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36 条记录 (耗时 0.032 秒)

    Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
    31.
    发明授权
    Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components 失效
    通过与血液成分缀合，保护内源性治疗肽免受肽酶活性的影响

    公开(公告)号：US07256253B2

    公开(公告)日：2007-08-14

    申请号：US11066697

    申请日：2005-02-25

    申请人： Dominique P. Bridon ,  Alan M. Ezrin ,  Peter G. Milner ,  Darren L. Holmes ,  Karen Thibaudeau

    发明人： Dominique P. Bridon ,  Alan M. Ezrin ,  Peter G. Milner ,  Darren L. Holmes ,  Karen Thibaudeau

    IPC分类号： A61K38/00 ,  C07K14/00

    CPC分类号： C07K19/00

    摘要： A secretin or secretin derivative protected against peptidase activity. The secretin or derivative comprises a peptidic sequence and a reactive group selected from the group consisting of succinimidyl and maleimido groups capable of reacting with an amino group, hydroxyl group or thiol group on a blood component to form a stable covalent bond. The reactive group is attached at a position along the peptidic sequence that provides, when conjugated to a blood component, a higher stability against peptidase degradation than the unconjugated secretin or derivative, and therefore an increased maintenance of the therapeutic activity compared to the unconjugated secretin or derivative. Such a compound is thus effective to provide a source of secretin having a high stability against peptidases. A method for synthesizing such a compound is also described.

    摘要翻译： 保护蛋白酶活性的促胰液素或促胰液素衍生物。 分泌素或衍生物包含肽类序列和选自能够与血液成分上的氨基，羟基或硫醇基反应形成稳定的共价键的琥珀酰亚胺基和马来酰亚胺基的反应性基团。 反应性基团连接在沿着肽序列的位置，当与血液成分缀合时，其比非共轭分泌素或衍生物具有比肽酶降解更高的稳定性，因此与未缀合的促胰液素相比，治疗活性的维持得到增加 衍生物。 因此，这样的化合物有效地提供对肽酶具有高稳定性的促胰液素来源。 还描述了合成这种化合物的方法。

    Methods for producing novel conjugates of thrombin inhibitors
    34.
    发明授权
    Methods for producing novel conjugates of thrombin inhibitors 失效
    生产凝血酶抑制剂新型缀合物的方法

    公开(公告)号：US5942620A

    公开(公告)日：1999-08-24

    申请号：US108534

    申请日：1998-07-01

    申请人： Alexander Krantz ,  Alan M. Ezrin ,  Yonghong Song

    发明人： Alexander Krantz ,  Alan M. Ezrin ,  Yonghong Song

    IPC分类号： C12N5/06 ,  A61K38/00 ,  A61K47/48 ,  A61P7/02 ,  C07K5/068 ,  C07K14/765 ,  C07K16/18 ,  C07D215/02

    CPC分类号： A61K47/48007 ,  A61K47/48238 ,  A61K47/48384

    摘要： Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have thrombin inhibition activity are provided. Specifically, the thrombin inhibitor compounds of the present invention are derivatives of the known thrombin inhibitor argatroban, which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated thrombin inhibitors thereby have extended lifetimes in the bloodstream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining thrombin inhibitory activity for extended periods of time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting thrombin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.

    摘要翻译： 提供了包含化学反应中间体的新型化合物，其可与血液成分上的可用反应性官能团反应以形成共价键，其中发现所得的共价结合的缀合物具有凝血酶抑制活性。 具体地，本发明的凝血酶抑制剂化合物是已知的凝血酶抑制剂阿加曲班的衍生物，其可以与各种血液成分上的化学反应性官能团共价连接。 与未缀合的母体药物相比，缀合的凝血酶抑制剂在血液中的寿命延长，因此与未缀合的母体药物相比，能够延长凝血酶抑制活性。 本文还提供用于抑制体内凝血酶活性的方法，包括向哺乳动物宿主的血流施用本发明的新化合物。