[4-(1-methylpiperidin-4-ylidene)-4H-3-thiabenzo[f]azulen-2-yl]carboxylic acid | 1176737-70-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 环七噻吩
• 英文名称: [4-(1-methylpiperidin-4-ylidene)-4H-3-thiabenzo[f]azulen-2-yl]carboxylic acid
• 英文别名: 2-(1-Methylpiperidin-4-ylidene)-4-thiatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),5,8,10,12-hexaene-5-carboxylic acid
• CAS: 1176737-70-4
• 化学式: C₂₀H₁₉NO₂S
• 分子量: 337.442
• InChiKey: CRVWVOZAUCFIPD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  24
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  68.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• PIPERIDINE DERIVATIVE
  申请人：Nippon Zoki Pharmaceutical Co., Ltd.

  公开号：EP2243778A1

  公开（公告）日：2010-10-27

  The present invention provides a compound a piperidine derivative having excellent histamine receptor antagonistic action, which is useful as active ingredients of a pharmaceutical composition, especially an antihistamine. The piperidine derivative of the present invention has a potent histamine receptor antagonistic action. Furfiher, the compound of the present invention shows low brain transfer even in a cerebral receptor binding test where a mouse is orally administered with the compound, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The piperidine derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.

  本发明提供了一种化合物，它是一种哌啶衍生物，具有优异的组胺受体拮抗作用，可作为药物组合物，特别是抗组胺药物的活性成分。本发明的哌啶衍生物具有强效的组胺受体拮抗作用。此外，即使在小鼠口服本发明化合物的脑受体结合试验中，本发明化合物的脑转移率也很低，因此本发明化合物具有减轻中枢神经系统副作用（如嗜睡）的优选特性。本发明的哌啶衍生物作为一种新型抗组胺药非常有用，它对中枢神经系统的副作用较小，如嗜睡。