(2R,3S)-N1-[6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2-(2-methylpropyl)-3-allyl-butanediamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: (2R,3S)-N1-[6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2-(2-methylpropyl)-3-allyl-butanediamide
• 英文别名: (2S,3R)-N'-(5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl)-3-(2-methylpropyl)-2-prop-2-enylbutanediamide
• 化学式: C₂₆H₃₁N₃O₃
• 分子量: 433.55
• InChiKey: HOYMESLUQGPPOQ-ZOAFEQKISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  32
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  92.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (2S,3R)-5-methyl-3-[(5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl)carbamoyl]-2-prop-2-enylhexanoic acid 在 氨 、 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 18.0h， 以55%的产率得到(2R,3S)-N1-[6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2-(2-methylpropyl)-3-allyl-butanediamide
  参考文献：
  名称：

  Succinoylaminobenzodiazepines as inhibitors of Abeta protein production

  摘要：

  这项发明涉及具有以下结构式（I）的新型内酰胺，以及它们的药物组合物和使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地说，抑制Aβ肽的产生，从而防止神经沉积物的淀粉样蛋白形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经疾病的治疗，如阿尔茨海默病和唐氏综合征。

  公开号：

  US20060025407A1

文献信息

• Succinoylamino benzodiazepines as inhibitors of Abeta protein production
  申请人：Olson E. Richard

  公开号：US20060122169A1

  公开（公告）日：2006-06-08

  This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有以下公式（I）的新型内酰胺，其制药组合物以及使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地说，抑制Aβ肽的产生，从而防止神经沉积物的淀粉样蛋白形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，例如阿尔茨海默病和唐氏综合症。
• SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF ABETA PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20080207602A1

  公开（公告）日：2008-08-28

  This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有公式（I）的新型内酰胺，它们的制药组合物及其使用方法。这些新化合物抑制淀粉样前体蛋白的加工，更具体地抑制Aβ-肽的产生，从而防止神经蛋白淀积的形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，例如阿尔茨海默病和唐氏综合症。
• SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF AB PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20090069293A1

  公开（公告）日：2009-03-12

  This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有以下化学式（I）的新型内酰胺，它们的药物组合物以及它们的使用方法。这些新化合物抑制淀粉样前体蛋白的处理，更具体地抑制Aβ-肽的产生，从而防止淀粉样蛋白的神经沉积物的形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经疾病的治疗，如阿尔茨海默病和唐氏综合症。
• SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF Abeta PROTEIN PRODUCTION
  申请人：Olson Richard E.

  公开号：US20080171735A1

  公开（公告）日：2008-07-17

  This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有公式（I）的新型内酰胺，以及它们的制药组合物和使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地抑制Aβ-肽的产生，从而防止神经沉积物的淀粉样蛋白形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，如阿尔茨海默病和唐氏综合症。
• US7053084B1
  申请人：——

  公开号：US7053084B1

  公开（公告）日：2006-05-30