3-Amino-1,5-Bis-(2-propyl)-1,5-benzodiazepine-2,4-dione | 186490-51-7

• 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-1,5-Bis-(2-propyl)-1,5-benzodiazepine-2,4-dione
• 英文别名: 3-amino-2,4-dioxo-1,5-bis-(1-methylethyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine；3-amino-1,5-diisopropyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepine；3-amino-1,5-di(propan-2-yl)-1,5-benzodiazepine-2,4-dione
• CAS: 186490-51-7
• 化学式: C₁₅H₂₁N₃O₂
• 分子量: 275.351
• InChiKey: XDHGFWHUDRIVNC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.47
• 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-1,5-Bis-(2-propyl)-1,5-benzodiazepine-2,4-dione 、 N-[2-(3,5-二氟苯基)乙酰基]-L-丙氨酸 生成 3-[N'-(3,5-difluorophenylacetyl)-L-alaninyl]amino-2,4-dioxo-1,5-bis-(1-methylethyl)-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-(1-methylethyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine 在 palladium-carbon H2 作用下， 以 乙醇 为溶剂， 生成 3-Amino-1,5-Bis-(2-propyl)-1,5-benzodiazepine-2,4-dione
  参考文献：
  名称：

  N-(2,4-Dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3yl) -3- amides

  摘要：

  这项发明涉及由结构式I表示的新化合物，这些化合物在治疗心律失常方面非常有用。

  公开号：

  US05691331A1

文献信息

• 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
  申请人：——

  公开号：US20020045747A1

  公开（公告）日：2002-04-18

  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。
• 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。
• N-(2,4-Dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3yl) -3- amides
  申请人：Merck & Co., Inc.

  公开号：US05691331A1

  公开（公告）日：1997-11-25

  This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.

  这项发明涉及由结构式I表示的新化合物，这些化合物在治疗心律失常方面非常有用。
• Benzodiazepine derivatives as app modulators
  申请人：——

  公开号：US20040082572A1

  公开（公告）日：2004-04-29

  A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed. The compounds modulate the processing of amyloid precursor protein by &ggr;-secretase, and hence find use in the treatment or prevention of conditions associated with the deposition of &bgr;-amyloid, such as Alzheimer's disease. 1

  公开了一种式(I)的新型1,4-和1,5-苯二氮平类化合物。这些化合物调节&ggr;-分泌酶对淀粉样前体蛋白的加工作用，因此可用于治疗或预防与&bgr;-淀粉样蛋白沉积相关的疾病，如阿尔茨海默病。
• [EN] BENZODIAZEPINE DERIVATIVES AS APP MODULATORS<br/>[FR] DERIVES DE BENZODIAZEPINE UTILISES COMME MODULATEURS DE LA PROTEINE PRECURSEUR AMYLOIDE (APP)
  申请人：MERCK SHARP & DOHME

  公开号：WO2001090084A1

  公开（公告）日：2001-11-29

  A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed. The compounds modulate the processing of amyloid precursor protein by η-secretase, and hence find use in the treatment or prevention of conditions associated with the deposition of β-amyloid, such as Alzheimer's disease.

  一种新型的1,4-和1,5-苯二氮平类化合物的式(I)被揭示。这些化合物通过调节η-分泌酶对淀粉样前体蛋白的加工，因此可用于治疗或预防与β-淀粉样蛋白沉积有关的疾病，如阿尔茨海默病。