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結合有喜樹鹼類及抗癌效果增強劑之高分子化合物及其用途
专利权人:
NIPPON KAYAKU KABUSHIKI KAISHA
发明人:
YAMAMOTO, KEIICHIRO,山本啓一朗,OKAZAKI, MANAMI,冈崎麻奈实,岡崎麻奈實
申请号:
TW102140567
公开号:
TW201427693A
申请日:
2013.11.07
申请国别(地区):
TW
年份:
2014
代理人:
摘要:
An object of the present invention is to provide a high molecular compound combining camptothecin and antitumor effect potentiator, especially PARP inhibitor, in the same molecular, and the high molecular compound has lower toxicity to the normal cell and can effectively convey and release the two agents to an affected area, so as to increase the therapeutic effect thereof. The high molecular compound is represented by the following formula (1). (In the formula, R1 represents (C1-C4) alkyl with substituent; t represents an integer from 45 to 450; A represents (C1-C6) alkylene; d+e+f+g+h represents an integer from 6 to 60; compared to d+e+f+g+h, d is 5 to 50%, e is 5 to 90%, f is 0 to 90%, g is 0 to 90%, and h is 0 to 90%; R2 represents hydrogen atom or (C1-C4) acyl; R3 represents antitumor effect potentiator residue or aspartic acid residue combined with antitumor effect potentiator; R4 represents aspartic acid residue and/or asparagine residues amine imide; and R5 represents N(R6)CONH(R7), where R6 and R7 can be identical or different and represent (C3-C6) branched or cyclic alkyl or (C1-C5) branched or straight chain alkyl capable of being replaced by three amino).本發明之目的在於提供一種於同一分子中結合有喜樹鹼類及抗癌效果增強劑,尤其是PARP抑制劑之高分子化合物,以及因此對正常細胞毒性較低,並且有效地向患部傳達並釋放二劑,藉此引起藥效之提高。提供一種下述通式(1)所表示之高分子化合物。[式中,R1表示亦可具有取代基之(C1-C4)烷基,t表示45-450之整數,A表示(C1-C6)伸烷基,d+e+f+g+h表示6-60之整數,相對於d+e+f+g+h,d之比率為5-50%,e之比率為5-90%,f之比率為0-90%,g之比率為0-90%,h之比率為0-90%,R2表示氫原子或(C1-C4)醯基,R3表示抗癌效果增強劑殘基或結合有抗癌效果增強劑之天冬胺酸殘基,R4表示天冬胺酸殘基及/或天冬胺醯亞胺殘基,R5表示N(R6)CONH(R7),R6、R7可相同,亦可不同,表示(C3-C6)支鏈或環狀烷基或者亦可經三級胺基取代之(C1-C5)支鏈或直鏈烷基]。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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