4-Oxoindeno[2,1-b]thiophene-6-carboxylic acid | 925931-67-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 4-Oxoindeno[2,1-b]thiophene-6-carboxylic acid
• CAS: 925931-67-5
• 化学式: C₁₂H₆O₃S
• 分子量: 230.244
• InChiKey: DABJYKPAJGGILZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  82.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• ACYLGUANIDINE DERIVATIVE OR SALT THEREOF
  申请人：Yamada Hiroyoshi

  公开号：US20100168096A1

  公开（公告）日：2010-07-01

  [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT 2B receptor and 5-HT 7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.

  [问题] 提供一种可用于预防和/或治疗与5-HT2B受体和5-HT7受体有关的疾病的化合物，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛。 [解决方法] 发现具有三环结构的酰基胍衍生物或其药学上可接受的盐具有强烈的对5-HT2B受体和5-HT7受体的拮抗作用。此外，本发明的化合物具有对两种受体的拮抗作用，与单独使用针对其中任一受体的选择性拮抗剂相比，具有更优越的药理作用。基于上述，本发明的化合物在预防和/或治疗与5-HT2B受体和5-HT7受体有关的疾病，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛方面具有用途。
• US8076348B2
  申请人：——

  公开号：US8076348B2

  公开（公告）日：2011-12-13