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    Contrast agents endowed with high relaxivity for use in magnetic resonance imaging (MRI) which contain a chelating moiety with polyhydroxylated substituents
    7.
    发明授权
    Contrast agents endowed with high relaxivity for use in magnetic resonance imaging (MRI) which contain a chelating moiety with polyhydroxylated substituents 有权
    对比剂具有高的放松性，用于磁共振成像（MRI），其含有具有多羟基化取代基的螯合部分

    公开(公告)号：US07988950B2

    公开(公告)日：2011-08-02

    申请号：US11630605

    申请日：2005-06-28

    申请人： Silvio Aime ,  Matteo Galli ,  Luciano Lattuada ,  Pierfrancesco Morosini ,  Fulvio Uggeri ,  Kondareddiar Ramalingam

    发明人： Silvio Aime ,  Matteo Galli ,  Luciano Lattuada ,  Pierfrancesco Morosini ,  Fulvio Uggeri ,  Kondareddiar Ramalingam

    IPC分类号： A61B5/055 ,  A61K49/10 ,  C07F5/00

    CPC分类号： C07H15/26 ,  A61K49/085 ,  A61K49/124 ,  C07C237/08 ,  C07D243/08 ,  C07D243/10 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/5728 ,  C07H17/02

    摘要： The present invention relates to a novel class of paramagnetic ion-based contrast i agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a pharmacokinetic i profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity. Formula (I): A(LR)v wherein: A is a linear or cyclic chelating backbone moiety; R is, independently, H or a C2-C70aminopolyol moiety comprising a ‘straight or branched alkyl chain substituted by from 2 to 30 hydroxyl groups, the said chain being optionally interrupted by one or more groups selected from -0-, —NH—, —N NCO—; and optionally substituted by one or more C4-C10 cyclic units; L is, independently, a direct bond or “a divalent straight or branched linker moiety between A and R, at most comprising 20 carbon atoms; V is a positive integer from 1 to 7; with the proviso that at least one of the R groups is other than H; or a physiologically acceptable salt of such ligand.

    摘要翻译： 本发明涉及一类新颖的式（I）的顺磁离子型对比剂，其中螯合骨架部分通过存在一个或多个多羟基化链而被高度官能化，其显示类似于 常用的T1一般血管外药物（NSA），但其进一步特征在于较高的松弛度。 式（I）：A（LR）v其中：A是直链或环状螯合骨架部分; R独立地是H或包含被2至30个羟基取代的“直链或支链烷基链”的C2-C70氨基多酚部分，所述链任选地被一个或多个选自-O-，-NH-， -N'， - CO - ， - CONH - ， - NHCO-，-CON'或> NCO-; 并任选地被一个或多个C 4 -C 10环单元取代; L独立地是直接键或“A和R之间的二价直链或支链连接体部分，最多包含20个碳原子; V是1到7的正整数; 条件是至少一个R基团不是H; 或这种配体的生理上可接受的盐。