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    In vivo enhancement of cellular accumulation of lipophilic cationic organometallic compounds by reduction of intramembrane potential
    1.
    发明授权
    In vivo enhancement of cellular accumulation of lipophilic cationic organometallic compounds by reduction of intramembrane potential 失效
    通过降低膜内电位体内增强亲脂阳离子有机金属化合物的细胞积累

    公开(公告)号：US5277897A

    公开(公告)日：1994-01-11

    申请号：US945916

    申请日：1992-09-17

    申请人： David R. Piwnica-Worms ,  James F. Kronauge

    发明人： David R. Piwnica-Worms ,  James F. Kronauge

    IPC分类号： A61K31/28 ,  A61K49/00 ,  A61K51/04 ,  A61K31/69

    CPC分类号： A61K51/0476 ,  A61K31/28 ,  A61K2121/00 ,  A61K2123/00 ,  Y10S514/836 ,  Y10S514/946

    摘要： The invention relates to compositions that comprise (1) lipophilic cationic organometallic complexes, particularly hexakis(2-methoxyisobutylisonitrile)technetium(I) complex, and (2) an agent that decreases the intramembrane potential of a living cell. Agents which decrease the intramembrane potential of a living cell include the lipophilic anions, especially tetraphenylborate anion. The invention also relates to methods in which the compositions are administered in vivo and in vitro when it is desirable to obtain enhanced cellular accumulation of lipophilic cationic organometallic complexes. The compositions and methods are useful for diagnosis and treatment, pSTATEMENT AS TO RIGHTS TO INVENTIONS MADE UNDER FEDERALLY-SPONSORED RESEARCH AND DEVELOPMENTPart of the work performed during development of this invention utilized U.S. Government funds. The U.S. Government has certain rights in this invention.

    摘要翻译： 本发明涉及包含（1）亲脂阳离子有机金属络合物，特别是六（2-甲氧基异丁基腈）锝（I）络合物的组合物，和（2）降低活细胞的膜电位的试剂。 降低活细胞的膜电位的药剂包括亲脂性阴离子，特别是四苯硼酸盐阴离子。 本发明还涉及当期望获得增强的亲脂性阳离子有机金属配合物的细胞积聚时，组合物在体内和体外施用的方法。 组合物和方法可用于诊断和治疗，特别是体内组织成像。

    Technetium- and Rhenium-Bis(heteroaryl) Complexes, and Methods of Use Thereof
    3.
    发明申请
    Technetium- and Rhenium-Bis(heteroaryl) Complexes, and Methods of Use Thereof 审中-公开
    锝和铼 - 双（杂芳基）络合物及其使用方法

    公开(公告)号：US20100303725A1

    公开(公告)日：2010-12-02

    申请号：US12750533

    申请日：2010-03-30

    申请人： John W. Babich ,  Kevin B. Maresca ,  James F. Kronauge, JR.

    发明人： John W. Babich ,  Kevin B. Maresca ,  James F. Kronauge, JR.

    IPC分类号： A61K49/00 ,  C07D233/61 ,  C07F15/00 ,  A61K31/555 ,  C07K1/00

    CPC分类号： C07F13/005 ,  C07D213/38

    摘要： One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

    摘要翻译： 本发明的一个方面涉及放射性核素与各种杂芳基配体的复合物，例如咪唑基和吡啶基配体，以及它们在放射性药物中用于多种临床诊断和治疗应用的复合物。 本发明的另一方面涉及形成上述配合物的一部分的咪唑基和吡啶基配体。 还描述了制备放射性核素复合物的方法。 本发明的另一方面涉及基于通过固相合成方法与小肽缀合的衍生化赖氨酸，丙氨酸和双氨基酸的咪唑基和吡啶基配体。 另外，本发明涉及使用本发明复合物成像哺乳动物区域的方法。

    Technetium- and rhenium-bis(heteroaryl) complexes, and methods of use thereof
    4.
    发明授权
    Technetium- and rhenium-bis(heteroaryl) complexes, and methods of use thereof 失效
    锝和铼 - 双（杂芳基）络合物及其使用方法

    公开(公告)号：US07824661B2

    公开(公告)日：2010-11-02

    申请号：US11057714

    申请日：2005-02-14

    申请人： John W. Babich ,  Kevin B. Maresca ,  James F. Kronauge, Jr.

