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    Gastrin Releasing Peptide Compounds
    3.
    发明申请
    Gastrin Releasing Peptide Compounds 审中-公开
    胃泌素释放肽化合物

    公开(公告)号：US20080008649A1

    公开(公告)日：2008-01-10

    申请号：US11751337

    申请日：2007-05-21

    申请人： Enrico Cappelletti ,  Luciano Lattuada ,  Karen Linder ,  Edmund Marinelli ,  Palaniappa Nanjappan ,  Adrian Nunn ,  Natarajan Raju ,  Kondareddiar Ramalingam ,  Rolf Swenson ,  Michael Tweedle ,  Mary Maddalena

    发明人： Enrico Cappelletti ,  Luciano Lattuada ,  Karen Linder ,  Edmund Marinelli ,  Palaniappa Nanjappan ,  Adrian Nunn ,  Natarajan Raju ,  Kondareddiar Ramalingam ,  Rolf Swenson ,  Michael Tweedle ,  Mary Maddalena

    IPC分类号： A61K51/08 ,  A61P35/04

    CPC分类号： C07K14/57572 ,  A61K49/085 ,  A61K49/122 ,  A61K49/14 ,  A61K51/088

    摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided. Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer, methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer.

    摘要翻译： 用于具有式MNOPG的诊断成像或治疗的新的和改进的化合物，其中M是具有以下结构的金属螯合剂：其中R 1 -R 5和FG如本文所定义（以与金属放射性核素复合的形式） NOP是含有至少一个具有环状基团，至少一个取代的胆汁酸或至少一个非α氨基酸的非α氨基酸的接头，G是GRP受体靶向肽。 在优选的实施方案中，M是Aazta金属螯合剂或其衍生物。 还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。 还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。 还提供了用于制备放射治疗剂的方法和试剂盒。 还提供了治疗前列腺肿瘤或延缓前列腺肿瘤进展的新方法，包括治疗前列腺癌骨或软组织转移的方法，治疗激素敏感性和激素难治性前列腺癌的方法，延迟激素进展的方法 敏感前列腺癌，用于促进激素敏感性前列腺癌患者的联合治疗，并减少激素敏感性前列腺癌患者异常血管通透性。

    Octapeptide bombesin analogs
    6.
    发明授权
    Octapeptide bombesin analogs 失效
    八肽铃蟾肽类似物

    公开(公告)号：US5877277A

    公开(公告)日：1999-03-02

    申请号：US337127

    申请日：1994-11-10

    申请人： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    发明人： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    IPC分类号： A61K38/00 ,  C07K7/02 ,  C07K7/08 ,  C07K7/18 ,  C07K14/575 ,  C07K14/685 ,  C07K5/00 ,  C07K7/00 ,  C07K7/06

    CPC分类号： C07K7/086 ,  C07K14/57572 ,  C07K14/685 ,  C07K7/02 ,  C07K7/18 ,  A61K38/00

    摘要： A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. Cleavage of a peptide bond in the active site of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a .beta.-amino acid, or a .gamma.-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.

    摘要翻译： 具有活性位点和负责肽结合的结合位点的生物活性水陆两栖铃蟾肽，哺乳动物胃泌素释放肽（GRP）或哺乳动物生长激素释放因子（GRF）的线性（即非循环）类似物 到目标细胞上的受体。 在天然存在的铃蟾肽，GRP或GRF的活性位点中肽键的切割对于体内生物活性是不必要的。 类似物具有以下修饰之一：（a）活性位点内的氨基酸残基的缺失和活性位点之外的氨基酸残基的修饰，（b）在活性位点内置换两个氨基酸残基 具有合成氨基酸，β-氨基酸或γ-氨基酸残基的位点，或（c）非肽键代替活性位点的氨基酸残基与相邻氨基酸残基之间的肽键 。

    Gastrin releasing peptide antagonist
    7.
    发明授权
    Gastrin releasing peptide antagonist 失效
    胃泌素释放肽拮抗剂

    公开(公告)号：US5028692A

    公开(公告)日：1991-07-02

    申请号：US343092

    申请日：1989-04-25

    申请人： Allen I. Oliff ,  Walfred S. Saari

    发明人： Allen I. Oliff ,  Walfred S. Saari

    IPC分类号： C07K7/02 ,  C07K7/08 ,  C07K14/575

    CPC分类号： C07K7/02 ,  C07K14/57572 ,  C07K7/086

    摘要： Small cell lung carcinoma cells (SCLC) contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of peptide derivatives that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting activity of GRP.

    摘要翻译： 小细胞肺癌细胞（SCLC）含有胃泌素释放肽（GRP）受体。 细胞对GRP的反应是快速增长。 我们已经发现一组作为GRP拮抗剂的肽衍生物通过阻断GRP与其受体的结合，从而抑制对GRP的生长促进活性敏感的细胞的生长。