- 专利标题: Legumain activated doxorubicin derivative as well as preparation method and application thereof
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申请号: US14655869申请日: 2013-12-23
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公开(公告)号: US09982011B2公开(公告)日: 2018-05-29
- 发明人: Cheng Liu , Yuan Liu
- 申请人: Yafei (Shanghai) Biopharmaceutical Co., Ltd.
- 申请人地址: CN Shanghai
- 专利权人: Yafei (Shanghai) Biopharmaceutical Co., Ltd.
- 当前专利权人: Yafei (Shanghai) Biopharmaceutical Co., Ltd.
- 当前专利权人地址: CN Shanghai
- 代理机构: Lewis Kohn & Walker LLP
- 代理商 David M. Kohn; Kari Moyer-Henry
- 优先权: CN201210573744 20121226
- 国际申请: PCT/CN2013/001620 WO 20131223
- 主分类号: C07K1/107
- IPC分类号: C07K1/107 ; C07K5/103 ; C07K19/00 ; C07H15/26 ; C07H15/252 ; A61K31/704 ; A61K47/65 ; A61K47/54
摘要:
The present invention discloses doxorubicin derivatives for targeted activation by Legumain, its preparation method and use. The doxorubicin derivatives are obtained by condensation between the amino group of compound A and the carboxyl group of compound B and have the following structure: compounds A and B have the following structures, respectively: wherein R3 in compound B is Len or absent; R4 is any one amino acid selected from the group consisting of Ala and Thr; R5 is any one amino acid selected from the group consisting of Ala, Thr and Asn; R6 is wherein n=1-20; or wherein R7 is substituted or unsubstituted, linear or branched, saturated or unsaturated C1-C20 fatty hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon. The doxorubicin derivatives of the present invention are specifically tumor-targeted and have a long in vivo metabolic half-life, as compared with doxorubicin. They exhibit an efficient and safe anti-tumor effect and could be used to prepare an anti-tumor drug.