(R)-N-(1-azabicyclo[2.2.2]oct-3-yl)(E-3-(2-aminophenyl)propenamide) | 340681-76-7

• 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: (R)-N-(1-azabicyclo[2.2.2]oct-3-yl)(E-3-(2-aminophenyl)propenamide)
• 英文别名: (E)-3-(2-aminophenyl)-N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]prop-2-enamide
• CAS: 340681-76-7
• 化学式: C₁₆H₂₁N₃O
• 分子量: 271.362
• InChiKey: PHZYWNWABJJERF-NFAHFFEMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  58.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  甲酸 、 (R)-N-(1-azabicyclo[2.2.2]oct-3-yl)(E-3-(2-aminophenyl)propenamide) 在 乙酸酐 作用下， 反应 72.0h， 生成 (R)-N-(1-azabicyclo[2.2.2]oct-3-yl)(E-3-(2-formamidophenyl)propenamide)
  参考文献：
  名称：

  N-azabicyclo-amide derivatives

  摘要：

  通式I的化合物，其中A代表：D代表氧或硫，R1，R2和R3的定义如规范中所述，其对映体，其药学上可接受的盐，制备它们的过程，包含它们的药物组成物以及它们在治疗中的使用，特别是在治疗或预防精神障碍和智力障碍方面的使用。

  公开号：

  US06683090B1

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。
• 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
• US6683090B1
  申请人：——

  公开号：US6683090B1

  公开（公告）日：2004-01-27
• [EN] NEW USE AND NOVEL N-AZABICYCLO-AMIDE DERIVATIVES<br/>[FR] NOUVELLE UTILISATION ET NOUVEAUX DERIVES DE N-AZABICYCLO-AMIDE
  申请人：ASTRAZENECA AB

  公开号：WO2001036417A1

  公开（公告）日：2001-05-25

  This invention relates to new use of a compound of general formula (I) wherein: A represents (II), (III), (IV), (V), (VI); D represents oxygen, or sulfur; R1 represents hydrogen or methyl; R2 represents hydrogen, or C¿1?-C4 alkyl; and R?3¿ represents (A), (B), (C), or an enantiomer thereof, and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment of prophylaxis of psychotic disorders and intellectual impairment disorders.