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Tamoxifen derivatives for treatment of neoplastic diseases, especially with high HER2 protein level

机译:他莫昔芬衍生物,用于治疗肿瘤疾病,尤其是HER2蛋白水平高的

摘要

The invention relates to new mitochondrially targeted E/Z isomers of aliphatic triphenylphosphonium derivatives of tamoxifen, where the aliphatic chain is alkyl or alkenyl, and their corresponding tertiary amine salts and/or their mixtures (MitoTAX). Alkyl triphenylphosphonium derivatives of tamoxifen have the general formula (I):I,where n=8…12 and Z is selected from the group of organic or inorganic salts. Alkenyl triphenylphosphonium derivatives of tamoxifen have the general formula IA:IAwhere n=6…10 and Z has the above mentioned meaning.These compounds are applicable for the treatment of neoplastic diseases, especially those with high HER2 protein levels. The drug for the treatment of neoplastic diseases, according to the invention, contains at least one E/Z isomer of aliphatic triphenylphosphonium derivatives of tamoxifen of the general formula (I) and/or IA or their corresponding tertiary amine salts.
机译:本发明涉及他莫昔芬的脂族三苯基phosph衍生物的新的线粒体靶向的E / Z异构体,其中脂族链为烷基或烯基,及其相应的叔胺盐和/或它们的混合物(MitoTAX)。他莫昔芬的烷基三苯基phosph衍生物具有通式(I):I,其中n = 8…12,Z选自有机或无机盐。他莫昔芬的烯基三苯基phosph衍生物的通式为IA:IA,其中n = 6…10,Z具有上述含义。这些化合物可用于治疗肿瘤性疾病,尤其是HER2蛋白水平高的那些。根据本发明的用于治疗赘生性疾病的药物包含通式(I)的他莫昔芬的脂族三苯基derivatives衍生物和/或IA的至少一种E / Z异构体或其相应的叔胺盐。

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