Novel substituted azabenzoxazoles

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 498/04 (2006.01) A61K 31/4353 (2006.01) A61P 25/28 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2725940

The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds. or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH;

Nouveaux composés se liant aux amyloïdes et méthodes de mesure de leurs effets consistant à mesurer des changements de niveau des plaques amyloïdes chez des patients vivants. Plus précisément, méthode d'utilisation desdits composés comme traceurs dans le cadre d'une tomographie par émission de positions visant à étudier des dépôts d'amyloïdes dans le cerveau in vivo pour le diagnostic de la maladie d'Alzheimer. Ainsi, cette invention concerne l'utilisation des nouveaux composés qui se lient aux amyloïdes comme outil de diagnostic. De plus, l'invention concerne une méthode de mesure de l'efficacité clinique d'agents thérapeutiques de la maladie d'Alzheimer. Spécifiquement, l'invention porte sur des nouveau dérivés d'azabenzoxazole substitués aryle ou hétéroaryle, des compositions et des utilisations thérapeutiques ainsi que des méthodes de fabrication de tels composés.

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