3-{4-[6-(2-piperidin-1-ylethyl)-10H-9-oxa-3-thiabenzo[f]azulen-4-ylidene]piperidin-1-yl}propionic acid | 1176739-06-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噁庚英
• 英文名称: 3-{4-[6-(2-piperidin-1-ylethyl)-10H-9-oxa-3-thiabenzo[f]azulen-4-ylidene]piperidin-1-yl}propionic acid
• 英文别名: 3-[4-[8-(2-piperidin-1-ylethyl)-4H-thieno[3,2-c][1]benzoxepin-10-ylidene]piperidin-1-yl]propanoic acid
• CAS: 1176739-06-2
• 化学式: C₂₇H₃₄N₂O₃S
• 分子量: 466.645
• InChiKey: BMFSDOXUDIPMJJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  81.2
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• PIPERIDINE DERIVATIVE
  申请人：Higashiura Kunihiko

  公开号：US20100331365A1

  公开（公告）日：2010-12-30

  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. Further, 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.

  本发明提供了一种具有优异的组胺受体拮抗作用的哌啶衍生物化合物，可用作制药组合物的活性成分，特别是抗组胺药。本发明的哌啶衍生物具有强效的组胺受体拮抗作用。此外，本发明的化合物在小鼠口服后的脑组织受体结合测试中表现出低的脑转移率，因此具有减轻中枢神经系统副作用（如嗜睡）的优越性能。本发明的哌啶衍生物非常有用作为一种具有较小中枢神经系统副作用（如嗜睡）的新型抗组胺药。
• US8377967B2
  申请人：——

  公开号：US8377967B2

  公开（公告）日：2013-02-19