Patent · US Expired

Nitroaniline derivatives and their use as anti-tumour agents

US5571845A · kind A · utility

2Cited by
0References
9Claims
0Family size

Assignee

Inventors

Key dates

Filing dateMay 26, 1994
Grant dateNov 5, 1996
Priority date
Expiry dateMay 26, 2014

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D295/13
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The invention provides nitroaniline derivatives represented by general formula (I) 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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.