Legumain activated doxorubicin derivative as well as preparation method and application thereof
US9982011B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 23, 2013 |
| Grant date | May 29, 2018 |
| Priority date | — |
| Expiry date | Mar 20, 2034 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/1008
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
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 iswherein n=1-20; orwherein 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.