(2R,3S) N1-[(3S)-1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-yl]-2-(2-methylpropyl)-3-(cyclopentylethyl)-butanediamide

• 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: (2R,3S) N1-[(3S)-1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-yl]-2-(2-methylpropyl)-3-(cyclopentylethyl)-butanediamide
• 英文别名: (2S,3R)-2-(2-cyclopentylethyl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(2-methylpropyl)butanediamide
• 化学式: C₃₁H₄₀N₄O₃
• 分子量: 516.7
• InChiKey: SDUVBDDVKQDDPQ-ZLZBJJAKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.7
• 重原子数：
  38
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  105
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-cyclopentyl-1-iodoethane 、 (2R,3S)-N1-[1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-yl]-2-(2-methylpropyl)-3-allyl-N4-(3,5-difluorobenzyl)-butanediamide 、 琥珀酸根 、 、 3-氨基-1-甲基-5-苯基-1,3-二氢-2H-1,4-苯并二氮杂-2-酮 以After Steps 2 and 3, the title compound was isolated的产率得到(2R,3S) N1-[(3S)-1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-yl]-2-(2-methylpropyl)-3-(cyclopentylethyl)-butanediamide
  参考文献：
  名称：

  Succinoylaminobenzodiazepines as inhibitors of Abeta protein production

  摘要：

  本发明涉及具有以下式(I)的新型内酰胺，其药物组合物及使用方法。这些新化合物抑制淀粉样前体蛋白的处理，并更具体地抑制Aβ-肽的产生，从而防止神经元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，如阿尔茨海默症和唐氏综合症。

  公开号：

  US20060025407A1

文献信息

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

  公开号：US20060025407A1

  公开（公告）日：2006-02-02

  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.

  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。
• 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。
• Succinoylaminobenzodiazepines as inhibitors of Aβ protein production
  申请人：Bristol-Myers Squibb Pharma Company

  公开号：US07304049B2

  公开（公告）日：2007-12-04

  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，其药物组合物以及使用方法。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，从而防止神经元沉积淀粉样蛋白的形成。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。