N-[(1S)-1-{[(3S)-3-hydroxypyrrolidin-1-yl]methyl}-2-methyl-propyl]-N,4-dimethylbenzamide | 1380101-84-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-[(1S)-1-{[(3S)-3-hydroxypyrrolidin-1-yl]methyl}-2-methyl-propyl]-N,4-dimethylbenzamide
• 英文别名: N-[(2S)-1-[(3S)-3-hydroxypyrrolidin-1-yl]-3-methylbutan-2-yl]-N,4-dimethylbenzamide
• CAS: 1380101-84-7
• 化学式: C₁₈H₂₈N₂O₂
• 分子量: 304.433
• InChiKey: WBNLLFDKTFKCBO-DLBZAZTESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  43.8
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] NEW IKACH BLOCKERS<br/>[FR] NOUVEAUX BLOQUANTS DE L'IKACH
  申请人：ASTRAZENECA AB

  公开号：WO2012074469A1

  公开（公告）日：2012-06-07

  The invention relates to compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula (I) are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.

  该发明涉及按照公式(I)的化合物或其药用可接受的盐，其中m、n、R1、R2、R3、R4、R5、x和y如本文所定义。公式(I)的化合物在药理学上作为钾通道抑制剂具有药效，特别是乙酰胆碱激活的向内整流钾通道电流的抑制剂（即IKACh阻滞剂），并被认为在治疗心律失常方面有用，特别是在尤为心室上速心律失常，如心房颤动和心房扑动的治疗中。
• COMPOUNDS AND THEIR USE AS IKACH BLOCKERS
  申请人：Bostrõm Jonas

  公开号：US20120142659A1

  公开（公告）日：2012-06-07

  The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 , x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.

  本发明涉及化合物I式： 或其药学上可接受的盐，其中m、n、R1、R2、R3、R4、R5、x和y的定义如本文所述。式I的化合物在药理学上作为钾通道抑制剂是有效的，特别是作为乙酰胆碱操作的向内整流钾通道电流（即IKACh阻滞剂），并且被认为在治疗心律失常，特别是上室性心动过速（如心房颤动和心房扑动）方面是有用的。
• US8361998B2
  申请人：——

  公开号：US8361998B2

  公开（公告）日：2013-01-29