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Camptothecin derivative, polymeric compound combined with HSP90 inhibitor, and use thereof
专利权人:
发明人:
OKAZAKI, MANAMI,冈崎麻奈实,岡崎麻奈實,MARUYAMA, SAKIKO,丸山佐起子,丸山佐起子,MASUDA, AKIRA,增田亮,增田亮,YAMAMOTO, KEIICHIRO,山本启一朗,山本啟一朗
申请号:
TW104105732
公开号:
TW201613652A
申请日:
2015.02.17
申请国别(地区):
TW
年份:
2016
代理人:
摘要:
Provided is a pharmaceutical composition for efficiently delivering two drugs to an affected area, reducing side effects, and increasing drug efficacy. The polymeric compounds have the general formula (1) [wherein, R1 represents a hydrogen atom or a (C1 ~ C4) alkyl group which may have a substituent, t represents an integer of 45 ~ 450, A is (C1 ~ C6) alkylene group and, d + e + f + g + h represents an integer of 6 ~ 60, of d + e + f + g + h, ratio of d is 5-50%, the proportion of e is 5 to 90%, the proportion of f is 0 to 90%, the ratio of g is 0 to 90%, the ratio of h is 0 ~ 90%, R2 is a hydrogen atom or a (C1 ~ C4) acyl group, R3 represents aspartic acid residue bound with HSP90 inhibitor of HSP90 inhibitors, R4 represents an aspartic acid residue or aspartic acid imide residue, R5 represents a -N (R6) CONH (R7), the R6 and R7 represent branched or cyclic (C3 ~ C6 ) alkyl or a branched or straight chain (C1 ~ C5) alkyl group that may be substituted by tertiary amino group.本發明提供一種向患部有效率地傳遞2種藥劑,而減少副作用,且增強藥效之醫藥品。本發明之高分子化合物係以下述通式(1)表示:[式中,R1表示氫原子或可具有取代基之(C1~C4)烷基,t表示45~450之整數,A為(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之比例為5~50%,e之比例為5~90%,f之比例為0~90%,g之比例為0~90%,h之比例為0~90%,R2表示氫原子或(C1~C4)醯基,R3表示HSP90抑制劑或鍵結有HSP90抑制劑之天冬胺酸殘基,R4表示天冬胺酸殘基或天冬胺酸醯亞胺殘基,R5表示-N(R6)CONH(R7),R6、R7表示(C3~C6)支鏈或環狀烷基或者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
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