Nitrophenylaziridine compounds and their use as prodrugs
US6517836B1 · kind B1 · utility
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Key dates
| Filing date | Mar 6, 2001 |
| Grant date | Feb 11, 2003 |
| Priority date | — |
| Expiry date | Mar 6, 2021 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D249/08
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A range of aziridin-1-yl nitrobenzamides are provided for use as prodrugs in conjunction with nitroreductase (NR) enzymes. The amides may have 1 or 2-substituents which may be bulky and polar. For example, 5-(aziridin-1-yl)-N-[2-(4-morpholino)ethyl]-2,4-dinitrobenzamide of Formula (A) was found to be highly active against all NR+ cell lines tested.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.