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    Ion channel modulating activity I
    3.
    发明授权
    Ion channel modulating activity I 有权
    离子通道调节活性

    公开(公告)号：US08207219B2

    公开(公告)日：2012-06-26

    申请号：US12689909

    申请日：2010-01-19

    申请人： David Fedida ,  Gregory N. Beatch ,  Alan M. Ezrin ,  Peter M. R. Orth ,  Christian Hesketh

    发明人： David Fedida ,  Gregory N. Beatch ,  Alan M. Ezrin ,  Peter M. R. Orth ,  Christian Hesketh

    IPC分类号： A61K31/40

    CPC分类号： A61K31/40 ,  A61K31/455 ,  A61K31/4965 ,  A61K31/519 ,  C07D207/12

    摘要： Methods, compositions, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias. In these methods, early afterdepolarizations and prolongation of QT interval may be reduced or eliminated by administering ion channel modulating compounds to a subject in need thereof. The ion channel modulating compounds may be cycloalkylamine ether compounds, particularly cyclohexylamine ether compounds. Also described are compositions of ion channel modulating compounds and drugs which induce early afterdepolarizations, prolongation of QT interval and/or Torsades de Pointes.

    摘要翻译： 用于治疗或预防心律失常的方法，组合物，给药方案和给药途径。 在这些方法中，可以通过向有需要的受试者施用离子通道调节化合物来减少或消除早期后消极和延长QT间期。 离子通道调节化合物可以是环烷基胺醚化合物，特别是环己胺醚化合物。 还描述了诱导早期后极化，延长QT间期和/或Torsades de Pointes的离子通道调节化合物和药物的组合物。

    Ion channel modulating activity I
    4.
    发明授权
    Ion channel modulating activity I 有权
    离子通道调节活性

    公开(公告)号：US07674820B2

    公开(公告)日：2010-03-09

    申请号：US10914864

    申请日：2004-08-09

    申请人： David Fedida ,  Gregory N Beatch ,  Alan M Ezrin ,  Peter M R Orth ,  Christian Hesketh

    发明人： David Fedida ,  Gregory N Beatch ,  Alan M Ezrin ,  Peter M R Orth ,  Christian Hesketh

    IPC分类号： A61K31/40

    CPC分类号： A61K31/40 ,  A61K31/455 ,  A61K31/4965 ,  A61K31/519 ,  C07D207/12

    摘要： Methods, compositions, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias. In these methods, early afterdepolarizations and prolongation of QT interval may be reduced or eliminated by administering ion channel modulating compounds to a subject in need thereof. The ion channel modulating compounds may be cycloalkylamine ether compounds, particularly cyclohexylamine ether compounds. Also described are compositions of ion channel modulating compounds and drugs which induce early afterdepolarizations, prolongation of QT interval and/or Torsades de Pointes.

    摘要翻译： 用于治疗或预防心律失常的方法，组合物，给药方案和给药途径。 在这些方法中，可以通过向有需要的受试者施用离子通道调节化合物来减少或消除早期后消极和延长QT间期。 离子通道调节化合物可以是环烷基胺醚化合物，特别是环己胺醚化合物。 还描述了诱导早期后极化，延长QT间期和/或Torsades de Pointes的离子通道调节化合物和药物的组合物。

    Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
    5.
    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

    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： A61K38/54 ,  A61K39/395 ,  C07K14/47 ,  C07K16/18 ,  C07K16/28 ,  C07K19/00

    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
    6.
    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

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

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

    IPC分类号： C07K700

    CPC分类号： C07K14/70 ,  A61K38/00 ,  A61K47/64 ,  C07K14/665 ,  C07K2319/00

    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。

    Methods and compositions for producing novel conjugates of thrombin inhibitors and endogenous carriers resulting in anti-thrombins with extended lifetimes
    7.
    发明授权
    Methods and compositions for producing novel conjugates of thrombin inhibitors and endogenous carriers resulting in anti-thrombins with extended lifetimes 失效
    用于产生凝血酶抑制剂和内源性载体的新型缀合物的方法和组合物，导致具有延长的使用寿命的抗血栓素

    公开(公告)号：US06277863B1

    公开(公告)日：2001-08-21

    申请号：US09599379

    申请日：2000-06-22

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

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

    IPC分类号： A01N4342

    CPC分类号： A61K47/6803 ,  A61K47/51 ,  A61K47/62

    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。

    Methods and compositions for producing novel conjugates of thrombin inhibitors and endogenous carriers resulting in anti-thrombins with extended lifetimes
    8.
    发明授权
    Methods and compositions for producing novel conjugates of thrombin inhibitors and endogenous carriers resulting in anti-thrombins with extended lifetimes 失效
    用于产生凝血酶抑制剂和内源性载体的新型缀合物的方法和组合物，导致具有延长的使用寿命的抗血栓素

    公开(公告)号：US5840733A

    公开(公告)日：1998-11-24

    申请号：US674315

    申请日：1996-07-01

    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 ,  A61K31/415 ,  C07D401/06

    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。

    Uses of ion channel modulating compounds
    10.
    发明授权
    Uses of ion channel modulating compounds 有权
    使用离子通道调节化合物

    公开(公告)号：US07820712B2

    公开(公告)日：2010-10-26

    申请号：US11947679

    申请日：2007-11-29

    申请人： Gregory N. Beatch ,  Alan M. Ezrin

    发明人： Gregory N. Beatch ,  Alan M. Ezrin

    IPC分类号： A61K31/40

    CPC分类号： A61K31/455 ,  A61K31/40 ,  A61K31/4965 ,  A61K31/519 ,  C07D207/12

    摘要： Methods, formulations, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias, including the treatment or prevention of atrial fibrillation. In these methods, the disease or condition is treated or prevented by administering one or more ion channel modulating compounds to a subject, where the ion channel modulating compound or compounds produce specific plasma levels in the subject. The ion channel modulating compounds may be cycloalkylamine ether compounds, particularly cyclohexylamine ether compounds.

    摘要翻译： 用于治疗或预防心律失常的方法，制剂，给药方案和给药途径，包括治疗或预防心房颤动。 在这些方法中，通过向受试者施用一种或多种离子通道调节化合物来治疗或预防疾病或病症，其中离子通道调节化合物或化合物在受试者中产生特异性血浆水平。 离子通道调节化合物可以是环烷基胺醚化合物，特别是环己胺醚化合物。