Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents
US5691371A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 27, 1995 |
| Grant date | Nov 25, 1997 |
| Priority date | — |
| Expiry date | Sep 27, 2015 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D233/95
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Nitrobenzyl mustard quaternary salts of formula (I), ##STR1## and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.2 -- or CR.sub.1 .dbd.CR.sub.2-- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionaly substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or other groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH.dbd.replaced by --N.dbd.); with the proviso that when H-Cl or Br, Q=Me, and X=CH.sub.2 -- then Ar.noteq.2-nitrophenyl or 4-nitrophenyl.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.