Technetium-99M labeled peptides for imaging inflammation
    91.
    发明授权
    Technetium-99M labeled peptides for imaging inflammation 失效
    锝-99M标记的肽用于成像炎症

    公开(公告)号:US5714579A

    公开(公告)日:1998-02-03

    申请号:US462784

    申请日:1995-06-05

    摘要: This invention relates to compositions that are radiolabeled scintigraphic imaging agents, comprising a polybasic compound covalently linked to a radiolabel binding moiety and the composition further comprising a polysulfated glycan. The invention also provides methods for producing and using such compositions. Specifically, the invention relates to compositions comprised of technetium-99m (Tc-99m) labeled scintigraphic imaging agents comprising a polybasic compound having at least 5 chemical functionalities that are basic at physiological pH and a radiolabel-binding moiety, the composition further comprising a polysulfated glycan, the composition being capable of specifically binding to inflammatory sites in vivo. Methods and kits for making such compositions, and methods for using such compositions to image sites of infection and inflammation in a mammalian body, are also provided.

    摘要翻译: 本发明涉及放射性标记的闪烁照相成像剂的组合物,其包含与放射性标记结合部分共价连接的多元化合物,该组合物还包含多硫酸化聚糖。 本发明还提供了生产和使用这种组合物的方法。 具体地说,本发明涉及由锝-99m(Tc-99m)标记的闪烁照相成像剂组成的组合物,其包含在生理pH和放射性标记结合部分具有碱性的至少5种化学官能度的多元化合物,该组合物还包含多硫酸化 聚糖,该组合物能够在体内特异性结合炎性部位。 还提供了用于制备这种组合物的方法和试剂盒,以及使用这些组合物来成像哺乳动物体内感染和炎症部位的方法。

    Technetium-99m labeled peptides for imaging inflammation
    93.
    发明授权
    Technetium-99m labeled peptides for imaging inflammation 失效
    锝-99m标记的肽用于成像炎症

    公开(公告)号:US5561220A

    公开(公告)日:1996-10-01

    申请号:US73577

    申请日:1993-06-07

    摘要: This invention relates to compositions that are radiolabeled scintigraphic imaging agents, comprising a polybasic compound covalently linked to a radiolabel binding moiety and the composition further comprising a polysulfated glycan. The invention also provides methods for producing and using such compositions. Specifically, the invention relates to compositions comprised of technetium-99m (Tc-99m) labeled scintigraphic imaging agents comprising a polybasic compound having at least 5 chemical functionalities that are basic at physiological pH and a radiolabel-binding moiety, the composition further comprising a polysulfated glycan, the composition being capable of specifically binding to inflammatory sites in vivo. Methods and kits for making such compositions, and methods for using such compositions to image sites of infection and inflammation in a mammalian body, are also provided.

    摘要翻译: 本发明涉及放射性标记的闪烁照相成像剂的组合物,其包含与放射性标记结合部分共价连接的多元化合物,该组合物还包含多硫酸化聚糖。 本发明还提供了生产和使用这种组合物的方法。 具体地说,本发明涉及由锝-99m(Tc-99m)标记的闪烁照相成像剂组成的组合物,其包含在生理pH和放射性标记结合部分具有碱性的至少5种化学官能度的多元化合物,该组合物还包含多硫酸化 聚糖,该组合物能够在体内特异性结合炎性部位。 还提供了用于制备这种组合物的方法和试剂盒,以及使用这些组合物来成像哺乳动物体内感染和炎症部位的方法。

    One vial method for labeling protein/linker conjugates with
technetium-99M
    94.
    发明授权
    One vial method for labeling protein/linker conjugates with technetium-99M 失效
    用锝-99M标记蛋白质/接头偶联物的一个小瓶方法

    公开(公告)号:US5180816A

    公开(公告)日:1993-01-19

    申请号:US235908

    申请日:1988-08-24

    申请人: Richard T. Dean

    发明人: Richard T. Dean

    IPC分类号: C07K1/107 C07K5/083

    摘要: A one vial method for labeling a protein, such as an antibody or antibody fragment, with a radiometal such as Tc-99m or a rhenium isotope, is disclosed. The method comprises contacting in a single vial a mixture comprised of a reducing agent and a protein molecule covalently bound to a sulfhydryl containing bifunctional coupling agent with Tc or Re in an oxidized state. A one vial kit for labeling a protein with Tc or Re is also disclosed.

