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MULTIDENTATE BIFUNCTIONAL CHELATING AGENTS FOR RADIONUCLIDE COMPLEXATION IN DIAGNOSTICS AND THERAPY
MULTIDENTATE BIFUNCTIONAL CHELATING AGENTS FOR RADIONUCLIDE COMPLEXATION IN DIAGNOSTICS AND THERAPY
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机译:诊断和治疗中放射性核素络合的多齿双功能螯合剂
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摘要
The invention relates to octadentate ligands of a general formula R1-D-X-D-X-D-X-D-E-R2, wherein D is C(O)N(OH) or N(OH)C(O), pyrimidinone or pyridinone, each X independently of any other X is a saturated or partially unsaturated, substituted or unsubstituted linker comprising 8-11 atoms selected from any of N, C, O; R1 is alkyl, cycloalkyl, arene, or heteroarene, E is a saturated or partially unsaturated, substituted or unsubstituted chain comprising 1-50 atoms and R2 is a moiety capable of selectively binding to a biomolecule, or a nanoparticle. The invention further relates to complexes of the ligand, particularly radionuclides and their use in radioimmunotherapy and imaging.
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机译:本发明涉及通式R1-DXDXDXDE-R2的八齿配体,其中D是C(O)N(OH)或N(OH)C(O),嘧啶酮或吡啶酮,每个X独立于其他X是包含选自N,C,O中的8-11个原子的饱和或部分不饱和,取代或未取代的连接基; R 1为烷基,环烷基,芳烃或杂芳烃,E为包含1-50个原子的饱和或部分不饱和的取代或未取代的链,并且R 2为能够选择性结合生物分子或纳米粒子的部分。本发明进一步涉及配体,特别是放射性核素的配合物及其在放射免疫疗法和成像中的用途。
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