Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
US10087175B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 1, 2015 |
| Grant date | Oct 2, 2018 |
| Priority date | — |
| Expiry date | Apr 1, 2035 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D471/08
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described. At least one described molecular species exhibits an IC50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo, and led to 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.