Novel compound having affinity for amyloid

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 471/04 (2006.01) A61K 51/00 (2006.01) G01T 1/161 (2006.01)

Patent

CA 2655826

Disclosed is a compound having affinity for amyloid and satisfactorily rapid clearance from a normal tissue and reduced in toxicity including mutagenicity. Specifically disclosed are: a compound represented by the formula (1) and a salt thereof; and a low-toxic diagnostic agent for Alzheimer's disease comprising the compound or the salt thereof. (1) wherein R1 represents a group selected from a hydrogen, a hydroxyl group, a carboxyl group, a sulfate group, an amino group, a nitro group, a cyano group, an alkyl substituent group having 1 to 4 carbon atoms and an alkoxy substituent group having 1 to 4 carbon atoms; R2 represents a radioactive halogen substituent group; and m represents an integer ranging from 0 to 2.

L'invention concerne un composé qui présente une affinité pour une substance amyloïde, une clairance d'un tissu normal de rapidité satisfaisante, ainsi qu'une toxicité réduite, notamment une faible mutagénicité. Cette invention concerne de manière spécifique : un composé représenté par la formule (1), et un sel de ce composé; ainsi qu'un agent de diagnostic de faible toxicité de la maladie d'Alzheimer, qui comporte ledit composé ou le sel de ce composé. Dans la formule (1), R1 représente un groupe sélectionné parmi hydrogène, un groupe hydroxyle, un groupe carboxyle, un groupe sulfate, un groupe amino, un groupe nitro, un groupe cyano, un groupe substituant alkyle comportant 1 à 4 atomes de carbone et un groupe substituant alcoxy comportant 1 à 4 atomes de carbone; R2 désigne un groupe substituant halogène radioactif; et m représente un nombre entier compris entre 0 et 2.

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