(E)-N-(1-azabicyclo[2.2.2]octan-3-yl)-3-(2-chlorophenyl)prop-2-enamide

• 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: (E)-N-(1-azabicyclo[2.2.2]octan-3-yl)-3-(2-chlorophenyl)prop-2-enamide
• 化学式: C₁₆H₁₉ClN₂O
• 分子量: 290.79
• InChiKey: JEZKVTBNTCBZAF-AATRIKPKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 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：
  32.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Acrylamide derivatives as antirussive agent
  申请人：DOMPE' FARMACEUTICI S.p.A.

  公开号：EP0581165A2

  公开（公告）日：1994-02-02

  Acrylic amides having the formula wherein Ar represents a pyridyl radical or an optionally substituted benzyl radical; Ra represents hydrogen, lower alkyl, phenyl, cyano; Q represents the tropyl or quinuclidinyl radicals optionally N-oxo substituted, are described. The compounds of formula (I) show antitussive activity.

  丙烯酸酰胺的化学式为 其中 Ar 代表吡啶基或任选取代的苄基；Ra 代表氢、低级烷基、苯基、氰基；Q 代表任选被 N-氧代取代的托品基或喹啉基。 式（I）化合物具有抗呕吐活性。
• 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
• US7067261B2
  申请人：——

  公开号：US7067261B2

  公开（公告）日：2006-06-27
• [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.