N-(4-{2-[3-(hydroxymethyl)phenyl]ethyl}-1,3-thiazol-2-yl)acetamide | 1174632-89-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-(4-{2-[3-(hydroxymethyl)phenyl]ethyl}-1,3-thiazol-2-yl)acetamide
• 英文别名: N-(4-(3-(hydroxymethyl)phenethyl)thiazol-2-yl)acetamide；N-[4-[2-[3-(hydroxymethyl)phenyl]ethyl]-1,3-thiazol-2-yl]acetamide
• CAS: 1174632-89-3
• 化学式: C₁₄H₁₆N₂O₂S
• 分子量: 276.359
• InChiKey: ANLPTARYAXASDH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  90.5
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• GUANIDINE COMPOUND
  申请人：Astellas Pharma Inc.

  公开号：US20130143860A1

  公开（公告）日：2013-06-06

  [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.

  [问题]本发明提供一种化合物，用作药物组合物的活性成分，特别是用于预防和/或治疗与VAP-1相关的疾病的药物组合物。 [解决方法]本发明人对具有VAP-1抑制活性的化合物进行了深入研究，结果发现本发明的化合物或其盐表现出优异的VAP-1抑制活性，可用于预防和/或治疗与VAP-1相关的疾病，特别是糖尿病肾病或糖尿病黄斑水肿，从而完成了本发明。此外，本发明涉及一种药物组合物，特别是用于预防和/或治疗与VAP-1相关的疾病的药物组合物，其包括本发明的化合物或其盐和赋形剂。
• THIAZOLE DERIVATIVE AND USE THEREOF AS VAP-1 INHIBITOR
  申请人：Matsukawa Tatsuya

  公开号：US20110015240A1

  公开（公告）日：2011-01-20

  The invention provides a thiazole derivative useful as a VAP-1 inhibitor, as well as a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like, a method of inhibiting VAP-1 in a subject, and a method for the prophylaxis or treatment of VAP-1 associated disease in a subject. The thiazole derivative is a compound represented by the formula (I): R 1 —NH—X—Y—Z wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.

  本发明提供了一种噻唑衍生物，可用作VAP-1抑制剂，以及用于预防或治疗VAP-1相关疾病等的药物，用于在受体中抑制VAP-1的方法以及用于预防或治疗受体中VAP-1相关疾病的方法。该噻唑衍生物是由式（I）表示的化合物：R1-NH-X-Y-Z，其中每个符号如规范中所定义，或其药学上可接受的盐。
• Thiazole Derivative and use thereof as VAP-1 Inhibitor
  申请人：R-Tech Ueno, Ltd.

  公开号：EP2639229B1

  公开（公告）日：2014-11-26
• US8507690B2
  申请人：——

  公开号：US8507690B2

  公开（公告）日：2013-08-13
• US9051283B2
  申请人：——

  公开号：US9051283B2

  公开（公告）日：2015-06-09