1-[(1R)-3-methyl-1-[1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-ylcarbamoyl]-butyl]-cyclopent-3-enecarboxylic amide

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 1-[(1R)-3-methyl-1-[1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-ylcarbamoyl]-butyl]-cyclopent-3-enecarboxylic amide
• 英文别名: 1-[(2R)-4-methyl-1-[(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)amino]-1-oxopentan-2-yl]cyclopent-3-ene-1-carboxamide
• 化学式: C₂₈H₃₂N₄O₃
• 分子量: 472.587
• InChiKey: XMVLEUWQCFECLX-XEGCMXMBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  105
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-[(1R)-3-methyl-1-[1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-ylcarbamoyl]-butyl]-cyclopent-3-enecarboxylic amide 、 1,4-环己二烯 在 palladium dihydroxide 作用下， 以 甲醇 为溶剂， 生成 1-[(1R)-3-methyl-1-[1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-ylcarbamoyl]-butyl]-cyclopentanecarboxylic amide
  参考文献：
  名称：

  Lactams substituted by cyclic succinates as inhibitors of a beta protein production

  摘要：

  这项发明涉及具有式(I)的新型内内酰胺，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，从而防止淀粉样蛋白的神经沉积形成。更具体地说，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，如阿尔茨海默病和唐氏综合征。

  公开号：

  US20020137737A1
• 作为产物：
  描述：

  2,2-Diallyl-3-isobutyl-N4-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-succinamide 、 甲烷 在 Grubbs catalyst first generation 、 Ruthenium(2+);styrene;triphenylphosphane;dichloride silica gel 、 methanol-dichloromethane 作用下， 以 甲苯 、 二氯甲烷 为溶剂， 反应 8.0h， 以to give 48 mg of 32 (46%)的产率得到1-[(1R)-3-methyl-1-[1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-ylcarbamoyl]-butyl]-cyclopent-3-enecarboxylic amide
  参考文献：
  名称：

  LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Abeta PROTEIN PRODUCTION

  摘要：

  本发明涉及具有公式（I）的新型内酰胺、它们的制药组合物以及它们的使用方法。这些新型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。

  公开号：

  US20090062256A1

文献信息

• Lactams substituted by cyclic succinates as inhibitors of Abeta protein production
  申请人：Olson E. Richard

  公开号：US20050261274A1

  公开（公告）日：2005-11-24

  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，其制药组成物和使用方法。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，从而防止神经元中淀粉样蛋白的沉积形成。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。
• Lactams substituted by cyclic succinates as inhibitors of A-beta protein production
  申请人：——

  公开号：US20030119815A1

  公开（公告）日：2003-06-26

  This invention relates to novel lactams having the Formula (I): 1 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 A&bgr;-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 &bgr;-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，从而防止神经元中出现淀粉样蛋白质的沉积。更具体地说，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，如阿尔茨海默病和唐氏综合症。
• LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF ABETTA PROTEIN PRODUCTION
  申请人：Olson E. Richard

  公开号：US20080103128A1

  公开（公告）日：2008-05-01

  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.

  本发明涉及具有式(I)的新型内酰胺，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。
• Lactams substituted by cyclic succinates as inhibitors of A&bgr; protein production
  申请人：Bristol-Myers Squibb Pharma Company

  公开号：US06509333B2

  公开（公告）日：2003-01-21

  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 A&bgr;-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 &bgr;-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，它们的药物组成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加工，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系统疾病的治疗，例如阿尔茨海默病和唐氏综合症。
• US6509333B2
  申请人：——

  公开号：US6509333B2

  公开（公告）日：2003-01-21