首页> 外国专利> Method for obtaining conjugate of doxorubicin, trastuzumab and dendrimer PAMAM of 4th generation that has 64 amino groups on its surface and application of doxorubicin, 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 doxorubicin, trastuzumab and dendrimer PAMAM of 4th generation that has 64 amino groups on its surface and application of doxorubicin, 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个氨基的第四代阿霉素,曲妥珠单抗和树枝状聚合物PAMAM的缀合物的方法和表面具有64个氨基的第四代阿霉素,曲妥珠单抗和树枝状聚合物PAMAM的用途用于生产打算用于治疗的药物乳腺癌

摘要

the object of the application is the way to receive doxorubicin conjugate, trastuzumab and dendrymeru pamam generation 4 having surface amino group and 64 application of doxorubicin.trastuzumab and dendrymeru pamam generation 4 having surface amino groups to produce 64 your medicine for therapy of breast cancer.process to obtain a conjugate of doxorubicin and trastuzumab and dendrymeru pamam generation 4 having amino group on the surface 64, is thatin the first stage, part of sulphurous acid cis - akonitowego undergo modification of amino groups of doxorubicin.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 is carried out in pbs 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 tiolową - sh group, using trauta reagent (ethyl 2 - iminotiolanu).the modified dendrymerów pamam accompanied by monoclonal antibody previously sprzęgnięte hyphenated smcc.
机译:本申请的目的是接受具有表面氨基的阿霉素缀合物,曲妥珠单抗和第4代登革热pamam第4代和采用具有表面氨基的阿霉素,曲妥珠单抗和第4代登普瑞pamam第4代产生64种治疗乳腺癌的药物的方法。在表面64上具有氨基的阿霉素与曲妥珠单抗和第4代树突状pamam的共轭物的制备方法是,在第一阶段,在edc存在下,亚硫酸顺式-阿科尼托戈的一部分经历了阿霉素氨基的修饰。在表面dendrymeru结合酰胺键与先前修饰的底物之间形成(乙基n-(3-二甲基氨基)丙基-n'-乙二胺基),反应在室温下以pbs进行。为了连接至dendrymeru trastuzumab pamam,使用衔接子分子n-sukcynoimidylo-4-(nmaleimidometylo)cykloheksylokarboksylan-(smcc)在表面dendrymeru上保持其末端官能团形成反应。除表面dendrymeru外,还使用trauta试剂(乙基2-亚氨基tiolanu)tiolową-sh基团。修饰的dendrymerówpamam结合单克隆抗体,先前通过sprzęgnięte联用了smcc。

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