    摘要翻译: 公开了一种用于用诸如Tc-99m或铼同位素等放射性金属标记蛋白质,如抗体或抗体片段的方法。 该方法包括在单个小瓶中将由还原剂和与含巯基的双功能偶联剂共价结合的蛋白质分子组成的混合物与氧化态的Tc或Re接触。 还公开了用于用Tc或Re标记蛋白质的一个小瓶试剂盒。

    Cleavable bifunctional coupling agents
    95.
    发明授权
    Cleavable bifunctional coupling agents 失效
    可切换双功能偶联剂

    公开(公告)号:US5144043A

    公开(公告)日:1992-09-01

    申请号:US235999

    申请日:1988-08-24

    IPC分类号: A61K51/10 C07C327/32

    摘要: A bifunctional coupling agent for joining a sulfhydryl containing protein or peptide and a metallic radionuclide comprising a sulfhydryl selective electrophile, a chelator containing at least one protected thiol and a organic linking radical containing at least one cleavable site which serves to join said electrophile and said chelator is disclosed. A radiodiagnostic or radiotherapeutic precursor comprising an antibody or antibody fragment and the specified bifunctional coupling agent bound to a sulfhydryl group on the antibody or antibody fragment and a radiodiagnostic or radiotherapeutic agent comprising such precursor having a metallic radionuclide bound thereto are also disclosed.

    摘要翻译: 一种用于连接含巯基的蛋白质或肽和包含巯基选择性亲电子试剂的金属放射性核素的双功能偶联剂,含有至少一种保护的硫醇的螯合剂和含有至少一个可切割位点的有机连接基团,其用于将所述亲电试剂和所述螯合剂 被披露。 还公开了包含抗体或抗体片段的抗放射治疗或放射治疗前体,以及与抗体或抗体片段上的巯基结合的特定的双功能偶联剂和包含与其结合的金属放射性核素的前体的放射诊断或放射治疗剂。

    Imino ethers
    97.
    发明授权
    Imino ethers 失效
    亚麻醚

    公开(公告)号:US4490303A

    公开(公告)日:1984-12-25

    申请号:US421751

    申请日:1982-09-23

    摘要: Fluorescein esters and ethers including the dioleyl derivative of fluorescein are disclosed. These compounds have the useful property of being fluorescent under the influence of the proper frequency of electromagnetic irradiation. Further, dioleyl fluorescein is readily incorporated into low-density lipoproteins which can then become part of the cell matter; the compounds retain their fluorescent properties during this procedure. The fluorescence allows cells to be indentified and separated. The fluorescein esters and ethers are prepared from fluorescein and the novel reagent O-alkenyl-N,N'-dialkylisourea.

    摘要翻译: 公开了包含荧光素的二油基衍生物的荧光素酯和醚。 这些化合物在电磁辐射的适当频率的影响下具有荧光的有用特性。 此外,二烯基荧光素容易地并入低密度脂蛋白,然后可以成为细胞物质的一部分; 该化合物在此过程中保持其荧光性质。 荧光允许细胞被识别和分离。 荧光素酯和醚由荧光素和新型试剂O-烯基-N,N'-二烷基异脲制备。

    Fluorescein esters and ethers and the preparation thereof
    98.
    发明授权
    Fluorescein esters and ethers and the preparation thereof 失效
    荧光素酯和醚及其制备

