Indole derivatives

Details Indole derivatives Indole derivatives

C - Chemistry, Metallurgy

07

D

C07D 209/80 (2006.01) A61K 51/04 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2756887

An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also in-cludes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthe-sis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provid-ed is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceuti-cal composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.

La présente invention concerne un agent d'imagerie in vivo à base d'indole, qui se lie avec une affinité élevée au PBR, et présente une bonne absorption dans le cerveau après son administration, ainsi qu'une bonne liaison sélective au PBR. Ladite invention porte également sur un composant précurseur utile dans la synthèse de l'agent d'imagerie in vivo de l'invention, ainsi que sur un procédé de synthèse dudit agent d'imagerie in vivo, comprenant l'utilisation dudit composé précurseur. L'invention concerne en outre un kit destiné à réaliser ledit procédé. Par ailleurs, l'invention a trait à une cassette destinée à la synthèse automatisée dudit agent d'imagerie in vivo. En outre, certains aspects de l'invention portent sur une composition radiopharmaceutique comprenant ledit agent d'imagerie in vivo de l'invention, et sur des procédés d'utilisation dudit agent d'imagerie in vivo.

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