Novel heteroaryl substituted benzothiazoles

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 417/04 (2006.01) A61K 31/4436 (2006.01) A61K 31/496 (2006.01) A61P 25/28 (2006.01) C07D 417/14 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2640213

The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: ¢Chemical formula should be inserted here. Please see paper copy! and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer's disease therapeutic agents.

La présente invention concerne de nouveaux dérivés de benzothiazole substitués par un hétéroaryle, des précurseurs de ceux-ci et des utilisations thérapeutiques pour des tels composés, lesquels répondent à la formule de structure (I) ci-dessous : [Formule chimique], et des sels acceptables du point de vue pharmaceutique de ceux-ci, des compositions contenant ceux-ci et des procédés d'utilisation de ceux-ci. En outre, l'invention concerne de nouveaux dérivés de benzothiazole substitués par un hétéroaryle qui conviennent pour l'imagerie de dépôts amyloïdes chez des patients vivants, des compositions contenant ceux-ci, des procédés d'utilisation de ceux-ci et des procédés de fabrication de tels composés. Plus précisément, la présente invention concerne un procédé d'imagerie in vivo de dépôts amyloïdes dans le cerveau pour permettre le diagnostic ante mortem de la maladie d'Alzheimer ainsi que la mesure de l'efficacité clinique d'agents thérapeutiques pour la maladie d'Alzheimer.

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