Small molecule conjugates specifically activated in tumor microenvironment for targeting and use thereof
US10682371B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 21, 2015 |
| Grant date | Jun 16, 2020 |
| Priority date | — |
| Expiry date | Aug 21, 2035 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P35/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Provided is an anticancer compound including a cleavable linker specifically activated in a tumor microenvironment, and use thereof. The anticancer compound is represented by the following formula, wherein, R1 is a normal functional group or a protection group; R2 is Ala, Thr, Val or Ile; R3 is Ala, Val or Asn; R4 is a drug group linked via a hydroxyl group or an amino group; and the general formula of the drug is R4H. The anticancer compound is only activated at a local portion of a tumor, thus avoiding the defect of immune system damage of a traditional chemotherapeutic drug, and promoting tumor immunization by removing a tumor immunosuppression cell. The anticancer compound or pharmaceutical composition thereof is jointly used with immunotherapy, thus improving the effect of treating the tumor, and effectively inhibiting tumor metastasis and osseous metastasis.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.