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    • 6. 发明专利
    • Metal chelate of macrocyclic substituted polyaminocarboxylic acid and use thereof in diagnostic imaging
    • 大环取代的聚氨基甲酸的金属螯合物及其在诊断成像中的应用
    • JPH11279163A
    • 1999-10-12
    • JP37782298
    • 1998-12-10
    • Guerbet Saゲールベ
    • MEYER DOMINIQUEPORT MARCROUSSEAUX OLIVIERSIMONOT CHRISTIAN
    • A61K49/00A61K49/04A61K49/08C07D257/02C07F5/00
    • C07D257/02A61K49/085A61K49/106Y10S514/836
    • PROBLEM TO BE SOLVED: To obtain a chelate (an organic salt or an inorganic salt) to be a contrast medium for diagnostic magnetic resonance imaging by inclusion thereof in a medium by forming the chelate from a paramagnetic metal cation and a specific compound. SOLUTION: A chelate is formed from (A) a paramagnetic metal cation and (B) a compound represented by formula I [(m) is 1 or 2; R' is H, a 1-4C alkyl or a hyroxyalkyl; R is represented by formula II [(a) is 1 or 2; Z is a single bond, CH2 or the like; Z' is a single bond, O, S, CH2 , CO, NQ (Q is H, a 1-4C alkyl or the like) or the like; Z" is CO-NQ, NQ-CO or the like; R1 to R5 are each H, Br, Cl, I or the like, with the proviso that one or more and two or below of R1 to R5 are each an amide] to afford a chelate (an organic salt or an inorganic salt). The chelate is obtained by reacting a chelate of a metal cation M with a compound represented by formula III with an amine represented by formula IV in the presence of a coupling agent especially the one used when synthesizing a peptide.
    • 要解决的问题:通过从顺磁性金属阳离子和特定化合物形成螯合物,将其作为用于诊断磁共振成像的造影剂的螯合物(有机盐或无机盐)包含在介质中。 解决方案:螯合物由(A)顺磁金属阳离子形成,(B)由式I [(m)表示的化合物为1或2; R'是H,1-4C烷基或羟基烷基; R由式Ⅱ表示[(a)为1或2; Z是单键,CH2等; Z'是单键,O,S,CH 2,CO,NQ(Q是H,1-4C烷基等)等; Z“是CO-NQ,NQ-CO等; R 1〜R 5各自为H,Br,Cl,I等,条件是R 1〜R 5中的一个以上且以下分别为酰胺] 提供螯合物(有机盐或无机盐),螯合物通过使金属阳离子M 3+的螯合物与式III表示的化合物与式IV表示的胺在式 偶联剂,特别是合成肽时使用的偶联剂。