5-bromo-1-(tetrahydro-2H-pyran-2-yl)-3a,7a-dihydro-1H-indazole-3-carbaldehyde | 1467098-46-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧烷类
• 英文名称: 5-bromo-1-(tetrahydro-2H-pyran-2-yl)-3a,7a-dihydro-1H-indazole-3-carbaldehyde
• 英文别名: 5-bromo-1-(oxan-2-yl)-3a,7a-dihydroindazole-3-carbaldehyde
• CAS: 1467098-46-9
• 化学式: C₁₃H₁₅BrN₂O₂
• 分子量: 311.178
• InChiKey: IUNURWXCEAEIKI-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：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  41.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  5-溴吲哚 在 盐酸 、 4-甲基苯磺酸吡啶 、 sodium nitrite 作用下， 以 二氯甲烷 、 水 、 丙酮 为溶剂， 反应 8.0h， 生成 5-bromo-1-(tetrahydro-2H-pyran-2-yl)-3a,7a-dihydro-1H-indazole-3-carbaldehyde
  参考文献：
  名称：

  2-(1H-INDAZOL-3-YL)-1H-IMIDAZO[4,5-C]PYRIDINE AND THERAPEUTIC USES THEREOF

  摘要：

  披露了用于治疗各种疾病和病理的吲唑化合物。更具体地，本发明涉及使用吲唑化合物或其类似物，治疗由Wnt途径信号激活所特征的疾病（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病症/疾病。还提供了治疗与Wnt相关疾病状态的方法。

  公开号：

  US20160075701A1

文献信息

• 2-(1H-INDAZOL-3-YL)-3H-IMIDAZO[4,5-B]PYRIDINE AND THERAPEUTIC USES THEREOF
  申请人：Samumed, LLC

  公开号：US20160090380A1

  公开（公告）日：2016-03-31

  Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole 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吲唑化合物。更具体地，本发明涉及使用吲唑化合物或其类似物治疗由Wnt途径信号激活所特征的疾病（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病理状况/障碍/疾病。还提供了治疗与Wnt相关疾病状态的方法。
• INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF
  申请人：SAMUMED, LLC

  公开号：US20130267495A1

  公开（公告）日：2013-10-10

  Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease 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.

  揭示了用于治疗各种疾病和病理的吲唑化合物。更具体地，本发明涉及使用吲唑化合物或其类似物治疗由Wnt途径信号激活所特征化的疾病（例如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺病和骨关节炎）、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引起的遗传疾病和神经系统疾病/疾患。还提供了治疗与Wnt相关疾病状态的方法。
• [EN] INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF<br/>[FR] INHIBITEURS D'INDAZOLE DU TRAJET DE SIGNAL DE WNT ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：SAMUMED LLC

  公开号：WO2013151708A1

  公开（公告）日：2013-10-10

  Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease 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. One embodiment disclosed herein includes a compound having the structure of Formula I:

  本发明揭示了用于治疗各种疾病和病理的吲唑化合物。更具体地，本发明涉及使用吲唑化合物或其类似物治疗由Wnt通路信号激活引起的障碍（例如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺部疾病和骨关节炎），调节由Wnt通路信号介导的细胞事件，以及由于Wnt通路和/或一个或多个Wnt信号传递组分的突变或失调而引起的遗传疾病和神经状况/紊乱/疾病。还提供了治疗Wnt相关疾病状态的方法。本文所披露的一种实施例包括具有式I结构的化合物：
• 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
  申请人：Samumed, LLC

  公开号：US10023572B2

  公开（公告）日：2018-07-17

  Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole 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吲唑化合物。更具体地说，本发明涉及一种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炎）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 信号元件的突变或失调引起的遗传疾病和神经系统疾病/失调/疾病。此外，还提供了治疗 Wnt 相关疾病状态的方法。
• 2-(1H-indazol-3-yl)-3H-imidazo[4,5-B]pyridine and therapeutic uses thereof
  申请人：Samumed, LLC

  公开号：US10280166B2

  公开（公告）日：2019-05-07

  Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole 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吲唑化合物。更具体地说，本发明涉及一种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炎）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 信号元件的突变或失调引起的遗传疾病和神经系统疾病/失调/疾病。此外，还提供了治疗 Wnt 相关疾病状态的方法。