3-(1H-indol-2-yl)-1H-pyrazolo[4,3-b]pyridine | 1259851-18-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-b]pyridine
• CAS: 1259851-18-7
• 化学式: C₁₄H₁₀N₄
• 分子量: 234.26
• InChiKey: DMCCIGLSUATEMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  57.4
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  在 水 、 potassium carbonate 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-b]pyridine
  参考文献：
  名称：

  Identification of potent ITK inhibitors through focused compound library design including structural information

  摘要：

  A series of novel compound libraries inhibiting interleukin-2 inducible T cell kinase (ITK) were designed, synthesized and evaluated. In the first design cycle two library scaffolds were identified showing low micromolar inhibition of ITK. Further iterative design cycles including crystal structure information of ITK and structurally related kinases led to the identification of indolylindazole and indolylpyrazolopyridine compounds with low nanomolar ITK inhibition. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.09.119

文献信息

• [EN] 3-(1H-INDOL-2-YL)-1H-PYRAZOLO[4,3-B]PYRIDINES AND THERAPEUTIC USES THEREOF<br/>[FR] 3-(1H-INDOL-2-YL)-1H-PYRAZOLO[4,3-B]PYRIDINES ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：SAMUMED LLC

  公开号：WO2017023993A1

  公开（公告）日：2017-02-09

  4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

  披露了用于治疗各种疾病和病理的4-氮杂吲哚化合物。更具体地，本公开涉及使用4-氮杂吲哚化合物或其类似物，治疗通过Wnt途径信号激活表征的疾病（例如癌症、异常细胞增殖、血管生成、纤维化疾病、骨骼或软骨疾病和骨关节炎），调节由Wnt途径信号介导的细胞事件，以及由于Wnt途径和/或一个或多个Wnt信号组分的突变或失调而导致的遗传疾病和神经系统疾病/紊乱/疾病。还提供了治疗与Wnt相关疾病状态的方法。
• 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
  申请人：Samumed, LLC

  公开号：US10226453B2

  公开（公告）日：2019-03-12

  4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

  本发明公开了用于治疗各种疾病和病理的 4-氮杂吲唑化合物。更具体地说，本公开涉及 4-氮杂吲唑化合物或其类似物在治疗以 Wnt 通路信号激活为特征的疾病（如癌症、异常细胞增殖、血管生成、纤维化疾病、骨或软骨疾病以及骨关节病）中的用途、癌症、异常细胞增殖、血管生成、纤维化疾病、骨或软骨疾病和骨关节炎）、调节由 Wnt 通路信号介导的细胞事件以及由于 Wnt 通路和/或一种或多种 Wnt 信号成分的突变或失调引起的遗传性疾病和神经系统状况/失调/疾病。此外，还提供了治疗 Wnt 相关疾病状态的方法。