Novel compound having affinity to amyloid

C - Chemistry – Metallurgy – 07 – D

Patent

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

Patent

CA 2657312

Disclosed is a compound represented by the formula (1) or a salt thereof, which has an affinity to amyloid, shows a satisfactorily rapid clearance from a normal tissue and is reduced in toxicity such as mutagenicity. Also disclosed is a low-toxic diagnostic agent for Alzheimer's disease comprising the compound. (1) [wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen; and R3 represents a group represented by the formula: (wherein R1 represents a radioactive halogen substituent; m represents an integer of 0 to 4; and n represents an integer of 0 or 1) provided that at least one of A1, A2, A3 and A4 represents a carbon and R3 is bound to the carbon A1, A2, A3 or A4].

La présente invention concerne un composé représenté par la formule (1) ou un sel de celui-ci, qui présente une affinité envers un amyloïde, présente une clairance rapide de manière satisfaisante d'un tissu normal et est réduit en termes de toxicité telle que la mutagénicité. La présente invention concerne également un agent diagnostique à faible toxicité pour la maladie d'Alzheimer comprenant le composé. (1) [où A1, A2, A3 et A4 représentent indépendamment un atome de carbone ou d'azote ; et R3 représente un groupe représenté par la formule : (où R1 représente un substituant halogène radioactif ; m représente un nombre entier de 0 à 4 ; et n représente un nombre entier de 0 ou 1) à condition qu'au moins un parmi A1, A2, A3 et A4 représente un atome de carbone et R3 soit lié à l'atome de carbone A1, A2, A3 ou A4].

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