3-amino-7-chloro-1,3-dihydro-1-methyl-5-(2-chlorophenyl)-2H-1,4-benzodiazepin-2-one | 253185-55-6

• 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-7-chloro-1,3-dihydro-1-methyl-5-(2-chlorophenyl)-2H-1,4-benzodiazepin-2-one
• 英文别名: 3-amino-7-chloro-5-(2-chlorophenyl)-1,3-dihydro-1-methyl-2H-1,4-benzodiazepin-2-one；3-amino-7-chloro-5-(2-chlorophenyl)-1-methyl-3H-1,4-benzodiazepin-2-one
• CAS: 253185-55-6
• 化学式: C₁₆H₁₃Cl₂N₃O
• 分子量: 334.205
• InChiKey: VEDQVBVXZOZLBT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  58.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-amino-7-chloro-1,3-dihydro-1-methyl-5-(2-chlorophenyl)-2H-1,4-benzodiazepin-2-one 、 4-二甲氨基-1-萘异硫氰酸酯 在 乙醚 作用下， 以 1,1-二氯乙烷 为溶剂， 反应 4.0h， 以the title compound was obtained as a colorless solid (35 mg, 60%)的产率得到N-[7-chloro-5-(2-chlorophenyl)-2,3-dihydro-1-methyl-2-oxo-1H-1,4-benzodiazepin-3-yl]-N'-[4-(dimethylamino)-1-naphthalenyl]-thiourea
  参考文献：
  名称：

  Benzodiazepine derivatives, preparation thereof and use thereof

  摘要：

  化合物的公式（I），其中R1、R3、R4、R5和X如规范所定义，以及包括该化合物的盐、对映体和药物组合物已被制备。它们在治疗中很有用，特别是在疼痛管理方面。

  公开号：

  US07375101B2
• 作为产物：
  描述：

  3-(benzyloxycarbonyl)-amino-7-chloro-2,3-dihydro-1-methyl-5-(2-chlorophenyl)-1H-1,4-benzodiazepin-2-one 在 氢溴酸 、 potassium carbonate 作用下， 以 溶剂黄146 、 水 、 乙酸乙酯 为溶剂， 反应 5.0h， 生成 3-amino-7-chloro-1,3-dihydro-1-methyl-5-(2-chlorophenyl)-2H-1,4-benzodiazepin-2-one
  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：

  公开号：

  EP0951466B1

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。
• 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。
• 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：US20040106598A1

  公开（公告）日：2004-06-03

  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 that include 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β-淀粉样肽释放和/或合成的化合物，因此在治疗阿尔茨海默病方面具有用途。还公开了包括抑制β-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。
• 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：US20020111343A1

  公开（公告）日：2002-08-15

  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.

  本发明涉及一种抑制β-淀粉样肽释放和/或合成的化合物，因此具有治疗阿尔茨海默病的效用。本发明还涉及包含抑制β-淀粉样肽释放和/或合成的化合物的制药组合物，以及使用这种制药组合物预防和治疗阿尔茨海默病的方法。
• Heterocyclic 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：US20030130188A1

  公开（公告）日：2003-07-10

  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.

  本发明揭示了一些化合物，可以抑制&bgr;-淀粉样肽的释放和/或合成，因此在治疗阿尔茨海默病方面具有实用性。本发明还揭示了包含抑制&bgr;-淀粉样肽释放和/或合成的化合物的制药组合物，以及使用这些制药组合物预防和治疗阿尔茨海默病的方法。