ethyl 2-[[(1R)-1-cyclohexyl-2-[(2S)-2-[[4-[(E)-N'-hydroxycarbamimidoyl]phenyl]-methylcarbamoyl]azetidin-1-yl]-2-oxoethyl]amino]acetate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: ethyl 2-[[(1R)-1-cyclohexyl-2-[(2S)-2-[[4-[(E)-N'-hydroxycarbamimidoyl]phenyl]-methylcarbamoyl]azetidin-1-yl]-2-oxoethyl]amino]acetate
• 化学式: C₂₄H₃₅N₅O₅
• 分子量: 473.6
• InChiKey: YKKFPCDGRUDPJE-PZJWPPBQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  34
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  138
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• Aptamer thrombin complex for use as an antidote to direct acting thrombin inhibitors
  申请人：Rheinische Friedrich-Wilhelms-Universität Bonn

  公开号：EP2980218A1

  公开（公告）日：2016-02-03

  The present invention relates to a complex formed by thrombin and a thrombin-binding aptamer, said complex is capable of neutralizing the activity of a direct acting thrombin inhibitor, and to a use as an antidote to blood anticoagulants selected from direct acting thrombin inhibitors.

  本发明涉及一种由凝血酶和凝血酶结合适配体形成的复合物，所述复合物能够中和直接作用的凝血酶抑制剂的活性，还涉及作为选自直接作用的凝血酶抑制剂的血液抗凝剂的解毒剂的用途。
• Tuneable delivery of nanoparticle bound active plasmin for the treatment of thrombosis
  申请人：Indiana University Research and Technology Corporation

  公开号：US10583104B2

  公开（公告）日：2020-03-10

  Compositions and methods for therapeutic delivery are disclosed. More particularly, the present disclosure relates to nanoparticle compositions that sequester the activity of a target molecule while leaving other domains accessible to bind targeted tissues of interest. Methods for thrombus dissolution include administering a nanoparticle reversibly coupled to a target molecule that can dissolve a blood clot. Compositions and methods for inducing blood clotting are also disclosed. Methods for inducing blood clotting include administering a nanoparticle reversibly coupled to a target molecule that can induce the formation of a blood clot. Methods for sequestering a target molecule are also disclosed. The method includes reversibly coupling a target molecule to a nanoparticle having an affinity ligand that reversibly couples the target molecule, and thus, sequesters the target molecule activity until the target molecule interacts with its substrate resulting in the release of the target molecule.

  本发明公开了用于治疗递送的组合物和方法。更具体地说，本公开涉及纳米颗粒组合物，该组合物可封闭目标分子的活性，同时保留其他可接触的结构域以结合感兴趣的目标组织。溶解血栓的方法包括施用与目标分子可逆耦合的纳米粒子，该目标分子可溶解血栓。还公开了诱导血液凝结的组合物和方法。诱导血液凝结的方法包括施用与可诱导血凝块形成的靶分子可逆耦合的纳米粒子。还公开了封存目标分子的方法。该方法包括将目标分子可逆地偶联到具有亲和配体的纳米粒子上，亲和配体可逆地偶联目标分子，从而封存目标分子的活性，直到目标分子与其底物相互作用导致目标分子释放。
• TUNEABLE DELIVERY OF NANOPARTICLE BOUND ACTIVE PLASMIN FOR THE TREATMENT OF THROMBOSIS
  申请人：Indiana University Research and Technology Corporation

  公开号：US20170189362A1

  公开（公告）日：2017-07-06

  Compositions and methods for therapeutic delivery are disclosed. More particularly, the present disclosure relates to nanoparticle compositions that sequester the activity of a target molecule while leaving other domains accessible to bind targeted tissues of interest. Methods for thrombus dissolution include administering a nanoparticle reversibly coupled to a target molecule that can dissolve a blood clot. Compositions and methods for inducing blood clotting are also disclosed. Methods for inducing blood clotting include administering a nanoparticle reversibly coupled to a target molecule that can induce the formation of a blood clot. Methods for sequestering a target molecule are also disclosed. The method includes reversibly coupling a target molecule to a nanoparticle having an affinity ligand that reversibly couples the target molecule, and thus, sequesters the target molecule activity until the target molecule interacts with its substrate resulting in the release of the target molecule.
• RECOMBINANT SERINE PROTEASES
  申请人：ACADEMISCH ZIEKENHUIS LEIDEN

  公开号：US20180340163A1

  公开（公告）日：2018-11-29

  The present invention relates to recombinant proteins having serine protease polypeptides that have serine protease activity in the presence of a serine protease inhibitor and that are able to completely or partially reverse a serine protease inhibitor effect, for example in a subject treated with a serine protease inhibitor. More specifically, described herein are recombinant proteins and methods for completely or partially reversing an anti-coagulant effect of a coagulation inhibitor.
• US8795963B2
  申请人：——

  公开号：US8795963B2

  公开（公告）日：2014-08-05