trans-2-(3-(difluoromethoxy)phenyl)-N-({R}-1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)cyclopropanecarboxamide | 1257114-05-8

• 英文名称: trans-2-(3-(difluoromethoxy)phenyl)-N-({R}-1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)cyclopropanecarboxamide
• 英文别名: 2-[3-(difluoromethoxy)phenyl]-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl]cyclopropane-1-carboxamide
• CAS: 1257114-05-8
• 化学式: C₂₀H₁₉F₅N₂O₃
• 分子量: 430.374
• InChiKey: CKJPLHPNPBTILK-VHWKEVPUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  30
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  60.4
• 氢给体数：
  1
• 氢受体数：
  9

文献信息

• ARYL SUBSTITUTED CARBOXAMIDE DERIVATIVES AS CALCIUM OR SODIUM CHANNEL BLOCKERS
  申请人：Inoue Tadashi

  公开号：US20120101105A1

  公开（公告）日：2012-04-26

  The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Na v1.3 and Na v1.7 , and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

  本发明涉及公式(I)或其药学上可接受的盐的芳基取代羧酰胺衍生物，其具有T型钙通道或电压门控钠通道的阻滞活性，如Nav1.3和Nav1.7等Tetrodotoxin敏感(TTX-S)阻滞剂，并且在涉及T型钙通道或电压门控钠通道的疾病或疾病的治疗或预防中有用。本发明还涉及包含这些化合物的制药组合物以及在涉及T型钙通道或电压门控钠通道的疾病或疾病的预防或治疗中使用这些化合物和组合物的用途。
• US9101616B2
  申请人：——

  公开号：US9101616B2

  公开（公告）日：2015-08-11
• US9522140B2
  申请人：——

  公开号：US9522140B2

  公开（公告）日：2016-12-20