3-Amino-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine | 280568-95-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: 3-Amino-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine
• 英文别名: 3-amino-1,3,4,5-tetrahydro-1,5-dimethyl-2H-1,5-benzodiazepin-2,4-dione；3-amino-1,5-dimethyl-1,5-benzodiazepine-2,4-dione
• CAS: 280568-95-8
• 化学式: C₁₁H₁₃N₃O₂
• 分子量: 219.243
• InChiKey: ZKJACDIALNSUQY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  16
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  66.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-Amino-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine 、 methyl (+/-)-phenylglycinate hydrochloride 生成 3-[N'-(t-butoxycarbonyl)-L-alaninyl]-amino-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine
  参考文献：
  名称：

  Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds

  摘要：

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性治疗阿尔茨海默病的方法。

  公开号：

  US20020045747A1
• 作为产物：
  描述：

  3-Azido-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine 生成 3-Amino-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine
  参考文献：
  名称：

  Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds

  摘要：

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性治疗阿尔茨海默病的方法。

  公开号：

  US06528505B1

文献信息

• Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：Elan Pharmaceuticals, Inc.

  公开号：US06528505B1

  公开（公告）日：2003-03-04

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性治疗阿尔茨海默病的方法。
• Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：Elan Pharmaceuticals, Inc.

  公开号：US06509331B1

  公开（公告）日：2003-01-21

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。
• 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。
• Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting B-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：——

  公开号：US20020173504A1

  公开（公告）日：2002-11-21

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  本发明涉及抑制&bgr;-淀粉样肽的释放和/或合成的化合物，因此具有治疗阿尔茨海默病的效用。还公开了包含抑制&bgr;-淀粉样肽释放和/或合成的化合物的药物组合物，以及使用这种药物组合物预防和治疗阿尔茨海默病的方法。
• 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。