Radiolabeled vasoactive intestinal peptide analogs for diagnosis and radiotherapy
    26.
    发明授权
    Radiolabeled vasoactive intestinal peptide analogs for diagnosis and radiotherapy 失效
    放射性标记的血管活性肠肽类似物用于诊断和放射治疗

    公开(公告)号:US06608174B1

    公开(公告)日:2003-08-19

    申请号:US09629632

    申请日:2000-07-31

    IPC分类号: A61K3816

    摘要: The present invention encompasses radiolabeled peptide analogs of vasoactive intestinal peptide (VIP) labeled with a radionuclide useful for imaging target sites within mammalian living systems. The invention particularly provides radiolabeled VIP derivatives that bind selectively to the VIP receptor on target cells. Specifically, the invention relates to the radiolabeling of VIP-receptor specific agents and their subsequent use for radiodiagnostic and radiotherapeutic purposes. The invention encompasses methods for radiolabeling these peptides with radio-nuclides and the use of these peptides as scintigraphic imaging agents. The radiolabeled VIP derivatives of the present invention exhibit pharmacological activity and therefore are useful as either imaging agent for visualization of VIP-receptor positive tumors and metastases, as a radiodiagnostic agent or as a radio-therapeutic agent for the treatment of such tumors in vivo by specifically targeting the cytotoxic radionuclide selectively to the tumor site in mammalian living systems.

    摘要翻译: 本发明包括用放射性核素标记的血管活性肠肽(VIP)的放射性标记肽类似物,其用于成像哺乳动物生物系统内的靶位点。 本发明特别提供了放射性标记的VIP衍生物,其选择性地结合靶细胞上的VIP受体。 具体地,本发明涉及VIP-受体特异性试剂的放射性标记及其随后用于放射诊断和放射治疗目的。 本发明包括用放射性核素放射性标记这些肽的方法以及这些肽作为闪烁照相成像剂的用途。 本发明的放射性标记的VIP衍生物显示药理活性,因此可用作VIP-受体阳性肿瘤和转移的可视化显像剂,作为放射诊断剂或作为放射治疗剂,用于通过 特别是将细胞毒性放射性核素选择性地靶向哺乳动物生命系统中的肿瘤部位。

    Substance P analogs for the treatment of cancer
    27.
    发明授权
    Substance P analogs for the treatment of cancer 失效
    物质P类似物治疗癌症

    公开(公告)号:US06596692B1

    公开(公告)日:2003-07-22

    申请号:US09629642

    申请日:2000-07-31

    IPC分类号: A61K3800

    CPC分类号: C07K7/22 A61K38/00

    摘要: The present invention encompasses novel synthetic peptide analogs that are antagonists to Substance P, substance P like peptides and related peptides and are useful for the treatment of cancer. The invention particularly relates to the design and synthesis of the novel substance P antagonist analogs incorporating &agr;,&agr;-dialkylated amino acids in a site specific manner. The invention encompasses methods for the generation of these peptides, compositions containing these peptides and pharmacological applications of these peptides specifically in the treatment and prevention of cancer.

    摘要翻译: 本发明包括对物质P,物质P如肽和相关肽的拮抗剂的新型合成肽类似物,并且可用于治疗癌症。 本发明特别涉及以特定方式结合α,α-二烷基化氨基酸的新物质P拮抗剂类似物的设计和合成。 本发明包括用于产生这些肽的方法,含有这些肽的组合物和这些肽的药理学应用特异性地用于治疗和预防癌症。

    Antiangiogenic drugs
    28.
    发明授权
    Antiangiogenic drugs 失效
    抗血管生成药物

    公开(公告)号:US06492330B1

    公开(公告)日:2002-12-10

    申请号:US09248381

    申请日:1999-02-11

    IPC分类号: A61K3800

    摘要: The invention relates to the use of peptides individually or in combination, for treating and/or preventing angiogenesis. It also relates to the use of peptide analogs or a combination of peptides referred to as MuJ-7 as anticancer drugs in restricting the tumor growth and spread by inhibiting tumor angiogenesis. MuJ-7, in addition inhibits metastasis through its antiangiogenic activity in all cancers. The invention also relates to a pharmaceutical composition containing either individual peptides or in combination, and methods of treatment of human beings and animals for curing and/or preventing angiogenesis.

    摘要翻译: 本发明涉及肽单独或组合用于治疗和/或预防血管生成的用途。 它还涉及肽类似物或被称为MuJ-7的肽的组合作为抗癌药物在限制肿瘤生长和通过抑制肿瘤血管生成而扩散的用途。 MuJ-7还通过其所有癌症中的抗血管生成活性抑制转移。 本发明还涉及含有单个肽或组合的药物组合物,以及用于治疗和/或预防血管生成的人和动物的治疗方法。