Novel compound having affinity for amyloid

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 49/04 (2006.01)

Patent

CA 2670436

[PROBLEMS] To provide a compound useful as an amyloid-targeting imaging-diagnostic probe, and also provide a diagnostic agent for Alzheimer's disease comprising the compound. [MEANS FOR SOLVING PROBLEMS] A compound represented by the formula (1) or a salt thereof; and a diagnostic agent for Alzheimer's disease, comprising a compound represented by the formula or a salt thereof. (1) wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen; R1 represents a radioactive halogen substituent; R2 represents a group selected from the group consisting of a hydrogen, a hydroxyl group, a methoxy group, a carboxyl group, an amino group, an N-methylamino group, an N,N-dimethylamino group and a cyano group; and p represents an integer of 0 to 2, provided that at least one of A1, A2, A3 and A4 represents a carbon and R1 binds to the carbon represented by the at least one of A1, A2, A3 and A4.

[PROBLÈMES] obtenir un composé utile comme sonde de diagnostic par imagerie ciblant l'amyloïde et un agent diagnostique de la maladie d'Alzheimer comprenant ledit composé. [SOLUTIONS] un composé représenté par la formule (1) ou un de ses sels; et un agent diagnostique de la maladie d'Alzheimer, comprenant le composé représenté par la formule (1) ou l'un de ses sel. Dans la formule (1) A1, A2, A3 et A4 représentent indépendamment a carbone ou un azote; R1 représente un substituant halogène radioactif; R2 représente un groupe choisi parmi un hydrogène, un groupe hydroxyle, un groupe méthoxy, un groupe carboxyle, un groupe amino, un groupe N-méthylamino, un groupe N, N-diméthylamino et un groupe de cyano; et p représente un entier de 0 à 2, à condition qu'au moins un des A1, A2, A3 et A4 représente un carbone et que R1 se fixe au carbone représenté par le ou les A1, A2, A3 et A4.

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