New multifunctional ligands for potential use in the design therapeutic
or diagnostic radiopharmaceutical imaging agents
    6.
    发明授权
    New multifunctional ligands for potential use in the design therapeutic or diagnostic radiopharmaceutical imaging agents 失效
    用于设计治疗或诊断性放射性药物成像剂的新的多功能配体

    公开(公告)号:US5601800A

    公开(公告)日:1997-02-11

    申请号:US211905

    申请日:1994-07-29

    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.

    摘要翻译: PCT No.PCT / US92 / 09742 Sec。 371日期1994年7月29日第 102(e)日期1994年7月29日PCT 1991年11月9日PCT PCT。 公开号WO93 / 08839 日期1993年5月13日一类衍生自次膦酰亚胺的诊断和治疗化合物,其包括含有单次膦亚胺官能团的配体或膦亚胺基和膦或胂基,或氨基或第二次膦酰亚胺部分。 这些膦亚胺配体与早期过渡金属放射性核素(例如99mTc或186Re / 188Re)或后过渡金属(例如,105Rh或109Pd)络合。 与这些金属186Re / 188Re,99mTc和109Pd的配合物具有高体外和高体内稳定性。 络合物以高产率形成并且可以是中性的或带电的。 这些配体也可以用于形成具有顺磁性过渡金属(例如Fe和Mn)的稳定化合物,用于潜在的用作MRI造影剂。 还公开了使用配体和制备配体的应用。

    Method for treating liquid wastes
    8.
    发明授权
    Method for treating liquid wastes 失效
    液体废物处理方法

    公开(公告)号:US5478474A

    公开(公告)日:1995-12-26

    申请号:US165373

    申请日:1993-12-10

    摘要: The method of treating liquid waste in a media is accomplished by exposing the media to phosphinimines and sequestering .sup.99 Tc from the media by the phosphinimine (PN) functionalities. The system for treating the liquid waste in the media includes extraction of .sup.99 TcO.sub.4.sup.- from aqueous solutions into organic solvents or mixed organic/polar media, extraction of .sup.99 Tc from solutions on a solid matrix by using a container containing PN functionalities on solid matrices including an inlet and outlet for allowing flow of media through an immobilized phosphinimine ligand system contained within the container. Also, insoluble suspensions of phosphinimine functionalities on solid matrices in liquid solutions or present on supported liquid membranes (SLM) can be used to sequester .sup.99 Tc from those liquids.

    摘要翻译: 通过将介质暴露于次膦酰亚胺并通过膦亚胺(PN)官能团从介质中螯合99Tc来实现处理介质中废液的方法。 用于处理介质中的液体废物的系统包括将99TcO4-从水溶液中萃取到有机溶剂或混合有机/极性介质中,通过使用在包括入口的固体基质上含有PN官能团的容器从固体基质上的溶液中提取99Tc 和用于允许介质流过包含在容器内的固定化膦酰亚胺配体系统的出口。 此外,膦酰亚胺功能性在液体溶液中固体基质上的不溶性悬浮液或存在于载体液膜(SLM)上的不溶性悬浮液可用于从这些液体中螯合99Tc。

    Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy
    9.
    发明授权
    Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy 失效
    双功能螯合剂用于设计和开发位点特异性放射性药物和生物分子共轭策略

    公开(公告)号:US06635235B1

    公开(公告)日:2003-10-21

    申请号:US09602487

    申请日:2000-06-23

    IPC分类号: A61K5100

    CPC分类号: A61K49/0002 A61K51/0478

    摘要: There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the —PR2 containing biomolecules by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a —PR2 containing biomolecule.

    摘要翻译: 提供了以特异性方式用过渡金属或放射性金属标记生物分子的方法,以通过合成P2N2-双功能螯合剂中间体,将中间体与放射性金属或过渡金属络合来制备诊断或治疗药物化合物, 并以特异性方式将所得的金属络合的双功能螯合剂与生物分子共价连接。 还提供了通过合成P2N2-双功能螯合剂中间体,使中间体与放射性金属或过渡金属络合,并将所得的放射性金属络合的双功能螯合剂与生物分子共价连接的方法来合成含有-PPR的生物分子的方法 现场具体方式。 提供包含含有-PR2的生物分子的治疗或诊断剂。

    Gold-containing chemotherapeutic agents
    10.
    发明授权
    Gold-containing chemotherapeutic agents 失效
    含金化学治疗剂

    公开(公告)号:US06989158B1

    公开(公告)日:2006-01-24

    申请号:US10019192

    申请日:2000-06-23

    IPC分类号: A61K31/28 A61K33/24

    CPC分类号: A61K31/28

    摘要: There is provided a complex for use as a therapeutic pharmaceutical, the complex has a ligand containing at least one hydroxyalkyl phosphine donor group bound to a gold atom to form a stable gold-ligand complex. Also provided is a method of treating cancer by administering an effective amount of a complex having a ligand of at least one hydroxyalkyl phosphine group bound to a gold atom to form a stable gold-ligand complex. Also provided is a method of preventing the metastasis of cancer and arresting cell growth by administering an effective amount of a complex having a ligand of at least one hydroxyalkyl phosphine group bound to a gold atom to form a stable gold-ligand complex.

    摘要翻译: 提供了用作治疗药物的复合物,该配合物具有含有至少一个与金原子结合的羟烷基膦供体基团以形成稳定的金 - 配体络合物的配体。 还提供了通过施用有效量的具有与金原子结合的至少一个羟基烷基膦基团的配体的络合物以形成稳定的金 - 配体络合物来治疗癌症的方法。 还提供了通过施用有效量的具有与金原子结合的至少一个羟烷基膦基配体的配合物以形成稳定的金 - 配体络合物的方法来防止癌症转移和阻止细胞生长的方法。