1-Methyl-4-[2-(2H-tetrazol-5-yl)-6H-dibenz[b,e]oxepin-11-ylidene]piperidine | 1017795-87-7

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 1-Methyl-4-[2-(2H-tetrazol-5-yl)-6H-dibenz[b,e]oxepin-11-ylidene]piperidine
• 英文别名: 1-methyl-4-[2-(2H-tetrazol-5-yl)-6H-benzo[c][1]benzoxepin-11-ylidene]piperidine
• CAS: 1017795-87-7
• 化学式: C₂₁H₂₁N₅O
• 分子量: 359.431
• InChiKey: HRIJDFUUABXLGW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  27
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  66.9
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Oxepin derivative
  申请人：Higashiura Kunihiko

  公开号：US20100004456A1

  公开（公告）日：2010-01-07

  The present invention provides a compound, an oxepin derivative having excellent histamine receptor antagonistic action, which is useful as an antihistamine. The oxepin derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low intracerebral migration even when a mouse that is orally administered with the compound is subjected to an intracerebral receptor binding test, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The oxepin 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，即一种具有出色的组胺受体拮抗作用的噁吖啶衍生物，可用作抗组胺药。本发明的噁吖啶衍生物具有强效的组胺受体拮抗作用。此外，本发明的化合物即使经口给小鼠并进行颅内受体结合试验时，也表现出低颅内迁移，因此该化合物具有减轻中枢神经系统副作用（如嗜睡）的优良特性。本发明的噁吖啶衍生物非常有用，可作为一种新型抗组胺药，其中枢神经系统的副作用（如嗜睡）更小。
• OXEPIN DERIVATIVE
  申请人：Nippon Zoki Pharmaceutical Co., Ltd.

  公开号：EP2067777A1

  公开（公告）日：2009-06-10

  The present invention provides a compound, an oxepin derivative having excellent histamine receptor antagonistic action, which is useful as an antihistamine. The oxepin derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low intracerebral migration even when a mouse that is orally administered with the compound is subjected to an intracerebral receptor binding test, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The oxepin 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，一种具有优异组胺受体拮抗作用的氧塞平衍生物，可用作抗组胺药。本发明的氧塞平衍生物具有强效的组胺受体拮抗作用。此外，即使对口服本发明化合物的小鼠进行脑内受体结合试验，本发明化合物的脑内迁移率也很低，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。本发明的奥西平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。
• US8222419B2
  申请人：——

  公开号：US8222419B2

  公开（公告）日：2012-07-17