    公开(公告)号:US4304720A

    公开(公告)日:1981-12-08

    申请号:US145173

    申请日:1980-04-30

    摘要: Fluorescein esters and ethers including the dioleyl derivative of fluorescein are disclosed. These compounds have the useful property of being fluorescent under the influence of the proper frequency of electromagnetic irradiation. Further, dioleyl fluorescein is readily incorporated into low-density lipoproteins which can then become part of the cell matter; the compounds retain their fluorescent properties during this procedure. The fluorescence allows cells to be identified and separated. The fluorescein esters and ethers are prepared from fluorescein and the novel reagent O-alkenyl-N,N'-dialkylisourea.

    摘要翻译: 公开了包含荧光素的二油基衍生物的荧光素酯和醚。 这些化合物在电磁辐射的适当频率的影响下具有荧光的有用特性。 此外,二烯基荧光素容易地并入低密度脂蛋白,然后可以成为细胞物质的一部分; 该化合物在此过程中保持其荧光性质。 荧光允许细胞被鉴定和分离。 荧光素酯和醚由荧光素和新型试剂O-烯基-N,N'-二烷基异脲制备。

    Monoamine, diamide, thiol-containing metal chelating agents
    99.
    发明授权
    Monoamine, diamide, thiol-containing metal chelating agents 失效
    单胺,二酰胺,含硫醇的金属螯合剂

    公开(公告)号:US07238340B1

    公开(公告)日:2007-07-03

    申请号:US08253973

    申请日:1994-06-03

    IPC分类号: A61K51/00 A61K49/00

    摘要: Therapeutically active thiazole derivatives of formula (I) wherein R1-R2, X and X′ as are defined in the specification, processes for the preparation thereof, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor • (TGF-•), and pharmaceutical compositions for use in such therapy.

    摘要翻译: 在说明书中定义的其中R 1,R 2,X和X'的式(I)的治疗活性噻唑衍生物用于制备它们,其用途 特别是治疗或预防转化生长因子过度表达的疾病。 (TGF-β)和用于此类治疗的药物组合物。

    Somatostatin derivatives and their radiolabelled products
    100.
    发明授权
    Somatostatin derivatives and their radiolabelled products 失效
    生长抑素衍生物及其放射性标记物

    公开(公告)号:US06241965B1

    公开(公告)日:2001-06-05

    申请号:US08586670

    申请日:1996-04-22

    IPC分类号: A61K5100

    摘要: This invention relates to therapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labelled radiodiagnostic agents. Specifically, the invention relates to linear peptide derivatives and analogs of somatostatin, and embodiments of such peptides radiolabelled with a radioisotope, as well as methods and kits for making, radiolabelling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to linear peptide derivatives and analogues of somatostatin radiolabelled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specicically relates to linear peptide derivatives and analogues of somatostatin radiolabelled with cytotoxic radioisotopes such as rhenium-186 (186Re) and rhenium-188 (188Re) for use as radiotherapeutic agents. Methods and kits for making, radiolabelling and using such peptides diagnostically and therapeutically in a mammalian body are also provided.

    摘要翻译: 本发明涉及治疗试剂和肽,放射诊断试剂和肽,以及用于制备标记的放射诊断剂的方法。 具体地,本发明涉及生长抑素的线性肽衍生物和类似物以及用放射性同位素放射性标记的这种肽的实施方案,以及用于制造,放射性标记和使用这些肽用于放射诊断和放射治疗目的的方法和试剂盒。 本发明具体涉及用锝-99m放射性标记的生长抑素的线性肽衍生物和类似物及其作为闪烁照相成像剂的用途。 本发明还特异性地涉及放射性标记的细胞毒性放射性同位素如铼-186(186Re)和铼-188(188Re)的生长抑素的线性肽衍生物和类似物用作放射治疗剂。 还提供了用于在哺乳动物身体中诊断和治疗地制备,放射性标记和使用这些肽的方法和试剂盒。