(1R*,2S*)-2-(3-amino-2-methylpropyl)-1-(1-phenyl-1H-imidazol-4-yl)cyclopropane carboxylic acid | 1334540-68-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: (1R*,2S*)-2-(3-amino-2-methylpropyl)-1-(1-phenyl-1H-imidazol-4-yl)cyclopropane carboxylic acid
• 英文别名: 2-(3-Amino-2-methylpropyl)-1-(1-phenylimidazol-4-yl)cyclopropane-1-carboxylic acid
• CAS: 1334540-68-9
• 化学式: C₁₇H₂₁N₃O₂
• 分子量: 299.373
• InChiKey: TYNKRGKXUGBUBH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  81.1
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• CYCLOPROPANECARBOXYLIC ACID DERIVATIVE
  申请人：Nagata Tsutomu

  公开号：US20130012532A1

  公开（公告）日：2013-01-10

  A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R 1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R 2 , R 3 , and R 8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R 4 , R 5 , R 6 , R 7 , R 9 , and R 10 each independently represent a hydrogen atom or the like; and R 11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.

  以下是由下列通式（I）表示的化合物或其药学上可接受的盐，其中R1代表C1至C6烷基，该烷基可以被选自取代基A的一个至三个基团取代（取代基A：羟基、卤素基、氰基、硝基、氨基、羧基、C1至C3烷基等）；R2、R3和R8各自独立地代表氢原子或C1至C3烷基；R4、R5、R6、R7、R9和R10各自独立地代表氢原子或类似物；而R11代表氢原子或类似物。该化合物具有TAFIa酶抑制活性，可用作治疗心肌梗塞、心绞痛、急性冠状动脉综合征、脑梗死、深静脉血栓、肺栓塞等疾病的治疗药物。
• MEDICAL COMPOSITION FOR PROMOTING FIBRINOLYSIS
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3238721A1

  公开（公告）日：2017-11-01

  It is intended to provide a novel pharmaceutical composition that can promote fibrinolysis. The present invention provides a pharmaceutical composition for the promotion of fibrinolysis, comprising edoxaban or a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt. The present invention further provides a pharmaceutical composition for the promotion of fibrinolysis, comprising edoxaban or a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt and further comprising a TAFIa inhibitor.

  本发明旨在提供一种可促进纤维蛋白溶解的新型药物组合物。本发明提供了一种促进纤维蛋白溶解的药物组合物，包含埃多沙班或其药学上可接受的盐，或该化合物或该盐的水合物。本发明进一步提供了一种促进纤维蛋白溶解的药物组合物，该组合物包含埃多沙班或其药学上可接受的盐，或该化合物或盐的水合物，并进一步包含TAFIa抑制剂。
• INFLAMMATORY INTESTINAL DISEASE THERAPEUTIC AGENT
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3437641A1

  公开（公告）日：2019-02-06

  A therapeutic agent for inflammatory bowel diseases comprising as an active ingredient a compound represented by the formula (I) wherein R represents a hydrogen atom or a [1-(isobutyryloxy)ethoxy]carbonyl group or the like, or a pharmacologically acceptable salt thereof.

  一种治疗炎症性肠病的药物，其活性成分包括由式（I）代表的化合物，其中 R 代表氢原子或[1-（异丁酰氧基）乙氧基]羰基或类似物，或其药理学上可接受的盐。
• PHARMACEUTICAL COMPOSITION FOR PROMOTION OF FIBRINOLYSIS
  申请人：Daiichi Sankyo Company, Limited

  公开号：US20170368037A1

  公开（公告）日：2017-12-28

  It is intended to provide a novel pharmaceutical composition that can promote fibrinolysis. The present invention provides a pharmaceutical composition for the promotion of fibrinolysis, comprising edoxaban or a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt. The present invention further provides a pharmaceutical composition for the promotion of fibrinolysis, comprising edoxaban or a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt and further comprising a TAFIa inhibitor.
• THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASES
  申请人：DAIICHI SANKYO COMPANY, LIMITED

  公开号：US20190117624A1

  公开（公告）日：2019-04-25

  A therapeutic agent for inflammatory bowel diseases comprising as an active ingredient a compound represented by the formula (I) wherein R represents a hydrogen atom or a [1-(isobutyryloxy)ethoxy]carbonyl group or the like, or a pharmacologically acceptable salt thereof.