    发明人： John W. Babich ,  Kevin B. Maresca ,  James F. Kronauge, Jr.

    IPC分类号： A61K49/00

    CPC分类号： A61K51/0478 ,  C07F13/005

    摘要： One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

    摘要翻译： 本发明的一个方面涉及放射性核素与各种杂芳基配体的复合物，例如咪唑基和吡啶基配体，以及它们在放射性药物中用于多种临床诊断和治疗应用的复合物。 本发明的另一方面涉及形成上述配合物的一部分的咪唑基和吡啶基配体。 还描述了制备放射性核素复合物的方法。 本发明的另一方面涉及基于通过固相合成方法与小肽缀合的衍生化赖氨酸，丙氨酸和双氨基酸的咪唑基和吡啶基配体。 另外，本发明涉及使用本发明复合物成像哺乳动物区域的方法。

    Pharmaceutical Composition Of A Radioiodinated Benzamide Derivative And Methods Of Making Same
    5.
    发明申请
    Pharmaceutical Composition Of A Radioiodinated Benzamide Derivative And Methods Of Making Same 审中-公开
    放射性碘化苯甲酰胺衍生物的药物组成及其制备方法

    公开(公告)号：US20110206608A1

    公开(公告)日：2011-08-25

    申请号：US13062410

    申请日：2009-09-04

    申请人： Jianqing Chen ,  James F. Kronauge ,  John W. Babich

    发明人： Jianqing Chen ,  James F. Kronauge ,  John W. Babich

    IPC分类号： A61K51/04 ,  C07C237/30 ,  A61P35/00

    CPC分类号： A61K31/16

    摘要： Provided is a pharmaceutical composition comprising radioiodinated N-(2-(diethylamino)ethyl)-4-(4-fluorobenzamido)-5-iodo-2-methoxybenzamide of Formula I. The pharmaceutical composition provides a stable formulation for both storing and administering to patients having melanoma. Also provided is a novel method of iodinating the precursor compound.

    摘要翻译： 提供了包含式I的放射性碘化N-（2-（二乙基氨基）乙基）-4-（4-氟苯甲酰氨基）-5-碘-2-甲氧基苯甲酰胺的药物组合物。药物组合物提供稳定的制剂，用于储存和施用 患有黑色素瘤的患者 还提供了一种碘化前体化合物的新方法。

    Enhancement of cellular accumulation of lipophilic cationic organometallic compounds by reduction of intramembrane potential
    6.
    发明授权
    Enhancement of cellular accumulation of lipophilic cationic organometallic compounds by reduction of intramembrane potential 失效
    通过减少内皮细胞增强脂肪酸阳离子有机化合物的细胞积累

    公开(公告)号：US5186923A

    公开(公告)日：1993-02-16

    申请号：US594813

    申请日：1990-10-10

    申请人： David R. Piwnica-Worms ,  James F. Kronauge

    发明人： David R. Piwnica-Worms ,  James F. Kronauge

    IPC分类号： A61K31/28 ,  A61K49/00 ,  A61K51/04

    CPC分类号： A61K51/0476 ,  A61K31/28 ,  A61K2121/00 ,  A61K2123/00 ,  Y10S514/836 ,  Y10S514/946

    摘要： The invention relates to compositions that comprise (1) lipophilic cationic organometallic complexes, particularly hexakis(2-methoxyisobutylisonitrile)technetium(I) complex, and (2) an agent that decreases the intramembrane potential of a living cell. Agents which decrease the intramembrane potential of a living cell include the lipophilic anions, especially tetraphenylborate anion. The invention also relates to methods in which the compositions are administered in vivo and in vitro when it is desirable to obtain enhanced cellular accumulation of lipophilic cationic organometallic complexes. The compositions and methods are useful for diagnosis and treatment, particularly in vivo tissue imaging.

    摘要翻译： 本发明涉及包含（1）亲脂阳离子有机金属络合物，特别是六（2-甲氧基异丁基腈）锝（I）络合物的组合物，和（2）降低活细胞的膜电位的试剂。 降低活细胞的膜电位的试剂包括亲脂性阴离子，特别是四苯基硼酸盐阴离子。 本发明还涉及当期望获得增强的亲脂性阳离子有机金属配合物的细胞积聚时，组合物在体内和体外施用的方法。 组合物和方法可用于诊断和治疗，特别是体内组织成像。