Hypoxia-selective, weakly basic 2-nitroimidazole delivery...

C - Chemistry – Metallurgy – 07 – F

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C07F 5/02 (2006.01) A61K 51/04 (2006.01) A61P 7/00 (2006.01) A61K 47/48 (2006.01) A61M 36/00 (2006.01)

Patent

CA 2667684

The invention features a class of 2-nitroimidazole compounds with a secondary basic nitrogen atom and a linker bearing one or more therapeutic agents, cytotoxic agents, detectable labels, or chelating groups. In particular, the invention provides 2-nitroimidazole compounds containing a cluster of boron atoms for use in boron neutron capture therapy (BNCT). The 2-nitroimidazole compounds can be used to treat hypoxic conditions, including, e.g., cancer, inflammation, and ischemia. The weakly basic 2-nitroimidazole compounds target to hypoxic tissue and provide increased tissue concentration overall.

L'invention concerne une classe de composés 2-nitroimidazole avec un atome d'azote basique secondaire et un lieur portant un ou plusieurs agents thérapeutiques, agents cytotoxiques, marqueurs détectables ou groupes chélatants. En particulier, l'invention concerne des composés 2-nitroimidazole contenant un agrégat d'atomes de bore à utiliser en boroneutrothérapie (BNCT). Les composés 2-nitroimidazole peuvent être utilisés pour traiter les affections hypoxiques comprenant, par exemple, un cancer, une inflammation et une ischémie. Les composés 2-nitroimidazole faiblement basiques ciblent les tissus hypoxiques et assurent une augmentation globale de la concentration dans les tissus.

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