(RS)-N-(1-azabicyclo[2.2.2]oct-3-yl)(E-3-(4-methoxyphenyl)propenamide)

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: (RS)-N-(1-azabicyclo[2.2.2]oct-3-yl)(E-3-(4-methoxyphenyl)propenamide)
• 英文别名: N-(1-aza-bicyclo[2,2,2]oct-3-yl)-4-methoxycinnamamide；N-(1-aza-bicyclo[2.2.2]oct-3-yl)-4-methoxycinnamamide；(E)-N-(1-azabicyclo[2.2.2]octan-3-yl)-3-(4-methoxyphenyl)prop-2-enamide
• 化学式: C₁₇H₂₂N₂O₂
• 分子量: 286.374
• InChiKey: GERXVMRTEYKZPQ-QPJJXVBHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3-氨基奎宁 、 tetraethylamine 、 反式-4-甲氧基肉桂酸 、 氯甲酸乙酯 生成 (RS)-N-(1-azabicyclo[2.2.2]oct-3-yl)(E-3-(4-methoxyphenyl)propenamide)
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Novel piperidine derivative
  申请人：Ban Hitoshi

  公开号：US20050165057A1

  公开（公告）日：2005-07-28

  A compound of the formula (1): wherein m and n are independently an integer of 0 to 4, and m+n=4; L is cycloalkyl, substituted cycloalkyl, aromatic group, or substituted aromatic group; Y is aryl or substituted aryl; R is hydrogen, alkyl, etc.; R 31 , R 32 , R 33 , R 34 , R 35 and R 36 are the same or different and are selected, if two or more exist, independently from hydrogen, alkyl, etc., or a prodrug thereof, or a pharmaceutically acceptable salt of the same, which exhibits ACAT inhibitory activity, and is useful as an agent for treatment of hyperlipidemia and atherosclerosis.

  化合物的式子(1): 其中m和n独立地是0到4之间的整数，且m+n=4；L是环烷基，取代环烷基，芳香族基或取代芳香族基；Y是芳基或取代芳基；R是氢，烷基等；R31、R32、R33、R34、R35和R36相同或不同，如果存在两个或更多，则独立地从氢，烷基等中选择，或其前药，或其药学上可接受的盐，其表现出ACAT抑制活性，并且用作治疗高脂血症和动脉粥样硬化的药物。
• NOVEL PIPERIDINE DERIVATIVE
  申请人：Sumitomo Pharmaceuticals Company, Limited

  公开号：EP1500648A1

  公开（公告）日：2005-01-26

  A compound of the formula (1): wherein m and n are independently an integer of 0 to 4, and m+n=4; L is cycloalkyl, substituted cycloalkyl, aromatic group, or substituted aromatic group; Y is aryl or substituted aryl; R is hydrogen, alkyl, etc.; R31, R32, R33, R34, R35 and R36 are the same or different and are selected, if two or more exist, independently from hydrogen, alkyl, etc., or a prodrug thereof, or a pharmaceutically acceptable salt of the same, which exhibits ACAT inhibitory activity, and is useful as an agent for treatment of hyperlipidemia and atherosclerosis.

  式（1）的化合物： 其中 m 和 n 独立地为 0 至 4 的整数，且 m+n=4 ；L 为环烷基、取代环烷基、芳香基团或取代芳香基团；Y 为芳基或取代芳基；R 为氢、烷基等；R31、R32、R33、R34、R35 和 R36 相同或不同，且如果存在两个或多个，则独立地选自氢、烷基等、 或其原药，或其药学上可接受的盐，具有 ACAT 抑制活性，可作为治疗高脂血症和动脉粥样硬化的药物。
• Methods and compositions for treatment of central nervous system disorders
  申请人：Bencherif Merouane

  公开号：US20060160835A1

  公开（公告）日：2006-07-20

  The invention provides methods of screening for substances having an effect on a nicotine receptor by contacting a cell having a nicotine receptor with a test substance; and determining any increase or decrease in phosphorylation of Janus-Activated Kinase 2 (JAK2). An increase in phosphorylation of JAK2 indicates that the test substance stimulates the nicotine receptor, and wherein a decrease in phosphorylation of JAK2 indicates that the test substance inhibits the nicotine receptor. The invention also provides screening methods for identification of substances that affect nicotine receptor activity through activity mediated by the AT2 receptor. Related pharmaceutical compositions and methods of treatment are also provided.

  本发明提供了筛选对尼古丁受体有影响的物质的方法，方法是将具有尼古丁受体的细胞与测试物质接触；并确定Janus-Activated Kinase 2（JAK2）磷酸化的增加或减少。JAK2 磷酸化的增加表明受试物质刺激了尼古丁受体，而 JAK2 磷酸化的减少表明受试物质抑制了尼古丁受体。本发明还提供了筛选方法，用于鉴定通过 AT2 受体介导的活性影响尼古丁受体活性的物质。本发明还提供了相关的药物组合物和治疗方法。
• NEW USE AND NOVEL N-AZABICYCLO-AMIDE DERIVATIVES
  申请人：AstraZeneca AB

  公开号：EP1233964B1

  公开（公告）日：2005-06-22
• JP2003514818A
  申请人：——

  公开号：JP2003514818A

  公开（公告）日：2003-04-22