的后期,为了与dendrymeru trastuzumab pamam连接使用适配器分子n-sukcynoimidylo-4-(nmaleimidometylo)cykloheksylokarboksylan-(smcc)保留其末端官能团形式可以与噻唑胺和胺反应。除表面树枝状化合物外,还可以使用trauta试剂(乙基2-亚氨基tiolanu)来修饰tiolow u0105-sh基团。 。

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