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    • 8. 发明申请
    • Vitamin-targeted imaging agents
    • 维生素靶向成像剂
    • US20070031334A1
    • 2007-02-08
    • US11546099
    • 2006-10-11
    • Christopher LeamonMatthew Parker
    • Christopher LeamonMatthew Parker
    • A61K51/00
    • A61K51/08A61K47/54A61K47/551A61K51/025A61K51/0402A61K51/0459A61K51/0497A61K51/088
    • The invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The invention provides a compound of the formula for use in such methods. In the compound, V is a vitamin that is a substrate for receptor-mediated transmembrane transport in vivo, or a vitamin receptor binding derivative or analog thereof, L is a divalent linker, R is a side chain of an amino acid of the formula H2NCHRCOOH, M is a cation of a radionuclide, n is 1 or 0, K is 1 or 0, and the compound can be in a pharmaceutically acceptable carrier therefor. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.
    • 本发明涉及通过使用这样的维生素作为成像剂的靶向配体,将基于放射性核素的成像剂靶向具有维生素或维生素受体结合衍生物或其类似物的受体的细胞的化合物和方法。 本发明提供了用于这些方法的式的化合物。 在化合物中,V是作为体内受体介导的跨膜转运的底物的维生素或维生素受体结合衍生物或其类似物,L是二价连接基,R是式H的氨基酸的侧链 NCHRCOOH,M是放射性核素的阳离子,n是1或0,K是1或0,并且该化合物可以在其药学上可接受的载体中。 基于维生素的化合物可用于将放射性核素靶向细胞,例如各种肿瘤细胞类型,用于靶向细胞的诊断成像。