Sigma-1 receptor ligand with acetylcholinesterase inhibition...

A - Human Necessities – 61 – K

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A61K 31/56 (2006.01)

Patent

CA 2534777

A novel compound and method for preventing or treating neurodegenerative diseases by inhibiting acetylcholinesterase and binding the sigma-1 receptor are disclosed. Dimethylcarbamic acid 2,3-bis-dimethylcarbamoyloxy-6-[4-(4- ethyl-piperazin-yl)-butyryl]-phenyl ester and its derivatives represent a novel therapeutic strategy against .beta.-amyloid peptide induced neurotoxicity, in inhibiting acetylcholinesterase, in improving cholinergic transmission, in binding the sigma-l receptor, and in releasing a metabolite that is active both as a sigma-1 receptor ligand and an antioxidant.

L'invention concerne un nouveau composé et une nouvelle méthode permettant de prévenir ou de traiter des maladies neurodégénératives par inhibition de l'acétylcholinestérase et liaison du récepteur sigma-1. L'ester 2,3-bis-diméthylcarbamoyloxy-6-[4-(4-éthyl-piperazin-yl)-butyryl]-phényl d'acide diméthylcarbamique et ses dérivés représentent une nouvelle stratégie thérapeutique contre la neurotoxicité induite par le peptide amyloïde bêta, pour inhiber l'acétylcholinestérase, améliorer la transmission cholinergique, lier le récepteur sigma-1, et lilbérer un métabolite qui est actif à la fois en tant que récepteur sigma-1 et en tant qu'anti-oxydant.

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