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    THERAPEUTIC PEPTIDES
    6.
    发明授权
    THERAPEUTIC PEPTIDES 失效
    肽药物

    公开(公告)号：EP0438519B1

    公开(公告)日：1998-05-06

    申请号：EP89912292.3

    申请日：1989-10-13

    申请人： The Administrators of The Tulane Educational Fund

    发明人： COY, David, H. ,  MOREAU, Jacques-Pierre ,  TAYLOR, John, E. ,  KIM, Sun, Hyuk

    IPC分类号： C07K7/02 ,  C07K14/595 ,  A61K38/16

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

    摘要： In general, the invention features a linear (i.e., non-cyclic) bombesin analog of biologically active mammalian gastrin-releasing peptide (GRP) and amphibian bombesin, having an active site and a binding site responsable for the binding of the peptide to a receptor on a target cell; cleavage of a peptide bond in the active site of naturally occuring bombesin or GRP is unnecessary for in vivo bilogical activity. The analog has one of the following modifications: (a) a deletion of a residue within the active site and a modification of a residue outside of the active site, or (b) a remplacement of one or two residues within the active site with a synthetic amino acid. The analog is capable of binding to the receptor and acting as a competitive inhibitor of the naturally occurring peptide by binding to the receptor and, by virtue of one of the modifications, failing to exhibit the in vivo biological activity of the naturally occurring peptide.

    ANALOGS OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND METHODS FOR THEIR USE
    8.
    发明公开
    ANALOGS OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND METHODS FOR THEIR USE 审中-公开
    ANALOGA DESPITUITÄRENADENYLATCYCLASE-AKTIVIERENDEN POLYPEPTIDS（PACAP）UND VERFAHREN ZU DEREN VERWENDUNG

    公开(公告)号：EP3019184A1

    公开(公告)日：2016-05-18

    申请号：EP14806816.6

    申请日：2014-06-09

    申请人： The Administrators of the Tulane Educational Fund

    发明人： COY, David, H. ,  MADERDRUT, Jerome, L.

    IPC分类号： A61K38/00 ,  A61P35/00

    CPC分类号： C07K14/4705 ,  A61K38/13 ,  A61K38/14 ,  A61K38/1816 ,  A61K45/06 ,  A61K47/64 ,  A61K49/0004 ,  A61K51/08 ,  C07K14/57563 ,  A61K2300/00

    摘要： This invention relates to analogs of pituitary adenylate cyclase-activating polypeptide (PACAP), which are agonists for the PACAP/vasoactive intestinal peptide (VIP) receptors: PAC
    1 , VPAC
    1 and VPAC
    2 receptors. These PACAP analogs can be used as prophylactic/therapeutic agents for a wide range of medical disorders. These PACAP analogs coupled to suitable radionuclides can be used in the localization, diagnosis and treatment of disseminated cancers and metastatic tumors, and coupled to small molecule therapeutics can be used as vectors for targeted drug delivery. This invention also provides pharmaceutical compositions of one or more PACAP analogs of the invention either alone or in combination with one or more other prophylactic/therapeutic agent.

    摘要翻译： 本发明涉及垂体腺苷酸环化酶活化多肽（PACAP）的类似物，其是PACAP /血管活性肠肽（VIP）受体的激动剂：PAC1，VPAC1和VPAC2受体。 这些PACAP类似物可用作广泛的医学疾病的预防/治疗剂。 耦合到合适的放射性核素的这些PACAP类似物可用于弥散性癌症和转移性肿瘤的定位，诊断和治疗，并且与小分子治疗剂相结合可用作靶向药物递送的载体。 本发明还提供本发明的一种或多种PACAP类似物的药物组合物，其单独或与一种或多种其它预防/治疗剂组合。