Patent · US Active

Immune-stimulating soluble doxorubicin-conjugated complex

US11319341B2 · kind B2 · utility

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7Claims
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Key dates

Filing dateFeb 20, 2020
Grant dateMay 3, 2022
Priority date
Expiry dateFeb 20, 2040

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07K5/1008
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

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 Leu 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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.