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New multifunctional ligands for potential use in the design therapeutic or diagnostic radiopharmaceutical imaging agents

机译:新的多功能配体可用于设计治疗性或诊断性放射性药物成像剂

摘要

A class of diagnostic and therapeutic compounds derived from phosphinimines that include ligands containing either a single phosphinimine functionality or both a phosphinimine group and a phosphine or arsine group, or an aminato group, or a second phosphinimine moiety. These phosphinimine ligands are complexed to early transition metal radionuclides (e.g. .sup.99m Tc or .sup.186 Re/.sup.188 Re) or late transition metals (e.g., .sup.105 Rh or .sup.109 Pd). The complexes with these metals .sup.186 Re/.sup.188 Re, .sup.99m Tc and .sup.109 Pd exhibit a high in vitro and high in vivo stability. The complexes are formed in high yields and can be neutral or charged. These ligands can also be used to form stable compounds with paramagnetic transition metals (e.g. Fe and Mn) for potential use as MRI contrast agents. Applications for the use of ligands and making the ligands are also disclosed.
机译:一类衍生自膦亚胺的诊断和治疗化合物,其包括含有单个膦亚胺官能团或膦亚胺基团和膦或a基,或氨基基团或第二膦亚胺部分的配体。这些膦亚胺配体与早期过渡金属放射性核素(例如99m Tc或186 Re / s188 Re)或晚期过渡金属(例如105 Rh或109 Pd)络合。与这些金属的186 Re / s 188 Re,99m Tc和109 Pd的配合物表现出很高的体外和体内稳定性。复合物以高收率形成,并且可以是中性的或带电荷的。这些配体还可用于与顺磁性过渡金属(例如,Fe和Mn)形成稳定的化合物,以潜在地用作MRI造影剂。还公开了使用配体和制备配体的申请。

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