3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-(pyridin-2-yl)-2,3-dihydro-1H-1,4 benzodiazepin-2-one | 330840-01-2

• 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: 3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-(pyridin-2-yl)-2,3-dihydro-1H-1,4 benzodiazepin-2-one
• 英文别名: (+/-)-3-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino 1-methyl-5-(pyridin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one；(2R,3S)-2-(cyclopropylmethyl)-3-hydroxy-N-(1-methyl-2-oxo-5-pyridin-2-yl-3H-1,4-benzodiazepin-3-yl)heptanamide
• CAS: 330840-01-2
• 化学式: C₂₆H₃₂N₄O₃
• 分子量: 448.565
• InChiKey: GKFRMALKSQVAJV-LOMQJKJHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  33
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  94.9
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-(pyridin-2-yl)-2,3-dihydro-1H-1,4 benzodiazepin-2-one 、 3-(RS)-氨基-1,3-二氢-1-甲基-5-(吡啶-2-基)-2H-1,4-苯并二氮杂-2-酮 在 isopropyl alcohol-hexane 作用下， 生成 3-[1-oxo-2-(S)-cyclopropylmethyl-heptyl]amino-1-methyl-5-(pyridin-2-yl)-2,3-dihydro-1,4-benzodiazepine-2-one
  参考文献：
  名称：

  Substituted lactams as inhibitors of abeta protein production

  摘要：

  本发明涉及具有药物和生物影响特性的新型内酰胺化合物，其化学式为（I）。本发明还涉及这些新型化合物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，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，如阿尔茨海默病和唐氏综合症。

  公开号：

  US20080221087A1

文献信息

• Hydroxyalkanoylaminolactams and related structures as inhibitors of a beta protein production
  申请人：——

  公开号：US20020052360A1

  公开（公告）日：2002-05-02

  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)的新颖内酰胺：1及其药物组合物及其使用方法。这些新颖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，从而防止神经系统中淀粉样蛋白沉积的形成。更具体地，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。
• Hydroxyalkanoylaminolactams and related structures as inhibitors of A-beta protein production
  申请人：——

  公开号：US20030166636A1

  公开（公告）日：2003-09-04

  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)的新颖内酰胺：及其药物组合物及其使用方法。这些新颖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，从而防止神经性淀粉样蛋白沉积的形成。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障碍，如阿尔茨海默病和唐氏综合症。
• Substituted lactams as inhibitors of A beta protein production
  申请人：——

  公开号：US20020025955A1

  公开（公告）日：2002-02-28

  This invention relates to novel lactams of Formula (I): 1 having drug and bio-affecting properties, their pharmaceutical compositions and 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.

  本发明涉及具有药物和生物影响性质的新型内酰胺化合物（I）的公式，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A&bgr;-肽的产生，从而防止淀粉样蛋白质的神经沉积形成。更具体地，本发明涉及与&bgr;-淀粉样蛋白产生相关的神经疾病的治疗，例如阿尔茨海默病和唐氏综合症。
• Hydroxyalkanoylaminolactams and related structures as inhibitors of A beta protein production
  申请人：Olson E. Richard

  公开号：US20050113363A1

  公开（公告）日：2005-05-26

  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加工，更具体地抑制Aβ肽的产生，从而防止神经淀粉样蛋白沉积物的形成。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。
• Substituted lactams as inhibitors of Abeta protein production
  申请人：——

  公开号：US20040138201A1

  公开（公告）日：2004-07-15

  This invention relates to novel lactams of Formula (I): 1 having drug and bio-affecting properties, their pharmaceutical compositions and 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.

  本发明涉及具有药物和生物影响性质的新型内酰胺化合物，其化学式为(I)：1，以及它们的制药组合物和使用方法。这些新的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，如阿尔茨海默病和唐氏综合症。