Nitroaniline derivatives and their use as anti-tumour agents
US5750782A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jul 23, 1996 |
| Grant date | May 12, 1998 |
| Priority date | — |
| Expiry date | Jul 23, 2016 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C237/34
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention provides nitroaniline derivatives represented by general formula (1) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN,COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents. ##STR1##
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.