Method for the preparation of GYK-DTPA
    5.
    依法登记的发明
    Method for the preparation of GYK-DTPA 失效
    gyk-dtpa的制备方法

    公开(公告)号:USH1312H

    公开(公告)日:1994-05-03

    申请号:US890519

    申请日:1992-05-28

    IPC分类号: C07K5/083 A61K37/02

    CPC分类号: C07K5/0806 Y02P20/55

    摘要: Disclosed herein is a novel method for preparing a DPTA tripeptide-chelator. In particular, a method for preparing GYK-DTPA is described. The method disclosed herein is an improvement over the known methods of preparation based on the cost and labor savings of the present invention. The present invention utilizes t-butyloxycarbonyl (Boc) protecting groups to facilitate the polypeptide-chelator production.

    摘要翻译: 本文公开了一种制备DPTA三肽螯合剂的新方法。 具体地说,描述了制备GYK-DTPA的方法。 本文公开的方法是基于本发明的成本和劳动力节省对已知的制备方法的改进。 本发明利用叔丁氧基羰基(Boc)保护基来促进多肽 - 螯合剂生产。

    Treatment methods using metal-binding targeted polypeptide constructs
    7.
    发明授权
    Treatment methods using metal-binding targeted polypeptide constructs 失效
    使用金属结合靶向多肽构建体的治疗方法

    公开(公告)号:US5609847A

    公开(公告)日:1997-03-11

    申请号:US480370

    申请日:1995-06-07

    摘要: The invention relates to a method of treating a patient in need thereof, including a need for diagnosis or treatment, comprising the administration of a metal complex of a polypeptide construct. The construct comprises a compound of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone,"P" is a polypeptide capable of targeting particular-cells, tissues or organs of the body,"A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group,R, R', and R" may be the same or different and may be hydrogen or an aliphatic group,m is an integer .gtoreq.2, provided that the groups R, R', R", L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain,n is an integer .gtoreq.0;or a pharmaceutically acceptable salt thereof. The constructs of the present invention are capable of binding a variety of metallic species.

    摘要翻译: 本发明涉及治疗有需要的患者的方法,包括需要诊断或治疗,包括施用多肽构建体的金属络合物。 构建体包含式(I)的化合物:ckbone,“P”是能够靶向身体的特定细胞,组织或器官的多肽,“A”可以是-NR'-NR“ - 或 其中L可以是脂族或芳族连接基团的基团-NR'-NR“-L-可以相同或不同,并且可以是氢或脂族基团,m是 整数> / = 2,条件是给定链的基团R,R',R“,L和”P“可以相同或不同于基团R,R',R”,L和“ P“,n是整数> / = 0; 或其药学上可接受的盐。 本发明的构建体能够结合各种金属物质。

    Metal-binding targeted polypeptide constructs
    10.
    发明授权
    Metal-binding targeted polypeptide constructs 失效
    金属结合靶向多肽构建体

    公开(公告)号:US5593656A

    公开(公告)日:1997-01-14

    申请号:US487221

    申请日:1995-06-07

    摘要: This invention relates to the preparation and use of novel open-chain or cyclic polypeptide constructs in which two or more polypeptide chains, in an open-chain construct, or one or more chains, in a cyclic construct, are chemically derivatized such that the resulting construct exhibits both metal-binding capability and tissue-, organ- or cell-targeting selectivity. In particular, the polypeptide constructs of the present invention comprise compounds of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone, "P" is a polypeptide capable of targeting particular cells, tissues or organs of the body, "A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group, R, R', and R" may be the same or different and may be hydrogen or an aliphatic group, m is an integer.gtoreq.2, provided that the groups R, R', R", L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain, n is an integer.gtoreq.0; or a pharmaceutically acceptable salt thereof. The constructs of the present invention are capable of binding a variety of metallic species.

    摘要翻译: 本发明涉及新型开链或环状多肽构建体的制备和应用,其中开链构建体中的两个或多个多肽链或环状构建体中的一个或多个链化学衍生化,使得得到 构建体表现出金属结合能力和组织,器官或细胞靶向选择性。 特别地,本发明的多肽构建体包含式(I)的化合物:其中“B”是烃主链,“P”是能够靶向特定细胞,组织或 身体的器官“A”可以是基团-NR'-NR“ - 或基团-NR'-NR”-L-,其中L可以是脂族或芳族连接基团,R,R' 并且R“可以相同或不同,并且可以是氢或脂族基团,m是整数> / = 2,条件是给定链的基团R,R',R”,L和“P” 可以与另一个链的基团R,R',R“,L和”P“相同或不同,n是整数> / = 0; 或其药学上可接受的盐。 本发明的构建体能够结合各种金属物质。