5-trifluoromethyl-2,3-dihydro-1-(5-chloro-2-hydroxyphenyl)-1H-2-oxo-benzimidazole | 141797-92-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: 5-trifluoromethyl-2,3-dihydro-1-(5-chloro-2-hydroxyphenyl)-1H-2-oxo-benzimidazole
• 英文别名: 5-trifluoromethyl-1-(5-chloro-2-hydroxyphenyl)-1,3-dihydro-2H-benzimidazol-2-one；5-trifluoromethyl-1-(5-chloro-2-hydroxyphenyl)-1,3-dihydro-2H-benzimidazole-2-one；1-(5-Chloro-2-hydroxyphenyl)-5-trifluoromethyl-1,3-dihydrobenzoimidazol-2-one；3-(5-chloro-2-hydroxyphenyl)-6-(trifluoromethyl)-1H-benzimidazol-2-one
• CAS: 141797-92-4
• 化学式: C₁₄H₈ClF₃N₂O₂
• 分子量: 328.678
• InChiKey: WYLYBVMNGZOYOH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  52.6
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-trifluoromethyl-2,3-dihydro-1-(5-chloro-2-hydroxyphenyl)-1H-2-oxo-benzimidazole 在 溴 作用下， 以 溶剂黄146 为溶剂， 生成 1,3-dihydro-1-(5-chloro-3-bromo-2-hydroxyphenyl)-5-trifluoromethyl-2H-benzimidazol-2-one
  参考文献：
  名称：

  Benzimidazole derivatives, their preparation and use

  摘要：

  一种具有以下结构式的化合物##STR1##其中R.sup.1为氢、NH.sub.2或C.sub.1-6-烷基，可以是支链的；X为O、S、NCN；Y为O、S；R.sup.4、R.sup.5、R.sup.6和R.sup.7独立地为氢、卤素、CF.sub.3、NO.sub.2、NH.sub.2、OH、C.sub.1-6-烷氧基、C(.dbd.O)-苯基或SO.sub.2NR.sup.IR.sup.II，其中R.sup.I和R.sup.II独立地为氢或C.sub.1-6-烷基；R.sup.11为氢、卤素、NO.sub.2或SO.sub.2NR'R"，其中R'和R"独立地为氢或C.sub.1-6-烷基；R.sup.13为氢、卤素、苯基、CF.sub.3、NO.sub.2；R.sup.12为氢或与R.sup.13一起形成可能为芳香或部分饱和的C.sub.4-7-碳环；R.sup.14为氢或与R.sup.13一起形成可能为芳香或部分饱和的C.sub.4-7-碳环；其制药组合物，以及一种治疗哺乳动物（包括人类）对钾通道开放敏感的疾病的方法，包括向需要的哺乳动物内有效给予上述第一化合物的有效量。

  公开号：

  US05200422A1

文献信息

• [EN] INHIBITORS OF HSP90<br/>[FR] INHIBITEURS DE HSP90
  申请人：NOVARTIS AG

  公开号：WO2006010594A1

  公开（公告）日：2006-02-02

  The invention relates to the use of benzoimidazolone compounds and salts thereof in the treatment of proliferative diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, pharmaceutical preparations comprising benzoimidazolone compounds, novel benzoimidazolone compounds, and a process for the preparation of the novel benzoimidazolone compounds.

  本发明涉及使用苯并咪唑酮化合物及其盐在治疗增殖性疾病方面的应用，以及用于治疗所述疾病的药物制剂的制造，包括含有苯并咪唑酮化合物的药物制剂，新颖的苯并咪唑酮化合物，以及制备新颖苯并咪唑酮化合物的方法。
• TRAUMA THERAPY
  申请人：Dobson Geoffrey Philip

  公开号：US20090324748A1

  公开（公告）日：2009-12-31

  The invention provides a method of reducing injury to cells, tissues or organs of a body following trauma by administering a composition to the body following trauma, including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) a local anaesthetic. Also provided is a composition for reducing injury to cells, tissues or organs of a body following trauma including: (i) and (ii). The composition may be hypertonic.

