(E)-3-styryl-1H-indazole-5-carbonitrile

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: (E)-3-styryl-1H-indazole-5-carbonitrile
• 英文别名: 3-((1E)-2-Phenylvinyl)-1H-indazole-5-carbonitrile；3-[(E)-2-phenylethenyl]-1H-indazole-5-carbonitrile
• 化学式: C₁₆H₁₁N₃
• 分子量: 245.283
• InChiKey: PQPZGVZTGJOYMD-SOFGYWHQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  52.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (E)-3-styryl-1H-indazole-5-carbonitrile 、 三正丁基叠氮化锡 以 甲苯 为溶剂， 生成 5-[3-((1E)-2-Phenylvinyl)-1H-Indazol-5-Yl]-2H-1,2,3,4-Tetrazole
  参考文献：
  名称：

  Indazole compounds, compositions thereof and methods of treatment therewith

  摘要：

  这项发明通常涉及使用吲唑化合物来治疗或预防与蛋白激酶相关的疾病，包括酪氨酸激酶，诸如增殖性疾病、炎症性疾病、异常血管生成及其相关疾病、动脉硬化、黄斑变性、糖尿病、肥胖、疼痛等。这些方法包括向有需要的患者施用有效量的吲唑化合物，以抑制、调节或控制酪氨酸激酶信号转导。本文中提供了一种新型的吲唑化合物或其药用可接受的盐。

  公开号：

  US20050009876A1
• 作为产物：
  描述：

  3-((1E)-2-Phenylvinyl)-1-perhydro-2H-pyran-2-yl-1H-indazole-5-carbonitrile 以 四氢呋喃 、 盐酸 为溶剂， 反应 18.0h， 生成 (E)-3-styryl-1H-indazole-5-carbonitrile
  参考文献：
  名称：

  Methods for treating, preventing and managing chronic lymphocytic leukemia with indazole compounds

  摘要：

  这项发明通常是针对使用吲唑类化合物治疗或预防慢性淋巴细胞白血病。该方法包括向需要治疗或预防慢性淋巴细胞白血病的患者给予有效量的吲唑类化合物，或其药学上可接受的盐或组合物。

  公开号：

  US20070060616A1

文献信息

• Methods for treating an inflammatory condition or inhibiting JNK
  申请人：——

  公开号：US20040127536A1

  公开（公告）日：2004-07-01

  This invention is generally directed to Indazole Derivatives having the following structure: 1 or pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of diseases and disorders that are responsive to JNK inhibition, such as an inflammatory disease or disorder. Thus, methods of treating such diseases and disorders are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

  这项发明通常涉及吲唑衍生物，具有以下结构： 1 或药用可接受的盐，其中R 1 ，R 2 和A如本文所述定义。这类化合物在治疗对JNK抑制剂有响应的广泛疾病和障碍，如炎症性疾病或障碍中具有用途。因此，还披露了治疗这些疾病和障碍的方法，以及包含一个或多个上述化合物的药物组合物。
• Indazole derivatives as JNK inhibitors and compositions and methods related thereto
  申请人：——

  公开号：US20020103229A1

  公开（公告）日：2002-08-01

  Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: 1 wherein R 1 , R 2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

  本发明公开了作为JNK选择性抑制剂的化合物。本发明的化合物是吲唑衍生物，具有以下结构： 1 其中R 1 ，R 2 和A如本文所述定义。此类化合物在治疗对JNK抑制产生响应的广泛病症方面具有用途。因此，还公开了治疗此类病症的方法，以及包含一个或多个上述化合物的药物组合物。
• Surfactant-Type Brønsted Acid Catalyzed Stereoselective Synthesis of<i>trans</i>-3-Alkenyl Indazoles from Triazenylaryl Allylic Alcohols in Water
  作者：Weijun Yang、Zhigen Yang、Lijun Xu、Lili Zhang、Xin Xu、Maozhong Miao、Hongjun Ren

  DOI：10.1002/anie.201306632

  日期：2013.12.23

  Testing the waters: An efficient dodecyl benzene sulfonic acid (DBSA) catalyzed approach to the synthesis of the title compounds in water is reported. Furthermore, upon cleavage of the pyrrolidine group from the trans‐3‐alkenyl‐2‐pyrrolidine‐2H‐indazoles with Zn in CH3COOH, trans‐3‐alkenyl‐1H‐indazoles are obtained in good to excellent yields.

  测试水域：报告了一种有效的十二烷基苯磺酸（DBSA）催化的方法，用于在水中合成标题化合物。此外，在从所述吡咯烷基团的裂解反式-3-烯基-2-吡咯烷-2- ħ用Zn -indazoles在CH 3 COOH，反式-3-烯-1- ħ -indazoles在良好获得优异的产率。
• Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith
  申请人：Signal Pharmaceuticals, LLC

  公开号：US07208513B2

  公开（公告）日：2007-04-24

  Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

  本发明揭示了具有选择性抑制JNK活性的化合物。本发明的化合物是具有以下结构的吲唑衍生物：其中R1、R2和A的定义如本文所述。这些化合物在治疗对JNK抑制有反应的广泛疾病方面具有用途。因此，本发明还揭示了治疗这些疾病的方法，以及包含上述化合物中的一个或多个化合物的制药组合物。
• Methods for treating, preventing and managing chronic lymphocytic leukemia with indazole compounds
  申请人：Bennett Brydon

  公开号：US20070060616A1

  公开（公告）日：2007-03-15

  This invention is generally directed to the use of Indazole Compounds for treating or preventing chronic lymphocytic leukemia. The methods comprise the treatment or prevention of chronic lymphocytic leukemia comprising administering an effective amount of an indazole compound, or a pharmaceutically acceptable salt or composition thereof, to a patient in need thereof.

  这项发明通常是针对使用吲唑类化合物治疗或预防慢性淋巴细胞白血病。该方法包括向需要治疗或预防慢性淋巴细胞白血病的患者给予有效量的吲唑类化合物，或其药学上可接受的盐或组合物。