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53 条记录 (耗时 0.056 秒)

    Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
    23.
    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。

    Long lasting anti-angiogenic peptides
    24.
    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：US07144854B1

    公开(公告)日：2006-12-05

    申请号：US09657431

    申请日：2000-09-07

    申请人： Dominique P. Bridon ,  Michele Rasamoelisolo ,  Karen Thibaudeau ,  Xicai Huang ,  Richard Beliveau

    发明人： Dominique P. Bridon ,  Michele Rasamoelisolo ,  Karen Thibaudeau ,  Xicai Huang ,  Richard Beliveau

    IPC分类号： A61K38/00

    CPC分类号： C12N9/6408

    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。

    Methods of treating or preventing thromboses
    27.
    发明授权
    Methods of treating or preventing thromboses 有权
    治疗或预防血栓形成的方法

    公开(公告)号：US6087375A

    公开(公告)日：2000-07-11

    申请号：US330744

    申请日：1999-06-11

    申请人： Dominique P. Bridon ,  Alan Ezrin ,  Peter Milner

    发明人： Dominique P. Bridon ,  Alan Ezrin ,  Peter Milner

    IPC分类号： C12N5/06 ,  A61K38/00 ,  A61K47/48 ,  A61P7/02 ,  C07K5/068 ,  C07K14/765 ,  C07K16/18 ,  C07D215/04 ,  A61K31/4709 ,  C07D215/06

    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。

    Method of treatment of diabetes and/or obesity with reduced nausea side effect
    29.
    发明授权
    Method of treatment of diabetes and/or obesity with reduced nausea side effect 失效
    减少恶心副作用的糖尿病和/或肥胖症的治疗方法

    公开(公告)号：US08039432B2

    公开(公告)日：2011-10-18

    申请号：US11595576

    申请日：2006-11-09

    申请人： Dominique P. Bridon ,  Jean-Paul Castaigne ,  Karen Thibaudeau

    发明人： Dominique P. Bridon ,  Jean-Paul Castaigne ,  Karen Thibaudeau

    IPC分类号： A61K38/26 ,  A61K38/28 ,  A61K38/38

    CPC分类号： A61K38/26 ,  A61K47/643

    摘要： The present invention provides methods of administering an insulinotropic peptide in an amount effective to treat a disorder or condition while reducing nausea side effect by administering to a subject in need thereof an insulinotropic peptide conjugated to albumin. The present invention also provides methods of selecting a subject for administration of a conjugated insulinotropic peptide. Exemplary disorders or conditions treatable with an insulinotropic peptide include obesity and type II diabetes.

    摘要翻译： 本发明提供以有效治疗病症或病症的量施用促胰岛素肽的方法，同时通过向有需要的受试者施用与白蛋白缀合的促胰岛素肽来减轻恶心副作用。 本发明还提供了选择用于给予共轭促胰岛素肽的受试者的方法。 用促胰岛素肽治疗的示例性疾病或病症包括肥胖症和II型糖尿病。

    LONG LASTING ANTI-ANGIOGENIC PEPTIDES
    30.
    发明申请
    LONG LASTING ANTI-ANGIOGENIC PEPTIDES 审中-公开
    长寿命抗血栓肽

    公开(公告)号：US20110071082A1

    公开(公告)日：2011-03-24

    申请号：US12759153

    申请日：2010-04-13

    申请人： Dominique P. Bridon ,  Michele Rasamoelisolo ,  Karen Thibaudeau ,  Xicai Huang ,  Richard Beliveau

    发明人： Dominique P. Bridon ,  Michele Rasamoelisolo ,  Karen Thibaudeau ,  Xicai Huang ,  Richard Beliveau

    IPC分类号： A61K38/38 ,  C07K19/00 ,  A61P35/00

    CPC分类号： C07K14/005 ,  A61K38/00 ,  C07K14/605 ,  C12N2740/16122

    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。