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    • 9. 发明申请
    • MULTI-USE MULTIMODAL IMAGING CHELATES
    • 多用途多模式成像螯合
    • WO03020701A3
    • 2003-07-31
    • PCT/US0227800
    • 2002-09-04
    • UNIV TEXAS TECH
    • BORNHOP DARRYL JMANNING CHARLES HGOEBEL TIMOTHY
    • A61K31/675A61K49/00A61K49/10A61K31/33C07D225/00C07D257/02
    • A61K31/675A61K49/0002A61K49/106A61K51/0482
    • Cyclen-based chelates can be used as contrast agents for multi-modal imaging of tissue cells. The cyclen-based chelates are preferably polyazamacrocyclic molecules formed from 1,4,7,10, tetraazacyclododecane ("cyclen") having varying chelating ions, phosphoester chains, and light harvesting moieties. By changing the chelating ion, phosphoester chain length and/or the light harvesting moiety different imaging techniques, such as MRI, CT, fluorescence and absorption, x-ray and NIR, may be employed to image the tissue cells. Additionally, the cyclen-based chelates may be conjugated to provide for site-specific delivery of the cyclen-based chelate to the desired tissue cells. The cyclen-based chelates may also be delivered to the tissue cells by attaching the cyclen-based chelates to a polymeric delivery vehicle. Although these cyclen-based chelates have a wide variety of application, the preferred use is for imaging of cancers cells, such as brain cancer, for improving resection of a cancerous tissue.
    • 基于Cyclen的螯合物可以用作组织细胞的多模式成像的造影剂。 基于cyclen的螯合物优选为由具有不同螯合离子,磷酸酯链和光捕获部分的1,4,7,10,四氮杂环十二烷(“cyclen”)形成的聚氮杂大环分子。 通过改变螯合离子,可以采用不同的成像技术,例如MRI,CT,荧光和吸收,X射线和NIR来对组织细胞成像,磷酸酯链长度和/或光捕获部分。 另外,可以将基于循环的螯合物缀合以提供基于循环的螯合物到所需组织细胞的位点特异性递送。 基于循环的螯合物也可以通过将基于循环的螯合物连接至聚合物递送载体而递送至组织细胞。 尽管这些基于循环的螯合物具有广泛的应用,但优选用于癌症细胞例如脑癌的成像以改善癌组织的切除。