Novel compound having affinity for amyloid

Details Novel compound having affinity for amyloid Novel compound having affinity for amyloid

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 51/00 (2006.01) C07D 487/04 (2006.01) C07F 7/22 (2006.01)

Patent

CA 2653783

Disclosed is a compound having affinity for amyloid, showing fully rapid clearance from a normal tissue, and reduced in toxicities including mutagenicity. Specifically, disclosed is a compound represented by the formula (1) or a salt thereof. Also disclosed is a low-toxic diagnostic agent for Alzheimer's disease, comprising a compound represented by the formula (1) or a salt thereof. (1) wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen; R1 represents a halogen substituent; R2 represents a halogen substituent; and m represents an integer ranging from 0 to 2, provided that at least one of R1 and R2 represents a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to A1, A2, A3 or A4 which represents a carbon.

La présente invention concerne un composé ayant une affinité pour la substance amyloïde, ledit composé présentant une clairance complète rapide dans un tissu normal et ayant peu d'effets toxiques, y compris les effets mutagènes. L'invention concerne spécifiquement un composé représenté par la formule (1) ou un de ses sels. L'invention concerne également un agent peu toxique de diagnostic de la maladie d'Alzheimer, ledit agent comprenant un composé représenté par la formule (1) ou un de ses sels. (1) dans laquelle A1, A2, A3 et A4 représentent indépendamment un carbone ou un azote; R1 représente un substituant halogène; R2 représente un substituant halogène; et m représente un nombre entier allant de 0 à 2, à condition qu'au moins un parmi R1 et R2 représente un substituant halogène radioactif, qu'au moins un parmi A1, A2, A3 et A4 représente un carbone et que R1 se lie au A1, A2, A3 ou A4 qui représente un carbone.

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