Novel heteroaryl substituted benzoxazoles

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 413/04 (2006.01) A61K 31/4439 (2006.01) A61K 31/506 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2655084

The present invention relates to novel heteroaryl substituted benzoxazole derivatives and therapeutic uses for such compounds, having the structural formula (Ia) 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 benzoxazole 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 benzoxazole substitués par hétéroaryle. Elle concerne l'utilisation à des fins thérapeutiques de ces composés de formule de structure (Ia), leur sel pharmaceutiquement acceptable, des compositions et des méthodes d'emploi. L'invention concerne également de nouveaux dérivés de benzoxazole substitués par hétéroaryle, qui sont appropriés pour la représentation de dépôts amyloïdes chez des patients vivants, leurs compositions, des méthodes d'utilisation et des procédés de production desdits composés. L'invention concerne plus particulièrement une méthode de représentation in vivo de dépôts amyloïdes dans le cerveau, qui permet de poser un diagnostic antemortem de la maladie d'Alzheimer, ainsi que de mesurer l'efficacité clinique de substances thérapeutiques contre la maladie d'Alzheimer.

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