Somatostatin analogs
    2.
    发明授权
    Somatostatin analogs 失效
    生长抑素类似物

    公开(公告)号:US06358491B1

    公开(公告)日:2002-03-19

    申请号:US09397792

    申请日:1999-09-16

    IPC分类号: A61K5100

    摘要: The invention provides novel peptide-based pharmacophores and compounds which bind somatostatin receptors with high affinity and which exhibit improved pharmacokinetic properties over known somatostatin analogs. The pharmacophores and compounds of the invention may be used in labeled or unlabeled form for diagnosing and/or treating somatostatin responsive diseases. The invention also provides radiopharmaceuticals and kits comprising these compounds, as well as methods for diagnosing and/or treating somatostatin receptor mediated diseases.

    摘要翻译: 本发明提供了新颖的基于肽的药效学和与高亲和力结合生长抑素受体的化合物,并且与已知的生长抑素类似物相比表现出改进的药代动力学性质。 本发明的药效团和化合物可以以标记或未标记的形式用于诊断和/或治疗生长抑素反应性疾病。 本发明还提供包含这些化合物的放射性药物和试剂盒,以及用于诊断和/或治疗生长抑素受体介导的疾病的方法。

    Radiolabeled somatostatin-derived peptides for imaging and therapeutic
uses
    5.
    发明授权
    Radiolabeled somatostatin-derived peptides for imaging and therapeutic uses 失效
    放射性标记的生长抑素衍生肽用于成像和治疗用途

    公开(公告)号:US6051206A

    公开(公告)日:2000-04-18

    申请号:US592323

    申请日:1996-05-06

    IPC分类号: A61K51/08 A61K51/00 A61M36/14

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

    摘要翻译: PCT No.PCT / US94 / 06274 Sec。 371日期:1996年5月6日 102(e)日期1996年5月6日PCT提交1994年6月3日PCT公布。 公开号WO95 / 00553 日期1995年1月5日本发明涉及治疗试剂和肽,包括放射治疗试剂和肽,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环肽衍生物和类似物,以及用放射性同位素放射性标记的这种肽的实施方案,以及用于制备放射性标记和用于放射诊断和放射治疗目的的这些肽的方法和试剂盒。 本发明具体涉及用锝-99m放射性标记的生长抑素的环肽衍生物和类似物及其用作闪烁照相成像剂。 本发明还具体涉及用作放射性治疗剂放射性标记的细胞毒性放射性同位素如铼-186(186Re)和铼-188(188Re)的生长抑素的环肽衍生物和类似物用于制造,放射性标记和使用这些肽的方法和试剂盒, 还提供了哺乳动物体内的治疗。

    Radiolabeled somatostatin receptor-binding peptides
    6.
    发明授权
    Radiolabeled somatostatin receptor-binding peptides 失效
    放射标记生长抑素受体结合肽

    公开(公告)号:US6017509A

    公开(公告)日:2000-01-25

    申请号:US92355

    申请日:1993-07-15

    摘要: This invention relates to therapeutic reagents and peptides, including radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to cyclic peptide derivatives and analogs of somatostatin, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re) for use as radiotherapeutic agents. Methods and kits for making, radiolabeling 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,包括放射治疗试剂和肽,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环肽衍生物和类似物,以及用放射性同位素放射性标记的这种肽的实施方案,以及用于制备放射性标记和用于放射诊断和放射治疗目的的这些肽的方法和试剂盒。 本发明具体涉及用锝-99m放射性标记的生长抑素的环肽衍生物和类似物及其用作闪烁照相成像剂。 本发明还具体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)用作放射治疗剂的生长抑素的环肽衍生物和类似物。 还提供了用于在哺乳动物体内制造,放射性标记和诊断和治疗上使用这些肽的方法和试剂盒。

    Technetium-99m labeled peptides for thrombus imaging
    8.
    发明授权
    Technetium-99m labeled peptides for thrombus imaging 失效
    锝-99m标记肽用于血栓成像

    公开(公告)号:US5925331A

    公开(公告)日:1999-07-20

    申请号:US335832

    申请日:1995-01-05

    摘要: This invention relates to radiolabeled reagents that are scintigraphic imaging agents for imaging sites of thrombus formation in vivo, and methods for producing such reagents. Specifically, the invention relates to reagents each comprised of a specific binding compound, capable of binding to at least one component of a thrombus, covalently linked to a radiolabel-binding moiety. The invention provides these reagents, methods and kits for making such reagents, and methods for using such reagents labeled with technetium-99m to image thrombus sites in a mammalian body.

    摘要翻译: PCT No.PCT / US93 / 04794 Sec。 371 1995年1月5日第 102(e)日期1995年1月5日PCT提交1993年5月21日PCT公布。 公开号WO93 / 23085 日期11月25日,日本本发明涉及用于体内血栓形成成像部位的闪烁照相成像剂的放射标记试剂及其制备方法。 具体地说,本发明涉及各自由特异性结合化合物组成的试剂,能够与至少一种共价连接于放射性标记结合部分的血栓成分结合。 本发明提供了用于制备这些试剂的这些试剂,方法和试剂盒,以及使用标示有锝-99m的试剂来形成哺乳动物体内的血栓位点的方法。

    Somatostatin-derived peptides for imaging and therapeutic uses
    10.
    发明授权
    Somatostatin-derived peptides for imaging and therapeutic uses 失效
    用于成像和治疗用途的生长抑素衍生肽

    公开(公告)号:US5820845A

    公开(公告)日:1998-10-13

    申请号:US466100

    申请日:1995-06-06

    摘要: This invention relates to therapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to peptide derivatives and analogs of somatostatin, and embodiments of such peptides labeled with technetium-99m (Tc-99m), as well as methods and kits for making, radiolabeling and using such peptides to image sites in a mammalian body. The invention also relates to peptide derivatives and analogues of somatostatin labeled with rhemium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re), and methods and kits for making, radiolabeling and using such peptides therapeutically in a mammalian body.

    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肽衍生物和类似物,以及用锝-99m(Tc-99m)标记的这些肽的实施方案,以及用于制备,放射性标记和使用这些肽成像哺乳动物体内的位点的方法和试剂盒 。 本发明还涉及用rhemium-186(186Re)和铼-188(188Re)标记的生长抑素的肽衍生物和类似物,以及用于在哺乳动物体内制备,放射性标记和使用这些肽的方法和试剂盒。