Long lasting anti-angiogenic peptides
    13.
    发明授权
    Long lasting anti-angiogenic peptides 失效
    持久的抗血管生成肽

    公开(公告)号:US07741286B2

    公开(公告)日:2010-06-22

    申请号:US11350703

    申请日:2006-02-08

    IPC分类号: A61K38/00

    摘要: Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly modified kringle 5 peptides are capable of forming a conjugate with a blood protein. Conjugates are prepared from anti-angiogenic peptides, particularly kringle 5 peptides, by combining the peptide with a reactive functional group with a blood protein. The conjugates may be formed in vivo or ex vivo. The conjugates are administered to patients to provide an anti-angiogenic effect.

    摘要翻译: 公开了修饰的抗血管生成肽。 修饰的肽能够形成肽酶稳定的抗血管生成肽。 修饰的抗血管生成肽,特别是修饰的三环5肽能够与血液蛋白形成缀合物。 通过将肽与反应性官能团与血液蛋白结合,由抗血管生成肽,特别是kringle 5肽制备缀合物。 缀合物可以在体内或离体形成。 向患者施用共轭物以提供抗血管生成作用。

    Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
    17.
    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:US06887470B1

    公开(公告)日:2005-05-03

    申请号:US09657276

    申请日:2000-09-07

    CPC分类号: C07K19/00

    摘要: A method for protecting a peptide from peptidase activity in vivo, the peptide being composed of between 2 and 50 amino acids and having a C-terminus and an N-terminus and a C-terminus amino acid and an N-terminus amino acid is described. In the first step of the method, the peptide is modified by attaching a reactive group to the C-terminus amino acid, to the N-terminus amino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable of forming a covalent bond in vivo with a reactive functionality on a blood component. In the next step, a covalent bond is formed between the reactive group and a reactive functionality on a blood component to form a peptide-blood component conjugate, thereby protecting said peptide from peptidase activity. The final step of the method involves the analyzing of the stability of the peptide-blood component conjugate to assess the protection of the peptide from peptidase activity.

    摘要翻译: 描述了一种在体内保护肽免受肽酶活性的方法,所述肽由2-50个氨基酸组成且具有C末端和N末端以及C末端氨基酸和N-末端氨基酸 。 在该方法的第一步中,通过将反应性基团连接到C末端氨基酸,N末端氨基酸或位于N末端和C末端之间的氨基酸来修饰肽, 使得修饰的肽能够在体内与血液成分上的反应性官能团形成共价键。 在下一步骤中,在反应性基团和血液成分上的反应性官能团之间形成共价键以形成肽 - 血液成分缀合物,从而保护所述肽免受肽酶活性。 该方法的最后步骤包括分析肽 - 血液成分缀合物的稳定性,以评估肽对肽酶活性的保护。

    Conjugates of opioids and endogenous carriers
    18.
    发明授权
    Conjugates of opioids and endogenous carriers 失效
    阿片样物质和内源性载体的结合物

    公开(公告)号:US06437092B1

    公开(公告)日:2002-08-20

    申请号:US09445986

    申请日:1999-12-16

    IPC分类号: C07K700

    摘要: Conjugated are prepared from antinociceptive a agents, particularly opioids or opioid analoges, more particularly deltorphins, enkephalins or analogs thereof, by combining said antinociceptive agent with a material providing a functionally reactive group capable of reacting with a blood component (preferably cell or protein). Said conjugates permit extension of the therapeutic life of the antinociceptive agent. They may be administered to patients to alleviate pain, produce analgesic effects, or assist in cases of narcotics withdrawal, and may also be used as probes for receptor activity. The administration to the patient ma be made either in vivo or ex vivo and may be performed by either introducing the derivative including the reactive functional group into the patient's vascular system or preparing such a conjugate externally (or in vitro) and introducing that conjugate to the patient's vascular system.

    摘要翻译: 通过将所述抗伤害感受剂与提供能够与血液成分(优选细胞或蛋白质)反应的功能反应性基团的材料组合,由抗感受伤害性药物,特别是阿片样物质或阿片样物质类似物,特别是去角质素,脑啡肽或类似物制备缀合物。 所述缀合物允许延长抗伤害感受剂的治疗寿命。 可以向患者施用以缓解疼痛,产生镇痛作用或辅助麻醉药物撤出的情况,也可用作受体活性的探针。 对患者的给药可以在体内或离体制备,并且可以通过将包含反应性官能团的衍生物引入患者的血管系统中或者从外部(或体外)引入该缀合物并将该缀合物引入到 患者血管系统。