2-[4-[((3R)-1-acetimidoyl-3-pyrrolidinyl)oxy]phenyl]-3-(6-amidino-1-ethyl-2-indolyl)propionic acid | 201933-36-0

• 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: 2-[4-[((3R)-1-acetimidoyl-3-pyrrolidinyl)oxy]phenyl]-3-(6-amidino-1-ethyl-2-indolyl)propionic acid
• 英文别名: 3-(6-carbamimidoyl-1-ethylindol-2-yl)-2-[4-[(3R)-1-ethanimidoylpyrrolidin-3-yl]oxyphenyl]propanoic acid
• CAS: 201933-36-0
• 化学式: C₂₆H₃₁N₅O₃
• 分子量: 461.564
• InChiKey: VZMXULILDCTQDZ-WTQRLHSKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  34
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  128
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• SORBEFACIENTS
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP0966973A1

  公开（公告）日：1999-12-29

  Pharmaceutical compositions for improving the absorption of drugs having poor absorbability in the digestive tract. The compositions contain drugs and anion exchange resins and show excellent absorbability in the digestive tract.

  药物组合物，用于提高消化道内吸收性差的药物的吸收。该组合物包含药物和阴离子交换树脂，能够在消化道内表现出极佳的吸收性。
• MEDICINAL COMPOSITION FOR PERCUTANEOUS ADMINISTRATION
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1043020A1

  公开（公告）日：2000-10-11

  A percutaneously absorbable medicinal composition comprising a percutaneous absorption enhancer and at least one member selected from the group consisting of aromatic amidine derivatives represented by formula (1): salts of the derivatives, solvates of the derivatives, and solvates of salts of the derivatives. The present invention provides a composition which exhibits high percutaneous absorbability, which can maintain an effective blood level for prolonged periods of time, which provides antithrombotic and anticoagulant effects.

  一种经皮吸收的药物组合物，包括经皮吸收增强剂以及选择自式（1）所表示的芳香族酰胺衍生物的至少一种成员：衍生物的盐，衍生物的溶剂，以及衍生物的盐的溶剂。本发明提供了一种组合物，具有高经皮吸收性，可以维持有效的血液水平长时间，具有抗血栓和抗凝血作用。
• PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP0953359A1

  公开（公告）日：1999-11-03

  The present invention is directed to a pharmaceutical composition for oral administration, comprising a basic drug, a lipophilic substance, and/or a cyclodextrin. The composition exhibits improved peroral absorption of a basic drug which is difficult to be absorbed by oral administration.

  本发明涉及一种口服药物组合物，其中包括一种碱性药物、一种亲脂性物质和/或一种环糊精。 该组合物改善了难以通过口服吸收的碱性药物的口腔吸收。
• PREVENTIVES/REMEDIES FOR MULTIPLE ORGAN FAILURE
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1110556A1

  公开（公告）日：2001-06-27

  The present invention relates to a preventive and/or therapeutic drug for hypercytokinemia, liver diseases, and syndromes caused by the aggravation of sepsis, containing an anti-thrombin agent and/or a thrombin production inhibitor as an active ingredient. The present invention is applicable to prevention of or therapy for diseases such as sepsis, severe sepsis, septic shock, and multiple organ dysfunction syndrome. More particularly, the present invention is useful for an emergency medical service, for treatment of injury caused by a traffic accident, burns, heat attacks, or severe infective diseases. In addition, the present invention is useful for prevention and treatment for hypercytokinemia and liver diseases.

  本发明涉及一种预防和/或治疗高细胞血症、肝脏疾病和败血症加重引起的综合征的药物，其活性成分含有抗凝血酶剂和/或凝血酶生成抑制剂。本发明适用于败血症、严重败血症、脓毒性休克和多器官功能障碍综合征等疾病的预防或治疗。更具体地说，本发明适用于紧急医疗服务，用于治疗交通事故、烧伤、热伤或严重感染性疾病引起的损伤。此外，本发明还可用于预防和治疗高细胞血症和肝脏疾病。
• Aromatic amidine derivatives and salts thereof
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP0540051B1

  公开（公告）日：1996-04-03