Novel compounds with affinity for amyloid

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 51/00 (2006.01)

Patent

CA 2669522

[PROBLEMS] To obtain a compound which is effective as an image diagnosis probe targeting amyloid and a diagnostic for Alzheimer's disease comprising this compound. [MEANS FOR SOLVING PROBLEMS] A compound represented by the following formula (1) or its salt: wherein A1, A2, A3 and A4 independently represent each carbon or nitrogen; R1 represents hydrogen or a group selected from the group consisting of a hydroxyl group, a carboxyl group, a sulfate group, an amino group, a nitro group, a cyano group, a non-radioactive halogen substitute, a C1-4 alkyl substituent and a C1-4 alkoxy substituent; and R2 represents a radioactive halogen substituent, provided that at least one of A1, A2, A3 and A4 is carbon and R1 attaches to A1, A2, A3 or A4 that is carbon; and a diagnostic for Alzheimer's disease comprising the compound represented by the above formula or its salt.

La présente invention a pour objet l'obtention d'un composé efficace en tant que sonde de diagnostic d'imagerie ciblant la substance amyloïde et le diagnostic de la maladie d'Alzheimer au moyen dudit composé. La présente invention concerne un composé représenté par la formule suivante (1) ou son sel, où A1, A2, A3 et A4 représentent indépendamment l'un de l'autre un atome de carbone ou un atome d'azote ; R1 représente un atome d'hydrogène ou un groupe choisi dans le groupe constitué d'un groupe hydroxyle, d'un groupe carboxyle, d'un groupe sulfate, d'un groupe amino, d'un groupe nitro, d'un groupecyano, d'un substitut halogéné non radioactif, d'un substituant alkyle en C1-C4 et d'un substituant alcoxy en C1-C4 ; et R2 représente un substituant halogéné radioactif, sous réserve qu'au moins un composé parmi A1, A2, A3 et A4 représente un atome de carbone et que R1 se fixe au composé A1, A2, A3 ou A4 qui représente un atome de carbone ; et un procédé de diagnostic de la maladie d'Alzheimer impliquant le composé, représenté par la formule ci-dessus, ou son sel.

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