4-{3-[2,5-dimethyl-4-(N-isopropyl-N-hydroxycarbonylmethyl-aminocarbonyl-amino)-phenyl]-propargylamino}-benzamidine | 276676-44-9

• 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: 4-{3-[2,5-dimethyl-4-(N-isopropyl-N-hydroxycarbonylmethyl-aminocarbonyl-amino)-phenyl]-propargylamino}-benzamidine
• 英文别名: 2-[[[4-[3-(4-Carbamimidoylanilino)prop-1-ynyl]-2,5-dimethylphenyl]-propan-2-ylcarbamoyl]amino]acetic acid
• CAS: 276676-44-9
• 化学式: C₂₄H₂₉N₅O₃
• 分子量: 435.526
• InChiKey: AKLLIMWWSRPHQE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  32
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  132
• 氢给体数：
  5
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4-{3-[2,5-dimethyl-4-(N-isopropyl-N-methoxycarbonylmethylaminocarbonyl-amino)-phenyl]-propargylamino}-benzamidine 在 lithium hydroxide 作用下， 以 溶剂黄146 为溶剂， 以68%的产率得到4-{3-[2,5-dimethyl-4-(N-isopropyl-N-hydroxycarbonylmethyl-aminocarbonyl-amino)-phenyl]-propargylamino}-benzamidine
  参考文献：
  名称：

  Substituted aryl and heteroaryl derivatives, their production and their use as medicines

  摘要：

  延长凝血酶时间的化合物。示例包括：(a) 雷卡-4-{3-[5-乙氧羰甲基-2-甲基-4-(2-甲基吡咯烷甲酰)-苯基]-丙炔基氨基}苯胺，(b) 雷卡-4-{3-[2,5-二甲基-4-(2-甲基吡咯烷甲酰)-苯基]-丙炔基氨基}苯胺，和(c) 4-[3-(2,5-二甲基-4-异丙羰基苯基)丙炔基氨基]苯胺。

  公开号：

  US06479524B1

文献信息

• SUBSTITUIERTE ARYL- UND HETEROARYLAMIDINDERIVATE, DEREN HERSTELLUNG UND DEREN VERWENDUNG ALS ARZNEIMITTEL
  申请人：Boehringer Ingelheim Pharma GmbH & Co.KG

  公开号：EP1140802B1

  公开（公告）日：2004-03-17
• USE OF DIPYRIDAMOLE FOR TREATMENT OF RESISTANCE TO PLATELET INHIBITORS
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP1747016A2

  公开（公告）日：2007-01-31
• USE OF DIPYRIDAMOLE IN COMBINATION WITH ANTITHROMBOTICS FOR TREATMENT AND PREVENTION OF THROMBOEMBOLIC DISEASES
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP1807086A1

  公开（公告）日：2007-07-18
• Use Of Dipyridamole For Treatment Of Resistance To Platelet Inhibitors
  申请人：Eisert Wolfgang

  公开号：US20090048173A1

  公开（公告）日：2009-02-19

  The invention relates to a method of treatment of resistance to platelet inhibitors, i.e. a method to overcome resistance of treatment with platelet inhibitors, said method comprising administering a therapeutically effective amount of dipyridamole in combination with a platelet inhibitor and, optionally, in combination with a third antithrombotic component such as direct thrombin inhibitors, factor Xa inhibitors, combined thrombin/factor Xa inhibitors, heparin, low molecular weight heparin, argatroban, bivalrudin, hirulog or polyglycans to a patient in need thereof. The invention further relates to the use of dipyridamole for the manufacture of a pharmaceutical composition for treatment of resistance to platelet inhibitors. The invention also relates to a method to diagnose resistance to treatment with platelet inhibitors, said method comprising measurement of the density of binding of Annexin V on platelets.
• Use of dipyridamole in combination with antithrombotics for treatment and prevention of thromboembolic diseases
  申请人：Eisert Wolfgang

  公开号：US20090075949A1

  公开（公告）日：2009-03-19

  The invention relates to a method of treating and preventing thromboembolic disorders, comprising administering dipyridamole in combination with an antithrombotic selected from direct thrombin inhibitors, factor Xa inhibitors and combined thrombin/factor Xa inhibitors to a patient, pharmaceutical compositions suitable for this method of treatment as well as the use of dipyridamole for the manufacture of these pharmaceutical compositions.