5-bromo-1-(tetrahydro-2H-pyran-2-yl)-N-(6-(trifluoromethyl)pyridin-3-yl)-1H-indazole-3-carboxamide | 1428066-17-4

• 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: 5-bromo-1-(tetrahydro-2H-pyran-2-yl)-N-(6-(trifluoromethyl)pyridin-3-yl)-1H-indazole-3-carboxamide
• 英文别名: 5-bromo-1-(tetrahydro-2H-pyran-2-yl)-N-(6-(trifluoromethyl) pyridin-3-yl)-1H-indazole-3-carboxamide；5-bromo-1-(oxan-2-yl)-N-[6-(trifluoromethyl)pyridin-3-yl]indazole-3-carboxamide
• CAS: 1428066-17-4
• 化学式: C₁₉H₁₆BrF₃N₄O₂
• 分子量: 469.261
• InChiKey: YRJITXZHFPMJPA-UHFFFAOYSA-N

物化性质

• 沸点：
  504.7±50.0 °C(Predicted)
• 密度：
  1.67±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  29
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  69
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  5-bromo-1-(tetrahydro-2H-pyran-2-yl)-N-(6-(trifluoromethyl)pyridin-3-yl)-1H-indazole-3-carboxamide 在 三乙基硅烷 、 potassium phosphate 、 四(三苯基膦)钯 、 三氟乙酸 作用下， 以 二氯甲烷 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 8.0h， 生成 5-(5-fluoropyridin-3-yl)-N-(6-(trifluoromethyl)pyridin-3-yl)-1H-indazole-3-carboxamide
  参考文献：
  名称：

  [EN] INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS
  [FR] INDAZOLE-3-CARBOXAMIDES ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA VOIE DE SIGNALISATION PAR WNT/Beta-CATÉNINE

  摘要：

  本文披露了用于治疗各种疾病和病理的吲唑-3-羧酰胺化合物。更具体地，本文涉及使用吲唑-3-羧酰胺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Wnt信号组分之一或多个的突变或失调而引起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。

  公开号：

  WO2013040215A1
• 作为产物：
  描述：

  5-溴吲唑-3-甲酸 在 对甲苯磺酸 、 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 反应 45.08h， 生成 5-bromo-1-(tetrahydro-2H-pyran-2-yl)-N-(6-(trifluoromethyl)pyridin-3-yl)-1H-indazole-3-carboxamide
  参考文献：
  名称：

  [EN] METHODS OF USING INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS
  [FR] PROCÉDÉS D'UTILISATION D'INDAZOLE-3-CARBOXAMIDES ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA VOIE DE SIGNALISATION WNT/β-CATÉNINE

  摘要：

  本公开涉及使用一种或多种吲唑-3-羧酰胺化合物或其盐或类似物，用于治疗独立选择自包括肌腱病、皮炎、牛皮癣、硬皮病、鱼鳞病、雷诺综合征和达里尔病的一种或多种疾病或症状；和/或促进伤口愈合。方法包括向受试者（例如，需要者）施用如本文中任何地方所述的一种或多种吲唑-3-羧酰胺化合物或其盐或类似物的治疗有效量。

  公开号：

  WO2018075858A1

文献信息

• [EN] INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS<br/>[FR] INDAZOLE-3-CARBOXAMIDES ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA VOIE DE SIGNALISATION PAR WNT/Beta-CATÉNINE
  申请人：SAMUMED LLC

  公开号：WO2013040215A1

  公开（公告）日：2013-03-21

  lndazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole-3- carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis 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.

  本文披露了用于治疗各种疾病和病理的吲唑-3-羧酰胺化合物。更具体地，本文涉及使用吲唑-3-羧酰胺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Wnt信号组分之一或多个的突变或失调而引起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。
• INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/BETA-CATENIN SIGNALING PATHWAY INHIBITORS
  申请人：Samumed, LLC

  公开号：US20140045815A1

  公开（公告）日：2014-02-13

  Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis 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.

  本发明揭示了用于治疗各种疾病和病理的吲唑并[3,2-c]吡唑-3-羧酰胺化合物。更具体地，本发明涉及使用吲唑并[3,2-c]吡唑-3-羧酰胺化合物或其类似物，治疗由Wnt通路信号激活引起的疾病（例如癌症，异常细胞增殖，血管生成和骨关节炎），调节由Wnt通路信号介导的细胞事件，以及由于Wnt通路和/或Wnt信号组分之一或多个的突变或失调引起的遗传疾病和神经系统疾病/疾病/病症。还提供了治疗Wnt相关疾病状态的方法。
• INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/Beta-CATENIN SIGNALING PATHWAY INHIBITORS
  申请人：Hood John

  公开号：US20130079329A1

  公开（公告）日：2013-03-28

  Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis 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并[3,2-c]异噁唑-3-羧酰胺化合物。更具体地，本发明涉及使用吲唑并[3,2-c]异噁唑-3-羧酰胺化合物或其类似物，治疗由Wnt途径信号激活引起的疾病（例如癌症、异常细胞增殖、血管生成和骨关节炎），调节由Wnt途径信号介导的细胞事件，以及由Wnt途径和/或一个或多个Wnt信号传导组分的突变或失调引起的遗传疾病和神经系统疾病/障碍/疾病的方法。还提供了治疗Wnt相关疾病状态的方法。
• Indazole-3-carboxamides and their use as Wnt/β-catenin signaling pathway inhibitors
  申请人：Samumed, LLC

  公开号：US08697887B2

  公开（公告）日：2014-04-15

  Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis 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.

  本发明揭示了用于治疗各种疾病和病理的吲唑并[3,4-b]吲唑-3-甲酰胺化合物。更具体地，本发明涉及使用吲唑并[3,4-b]吲唑-3-甲酰胺化合物或其类似物来治疗通过激活Wnt通路信号（例如癌症、异常细胞增殖、血管生成和骨关节炎）特征的疾病，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Wnt相关疾病状态的方法。
• Methods of using indazole-3-carb oxamides and their use as Wnt/B-catenin signaling pathway inhibitors
  申请人：Samumed, LLC

  公开号：US10806726B2

  公开（公告）日：2020-10-20

  This disclosure features the use of one or more indazole-3-carboxamide compounds or salts or analogs thereof, in the treatment of one or more diseases or conditions independently selected from the group consisting of a tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, and Darier's disease; and/or for promoting wound healing. The methods include administering to a subject (e.g., a subject in need thereof) a therapeutically effective amount of one or more indazole-3-carboxamide compounds or salts or analogs thereof as described anywhere herein.

  本发明公开了一种或多种吲唑-3-甲酰胺化合物或其盐或类似物在治疗一种或多种疾病或病症中的用途，这些疾病或病症独立地选自腱病、皮炎、银屑病、斑秃、鱼鳞病、雷诺氏综合征和达里尔病；和/或用于促进伤口愈合。这些方法包括向受试者（例如有需要的受试者）施用治疗有效量的一种或多种吲唑-3-甲酰胺化合物或其盐或类似物，如本文任何地方所述。