2-氨基-1H-苯并咪唑-1-甲酰胺 | 72431-61-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 中文名称: 2-氨基-1H-苯并咪唑-1-甲酰胺
• 英文名称: 2-amino-benzimidazole-1-carboxylic acid amide
• 英文别名: 2-Amino-benzimidazol-1-carbonsaeure-amid；2-Aminobenzimidazole-1-carboxamide
• CAS: 72431-61-9
• 化学式: C₈H₈N₄O
• 分子量: 176.178
• InChiKey: RNKKAEFQXDGJCN-UHFFFAOYSA-N

物化性质

• 沸点：
  454℃
• 密度：
  1.59
• 闪点：
  228℃

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  86.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (2-cyanoamino-phenyl)-urea 在 水 作用下， 生成 2-氨基-1H-苯并咪唑-1-甲酰胺
  参考文献：
  名称：

  Pellizzari, Gazzetta Chimica Italiana, 1919, vol. 49 I, p. 22

  摘要：

  DOI：

文献信息

• SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS
  申请人：Mjalli Adnan M.M.

  公开号：US20110237570A1

  公开（公告）日：2011-09-29

  The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit β-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved.

  本发明提供了替代的咪唑并[1,2-b]吡啶嗪衍生物，其药学上可接受的盐，以及上述任何一种的互变异构体，这些化合物抑制β-淀粉样前体蛋白裂解酶（BACE），这可能对治疗涉及BACE的疾病，如阿尔茨海默病，具有益处。本发明还提供了包括任何这些化合物的药物组合物以及在治疗涉及BACE的疾病、疾患或症状中使用任何这些化合物和组合物的用途。
• [EN] SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS ß-SECRETASE INHIBITORS<br/>[FR] DÉRIVÉS IMIDAZO[1,2-A]PYRIDINE SUBSTITUÉS, COMPOSITIONS PHARMACEUTIQUES, ET PROCÉDÉS D'UTILISATION COMME INHIBITEURS DE LA ?-SÉCRÉTASE
  申请人：HIGH POINT PHARMACEUTICALS LLC

  公开号：WO2010126745A1

  公开（公告）日：2010-11-04

  The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.

  本发明涉及替代咪唑[1,2-a]吡啶衍生物，其药学上可接受的盐，以及这些化合物或盐的互变异构体，其抑制β-淀粉样前体蛋白裂解酶（BACE）并且可能在治疗涉及BACE的疾病，如阿尔茨海默病中有用。该发明还涉及包含这些化合物的药物组合物以及在治疗涉及BACE的这类疾病中使用这些化合物和组合物。
• SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS
  申请人：Mjalli Adnan M. M.

  公开号：US20120101093A1

  公开（公告）日：2012-04-26

  The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.

  本发明涉及取代的咪唑并[1,2-a]吡啶衍生物、其药学上可接受的盐以及这些化合物或盐的互变异构体，其抑制β-淀粉样前体蛋白裂解酶（BACE），并且可能在治疗BACE参与的疾病，如阿尔茨海默病中有用。本发明还涉及包含这些化合物的制药组合物和使用这些化合物和组合物治疗BACE参与的这些疾病的方法。
• SUBSTITUTED ISOQUINOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS
  申请人：Mjalli Adnan M. M.

  公开号：US20120101125A1

  公开（公告）日：2012-04-26

  The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.

  本发明涉及取代的异喹啉衍生物、其药学上可接受的盐以及这些化合物或盐的互变异构体，它们抑制β-淀粉样前体蛋白裂解酶（BACE）并且可能在治疗BACE参与的疾病，如阿尔茨海默病方面有用。本发明还涉及包含这些化合物的制药组合物，以及使用这些化合物和组合物在治疗BACE参与的相关疾病方面的用途。
• Degradation of benomyl, picloram, and dicamba in a conical apparatus by zero-valent iron powder
  作者：Antoine Ghauch

  DOI：10.1016/s0045-6535(00)00184-3

  日期：2001.6

  Reduction of some pesticides (benomyl, picloram, and dicamba) was studied in an aerobic batch conical pilot system to investigate the disappearance of these pesticides on contact with iron powder (20 g/l, 325-mesh). Aqueous buffered solutions of the compounds were added to the system followed by zero-valent iron powder (ZVIP), and the decline in the pesticide concentrations was monitored over time. HPLC analyses show a complete disappearance of picloram (1.20 mg/l) after 20 min of reaction. Benomyl (1.00 mg/l) and dicamba (1.25 mg/l) disappear after 25 and 40 min, respectively. The t(50) values ranged From 3 to 5.5 min, and were about slightly less than the t(1/2) values reported when the log of the relative HPLC peak area was plotted versus time, where the relative peak area was calculated by dividing the measured peak area by the initial peak area. Pathways for the degradation of the studied pesticides by ZVIP are proposed. (C) 2001 Elsevier Science Ltd. All rights reserved.