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    • 7. 发明申请
    • 2-HYDROXY-1-OXO 1,2 DIHYDRO ISOQUINOLINE CHELATING AGENTS
    • 2-羟基-1-氧代1,2二氢异喹啉螯合剂
    • WO2007121453A2
    • 2007-10-25
    • PCT/US2007066814
    • 2007-04-17
    • UNIV CALIFORNIARAYMOND KENNETH NSEITZ MICHAEL
    • RAYMOND KENNETH NSEITZ MICHAEL
    • A61K31/472A61K49/10
    • C07D217/24A61K49/0002A61K49/085A61K49/126A61K51/0478A61K51/065C07D217/26
    • The invention provides a new class of strongly chelating multidentate ligands based on a 2-hydroxy-1-oxo-1,2-dihydro-isoquinoline-3-carboxylic acid scaffold (hereafter 1,2-HOIQO) in combination with polyamine backbones. The extremely stable bidentate 1,2- HOIQO moiety can be synthesized by standard synthetic methodology on a large scale. An advantageous feature is the possibility to introduce a wide range of substituents on the benzene ring by standard transformations (like electrophilic aromatic substitutions). This allows, for example, for the tuning of chemical, photophysical, and solubility properties, as well as the attachment of functional moieties, relevant for sensing and imaging applications (e.g. DNA, proteins, antibodies, fluorophores, etc.). The combination of the 1,2-HOIQO chelators with polyamine backbones provides very strongly binding ligands for a variety of metals including first-row transition metals, lanthanides, actinides, etc. Metal complexes of this kind are expected to be useful in a number of applications (e.g. luminescence, MRI, actinide sequestering, metal chelation therapy, metal radioisotope labeling, etc.).
    • 本发明提供了一类基于2-羟基-1-氧代-1,2-二氢异喹啉-3-羧酸支架(以下称为1,2-HOIQO)与多胺骨架组合的强螯合多齿配体。 非常稳定的二齿1,2- HOIQO部分可以通过大规模的标准合成方法合成。 有利的特征是可以通过标准转化(如亲电芳族取代)在苯环上引入宽范围的取代基。 这允许例如调节与传感和成像应用(例如DNA,蛋白质,抗体,荧光团等)相关的化学,光物理和溶解性质以及功能部分的附着。 1,2-HOIQO螯合剂与多胺骨架的组合为各种金属(包括一列过渡金属,镧系元素,锕系元素等)提供了非常强的结合性配体。预计这种金属络合物可用于多种 应用(例如发光,MRI,锕系隔离,金属螯合治疗,金属放射性同位素标记等)。