PFKFB3 inhibit and methods of use as an anti-cancer therapeutic
US10010542B2 · kind B2 · utility
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11Claims
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Key dates
| Filing date | May 9, 2017 |
| Grant date | Jul 3, 2018 |
| Priority date | — |
| Expiry date | May 9, 2037 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D401/06
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A novel compound, (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one, is provided herein. (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) with surprisingly superior efficacy and pharmacodynamic properties in vitro and in vivo. Also provided are pharmaceutical compositions including the compound and methods of use of the compound in treating cancer and tumors in vivo, as well as inhibiting glycolytic flux and PFKFB3 enzymatic activity in cells.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.