2-(4-isopropenylphenyl)-N-[(1R)-1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl]acetamide

• 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: 2-(4-isopropenylphenyl)-N-[(1R)-1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl]acetamide
• 英文别名: 2-(4-isopropenylphenyl)-N-{(1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl}acetamide；2-(4-prop-1-en-2-ylphenyl)-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl]acetamide
• 化学式: C₂₀H₂₁F₃N₂O₂
• 分子量: 378.394
• InChiKey: USJGPXLZVXNFNA-CQSZACIVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  51.2
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  乙醛肟 、 2-(4-isopropenylphenyl)-N-[(1R)-1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl]acetamide 在 N-氯代丁二酰亚胺 、 三乙胺 作用下， 反应 27.0h， 以23%的产率得到2-[4-(3,5-dimethyl-4,5-dihydro-isoxazol-5-yl)phenyl]-N-{(1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl}acetamide
  参考文献：
  名称：

  [EN] HETEROCYCLE PHENYL AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS
  [FR] ANTAGONISTES DE CANAUX CALCIQUES DE TYPE T À BASE DE PHÉNYLE AMIDE HÉTÉROCYCLIQUE

  摘要：

  本发明涉及杂环苯酰胺化合物，这些化合物是T型钙通道的拮抗剂，可用于治疗或预防涉及T型钙通道的疾病和疾病。该发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及T型钙通道的疾病中使用这些化合物和组合物。

  公开号：

  WO2009054984A1
• 作为产物：
  描述：

  2-methyl-5-(2,2,2-trifluoroethoxy)pyridine 在 盐酸 、 甲醇 、 N-羟基-7-氮杂苯并三氮唑 、 2,2,6,6-四甲基哌啶氧化物 、 水 、 对甲苯磺酸 、 copper(II) sulfate 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 、 间氯过氧苯甲酸 、 potassium bromide 作用下， 以 乙醚 、 二氯甲烷 、 氯仿 、 水 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 24.75h， 生成 2-(4-isopropenylphenyl)-N-[(1R)-1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl]acetamide
  参考文献：
  名称：

  WO2007/120729

  摘要：

  公开号：

文献信息

• Pyridyl Amide T-Type Calcium Channel Antagonists
  申请人：Barrow James C.

  公开号：US20090275550A1

  公开（公告）日：2009-11-05

  The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed 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 are involved.

  本发明涉及对T型钙通道具有拮抗作用的吡啶酰胺化合物，其在治疗或预防与T型钙通道有关的疾病和疾病中具有用途。本发明还涉及包含这些化合物的制药组合物以及使用这些化合物和组合物预防或治疗与T型钙通道有关的疾病的用途。
• Pyridyl amide T-type calcium channel antagonists
  申请人：Merck Sharp & Dohme Corp.

  公开号：US07875636B2

  公开（公告）日：2011-01-25

  The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed 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 are involved.

  本发明涉及吡啶酰胺类化合物，其是T型钙通道的拮抗剂，适用于治疗或预防涉及T型钙通道的疾病和疾病。本发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及T型钙通道的疾病中使用这些化合物和组合物。
• HETEROCYCLE PHENYL AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS
  申请人：Barrow James C.

  公开号：US20100261724A1

  公开（公告）日：2010-10-14

  The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed 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 are involved.

  本发明涉及杂环苯酰胺化合物，其为T型钙通道的拮抗剂，可用于治疗或预防涉及T型钙通道的疾病和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道的疾病中的使用。
• Heterocycle phenyl amide T-type calcium channel antagonists
  申请人：Barrow James C.

  公开号：US08637513B2

  公开（公告）日：2014-01-28

  The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed 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 are involved.

  本发明涉及杂环苯酰胺化合物，其为T型钙通道的拮抗剂，可用于治疗或预防涉及T型钙通道的疾病和疾病。本发明还涉及包含这些化合物的制药组合物及其在预防或治疗涉及T型钙通道的疾病中的使用。
• Treating essential tremor using (R)-2-(4-Isopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide
  申请人：Cavion, Inc.

  公开号：US11311522B1

  公开（公告）日：2022-04-26

  This invention relates to methods and materials for treating mammals having, or at risk of developing, one or more movement disorders (e.g., essential tremor, epilepsy, and/or Parkinson's disease). For example, compositions including one or more T-type calcium channel antagonists (e.g., one or more Cav3 antagonists such as CX-8998) are provided, as well as methods for administering such compositions to a mammal having, or at risk of developing, one or more movement disorders (e.g., essential tremor, epilepsy, and/or Parkinson's disease) to treat the mammal.

  本发明涉及治疗患有或有可能患有一种或多种运动障碍（如本质性震颤、癫痫和/或帕金森病）的哺乳动物的方法和材料。例如，本发明提供了包括一种或多种T型钙通道拮抗剂（如一种或多种Cav3拮抗剂，如CX-8998）的组合物，以及向患有或有可能患有一种或多种运动障碍（如本质性震颤、癫痫和/或帕金森病）的哺乳动物施用此类组合物以治疗该哺乳动物的方法。