  本发明提供了一种减少创伤后身体细胞、组织或器官受损的方法，包括在创伤后向身体注射一种组合物，其中包括：（i）一个钾通道开放剂或激动剂和/或腺苷受体激动剂；和（ii）一个局部麻醉剂。同时提供了一种用于减少创伤后身体细胞、组织或器官受损的组合物，包括（i）和（ii）。该组合物可以是高渗的。
• INHIBITORS OF HSP90
  申请人：Chene Patrick

  公开号：US20090069341A1

  公开（公告）日：2009-03-12

  The invention relates to the use of benzoimidazolone compounds and salts thereof in the treatment of proliferative diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, pharmaceutical preparations comprising benzoimidazolone compounds, novel benzoimidazolone compounds, and a process for the preparation of the novel benzoimidazolone compounds.

  本发明涉及在治疗增生性疾病和制造用于治疗该类疾病的药物制剂中使用苯并咪唑酮化合物及其盐，包括苯并咪唑酮化合物的药物制剂、新型苯并咪唑酮化合物和制备新型苯并咪唑酮化合物的方法。
• Improved tissue maintenance
  申请人：Hibernation Therapeutics Limited

  公开号：EP2471360A1

  公开（公告）日：2012-07-04

  The invention provides a method of reducing damage to a tissue, organ or cell from surgical procedures comprising administering a composition comprising a potassium channel opener/agonist and/or an adenosine receptor agonist (eg. adenosine) together with a local anaesthetic (eg. lignocaine) when perfusing the organ.

  本发明提供了一种减少外科手术对组织、器官或细胞的损伤的方法，包括在灌注器官时施用一种组合物，该组合物包含钾离子通道开启剂/激动剂和/或腺苷受体激动剂（如腺苷）以及局麻药（如木质素）。
• METHODS OF TREATMENT AND/OR PREVENTION OF DISORDERS AND SYMPTOMS RELATED TO BKCA AND/OR SK CHANNELOPHATHIES
  申请人：UNIVERSITE DE BORDEAUX

  公开号：EP3791873A1

  公开（公告）日：2021-03-17

  The present invention relates to compounds and compositions for use in a method of treating and/or preventing neurological or non-neurological channelopathies, i.e., pathologies which are caused specifically by defects in some of the calcium-activated potassium channels. Specific neurological channelopathies and/or synaptopathies targeted by the present invention include specific neuropsychiatric pathologies, such as particularly Fragile X Syndrome (FXS), Angelman syndrome, Williams-Beuren syndrome, autism, Autism spectrum disorders (ASDs), hyperacusis, Smith-Magenis syndrome, Prader-Willi syndrome, 7q11.23 duplication syndrome, and cri-du-chat syndrome, as well as other neuropathic disorders such as trembling, epilepsy and neuropathic pains associated and neurodegenerative diseases such as Parkinson's and Alzheimer diseases. Compounds, compositions and methods of the present invention are also particularly useful and efficient in alleviating neurological symptoms common to these neurological pathologies.

  本发明涉及用于治疗和/或预防神经性或非神经性通道病变方法的化合物和组合物，即专门由某些钙激活钾通道缺陷引起的病变。本发明所针对的特定神经通道病变和/或突触病包括特定的神经精神病理，尤其是脆性 X 综合征 (FXS)、安格曼综合征、威廉姆斯-伯伦综合征、自闭症、自闭症谱系障碍 (ASD)、听力障碍、史密斯-马吉尼斯综合征、普拉德-威利综合征、7q11.23 重复综合征、cri-du-chat 综合征，以及其他神经病理性疾病，如颤抖、癫痫和神经病理性疼痛，以及神经退行性疾病，如帕金森病和阿尔茨海默病。本发明的化合物、组合物和方法在缓解这些神经病变常见的神经症状方面也特别有用和有效。