N-(5-amidino-2-hydroxy-benzyl)-3-trifluoromethyl-4-(3-aminomethyl-1,4,5,6-tetrahydro-cyclopentapyrazol-1-yl)-benzamide | 459827-33-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(5-amidino-2-hydroxy-benzyl)-3-trifluoromethyl-4-(3-aminomethyl-1,4,5,6-tetrahydro-cyclopentapyrazol-1-yl)-benzamide
• 英文别名: 4-[3-(aminomethyl)-5,6-dihydro-4H-cyclopenta[c]pyrazol-1-yl]-N-[(5-carbamimidoyl-2-hydroxyphenyl)methyl]-3-(trifluoromethyl)benzamide
• CAS: 459827-33-9
• 化学式: C₂₃H₂₃F₃N₆O₂
• 分子量: 472.47
• InChiKey: QZOMOTSQDTVSFR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  34
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  143
• 氢给体数：
  5
• 氢受体数：
  8

文献信息

• Antithrombotic carboxylic acid amides
  申请人：——

  公开号：US20020183519A1

  公开（公告）日：2002-12-05

  Carboxylic acid amides of formula 1 having antithrombotic activity and a factor Xa-inhibiting activity. Exemplary are: 2-(5-amidino-2-hydroxy-phenyl)-N-[3-methyl-4-(2-tert-butoxycarbonylaminomethyl -benzimidazol-1-yl)-phenyl]-acetamide; 2-(5-amidino-2-hydroxy-phenyl)-N-[3-methyl-4-(2-aminomethyl-benzimidazol-1-yl)-phenyl]-acetamide; and 2-(5-amidino-2-hydroxy-phenyl)-N-[4-(4,5-dimethyl-2-oxo-2,3-dihydroimidazol-1-yl) -3-methyl-phenyl]-acetamide.

  公式1的羧酸酰胺具有抗血栓活性和Xa因子抑制活性。例如：2-(5-酰胺基-2-羟基苯基)-N-[3-甲基-4-(2-叔丁氧羰胺甲基-苯并咪唑-1-基)-苯基]-乙酰胺；2-(5-酰胺基-2-羟基苯基)-N-[3-甲基-4-(2-氨基甲基-苯并咪唑-1-基)-苯基]-乙酰胺；以及2-(5-酰胺基-2-羟基苯基)-N-[4-(4,5-二甲基-2-氧代-2,3-二氢咪唑-1-基)-3-甲基-苯基]-乙酰胺。
• NEW PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF THROMBOSIS
  申请人：Reilly A. Paul

  公开号：US20060222640A1

  公开（公告）日：2006-10-05

  The present invention relates to novel pharmaceutical compositions comprising at least one direct thrombin inhibitor and at least one additional active compound selected from the groups consisting of platelet inhibitors, low molecular weight heparins (LMWH) and heparinoids as well as unfractionated heparin, factor X a inhibitors, combined thrombin/factor X a inhibitors, fibrinogen receptor antagonists (glycolprotein IIb/IIa antagonists) and Vitamin K antagonists, optionally together with one or more pharmaceutically acceptable excipients or carriers for the treatment of thrombosis.

  本发明涉及新型药物组合物，该组合物包含至少一种直接凝血酶抑制剂和至少一种额外的活性化合物，这些化合物选自血小板抑制剂、低分子量肝素（LMWH）和肝素类以及未分馏肝素、因子 X a 抑制剂、凝血酶/因子 X a a 抑制剂、纤维蛋白原受体拮抗剂（糖蛋白 IIb/IIa 拮抗剂）和维生素 K 拮抗剂，可选择与一种或多种药学上可接受的赋形剂或载体一起用于治疗血栓。
• 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 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.