C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/04 (2006.01) A61K 31/443 (2006.01) A61K 31/4436 (2006.01) A61K 31/501 (2006.01) C07D 409/04 (2006.01) C07D 471/04 (2006.01)
Patent
CA 2680157
The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran 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.
L'invention concerne de nouveaux dérivés de benzothiophène et de benzofurane à substitution 2-hétéroaryle, leurs précurseurs, et les utilisations thérapeutiques de tels composés, ayant la formule structurelle (Ia) : et leur sel pharmaceutiquement acceptable, leurs compositions et leurs procédés d'utilisation. L'invention concerne en outre de nouveaux dérivés de benzothiophène et de benzofurane à substitution 2-hétéroaryle convenant pour une imagerie de dépôts amyloïdes chez des patients vivants, leurs compositions, et les procédés d'utilisation et de fabrication de tels composés. L'invention concerne plus spécifiquement un procédé d'imagerie de dépôts amyloïdes dans un cerveau in vivo, pour permettre un diagnostic ante mortem de la maladie d'Alzheimer, tout comme une mesure de l'efficacité clinique d'agents thérapeutiques contre la maladie d'Alzheimer.
Arzel Erwan
Swahn Britt-Marie
Wensbo David
Astrazeneca Ab
Fetherstonhaugh & Co.
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