新規アミロイド親和性化合物の使用及び製造方法

Utilisation de nouveaux composés à affinité pour les substances amyloïdes et leur procédé de production

Utilization of novel compounds with amyloid affinity and method of producing the same

Abstract

It is intended to provide a reagent for detecting amyloids in a biological tissue by which amyloids can be detected in vitro and in vivo at a high sensitivity using a compound having amyloid affinity and having been regulated in toxicity such as mutagenicity. A reagent for detecting amyloids deposited in a biological tissue which comprises a compound represented by the following general formula (1) or its salt. (1) wherein A1, A2, A3 and A4 each independently represents carbon or nitrogen; R1 represents a radioactive halogen substituent; R2 represents a group selected from the group consisting of hydrogen, hydroxyl, methoxy, carboxyl, amino, N-methylamino, N,N-dimethylamino and cyano; and m is an integer of 0 to 2; provided that at least one of A1, A2, A3 and A4 is hydrogen and R1 is bonded to A1, A2, A3 or A4 that is carbon.
アミロイドへの親和性を有し、かつ、変異原性等の毒性がおさえられた化合物を用いて、インビトロ(in vitro)及びインビボ(in vivo)でアミロイドを高感度に検出し得る、生体組織中のアミロイドの検出試薬を提供する。 下記式(1)で表される化合物またはその塩を含有してなる、生体組織に沈着したアミロイドの検出試薬。 (式中、A1、A2、A3及びA4はそれぞれ独立に炭素又は窒素、R1は放射性ハロゲン置換基、R2は水素、水酸基、メトキシ基、カルボキシル基、アミノ基、N−メチルアミノ基、N,N−ジメチルアミノ基及びシアノ 基からなる群より選ばれる基、mは0~2の整数である。ただし、A1、A2、A3及びA4のうちの少なくと も一つは炭素であって、R1は、炭素であるA1、A2、A3及びA4に結合する。)
L'invention concerne l'utilisation d'un réactif pour la détection de substances amyloïdes dans un tissu biologique, les substances amyloïdes pouvant être détectées in vitro et in vivo avec une sensibilité élevée à l'aide d'un composé présentant une affinité pour les substances amyloïdes et dont la toxicité a été régulée, notamment la mutagénicité. L'invention concerne un réactif permettant de détecter des substances amyloïdes déposées dans un tissu biologique, ledit réactif comprenant un composé représenté par la formule générale suivante (1) ou un sel dudit composé. Dans la formule (1), A1, A2, A3 et A4 représentent chacun indépendamment du carbone ou de l'azote; R1 représente un substituant halogène radioactif; R2 représente un groupe sélectionné dans le groupe constitué par hydrogène, hydroxyle, méthoxy, carboxyle, amino, N-méthylamino, N,N-diméthylamino et cyano; et m représente un entier compris entre 0 et 2; à condition qu'au moins un élément sélectionné parmi A1, A2, A3 et A4 représente hydrogène et que R1 soit lié à A1, A2, A3 ou A4 qui représente du carbone.

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