Nuclear export inhibitors of topoisomerase II alpha
US8623854B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Jun 13, 2011 |
| Grant date | Jan 7, 2014 |
| Priority date | — |
| Expiry date | Jul 30, 2031 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/22
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A method of treating cancer in a subject comprising the step of administering to the subject in need thereof an effective amount of a combination of a compound that binds a nuclear export signal (NES inhibitor) on topoisomerase IIα and a topoisomerase inhibitor. Twenty small molecule inhibitors (SMI) that bind to the two nuclear export sequences (NES) topo IIα have been identified from the NCI database using computer-generated molecular modeling. These SMI will improve the effectiveness of topo II directed therapeutics, particularly in the treatment of diseases such as multiple myeloma (MM). In vitro apoptosis assays indicate that these drugs may be effective as single agents or in combination with currently used cancer drugs that target topo II.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.