Nitro-imidazole hypoxia imaging agents

Details Nitro-imidazole hypoxia imaging agents Nitro-imidazole hypoxia imaging agents

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) A61K 31/4192 (2006.01) C07B 59/00 (2006.01) C07D 403/12 (2006.01)

Patent

CA 2683433

The present invention relates to novel radioactively labeled bioreducible tracers of Formula (I) useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.

Cette invention concerne des nouveaux traceurs bioréductibles à marquage radioactif représentés par la formule I et utilisés pour détecter des tumeurs hypoxiques ou un tissus ischémique in vivo. Dans un mode de réalisation, les traceurs consistent en un groupement fonctionnel 2-nitroimidazole, un triazole, un liant métaboliquement stable avec des substituants renforçant la pharmacocinétique, et un radioisotope. Le procédé d'imagerie in vivo privilégié dans cette invention est la tomographie par émission de positrons.

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