Bioreductive agents

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 471/14 (2006.01)

Patent

CA 2092617

ABSTRACT NOVEL BIOREDUCTIVE AGENTS Quinoxaline or pyrido pyrazine derivatives of formula (I) Image (I) wherein R' is: hydrogen, alkyl, alkylamino, dialkylamino, aminoalkylamino unsubstituted or substituted on the terminal amino group by one or two alkyl groups, aminoalkyl(N- alkyl)amino unsubstituted or substituted on the terminal amino group by one or two alkyl groups, hydroxyalkylamino, hydroxyalkyl(N-alkyl)amino, haloalkylamino, haloalkyl(N- alkyl)amino; a heterocyclic group which is a 1-pyrrolidino, 1- piperidino, 1-morpholino group, unsubstituted or substituted by one or more alkyl, hydroxy or halogen substituents, or an aziridino group unsubstituted or substituted by one or more or alkyl substituents; or a 1-piperazino group which is unsubstituted or substituted by one or more alkyl, hydroxy or halogen substituents in the 2- or 3- position and in the 4-position is unsubstituted or N-substituted by haloalkyl, cycloalkyl of 5 to 7 carbon atoms (unsubstituted or substituted by one or more alkyl, hydroxy or halogen substituents), or pyridyl (unsubstituted or substituted by one or more alkyl, haloalkyl, hydroxy, alkoxy, nitro or halogen substituents) or phenyl (unsubstituted or substituted by one or more alkyl, haloalkyl, hydroxy, alkoxy, nitro or halogen substituents), R' is a hydrocarbyl or heterocyolyl aromatic group unsubstituted or substituted by one or more substituents selected from halogen haloalkyl, alkyl, nitro, hydroxy, alkoxy and alkylenedioxy; X is -CH- or -N-; and X' is hydrogen or halogen; wherein the said alkyl groups and moieties incorporating alkyl groups contain form 1 to 6 carbon atoms and the said haloalkyl groups contain one or more halogen atoms: and pharmaceutically acceptable salts thereof are useful in the treatment of tumours, and in particular hypoxic tumours. Processes for producing the compounds and pharmaceutical compositions comprising them. Pharmaceutically acceptable salts of 1,2-dihydro-?- *piperazinyl-4-phenylimidazo pyridopyrazine oxides and 1,2- dihydro-8-piperazinyl-4-phenylimidazo quinoxaline oxides and 4-pyrido also are useful in the treatment of cancer and in particular in the treatment of hypoxic tumours. Processes for their preparation and pharmaceutical compositions containing them.

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