4-氯-7-甲基-5-氮杂吲哚 | 1082040-95-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 中文名称: 4-氯-7-甲基-5-氮杂吲哚
• 英文名称: 4-chloro-7-methyl-1H-pyrrolo[3,2-c]pyridine
• CAS: 1082040-95-6
• 化学式: C₈H₇ClN₂
• 分子量: 166.61
• InChiKey: FDDUNWBKKCPOCV-UHFFFAOYSA-N

物化性质

• 沸点：
  342.3±37.0 °C(Predicted)
• 密度：
  1.351±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  28.7
• 氢给体数：
  1
• 氢受体数：
  1

安全信息

• 危险类别：
  6.1
• 危险性防范说明：
  P261,P264,P270,P271,P280,P302+P352,P304+P340,P310,P330,P361,P403+P233,P405,P501
• 危险品运输编号：
  2811
• 危险性描述：
  H301,H311,H331
• 包装等级：
  III

反应信息

• 作为反应物：
  描述：

  4-氯-7-甲基-5-氮杂吲哚 在 [Pd(SIPr)(η³-cin)Cl] 、 水 、 potassium carbonate 、 sodium hydroxide 作用下， 以 甲醇 、 乙醇 、 水 为溶剂， 反应 1.5h， 生成 4-(7-methyl-1H-pyrrolo[3,2-c]pyridin-4-yl)benzoic acid
  参考文献：
  名称：

  WO2023/113023

  摘要：

  公开号：

文献信息

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

  公开号：WO2017024003A1

  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-氮杂吲唑化合物。更具体地，本公开涉及使用4-氮杂吲唑化合物或其类似物，治疗通过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、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条件/障碍/疾病。还提供了治疗与Wnt相关疾病状态的方法。
• [EN] 3-(1H-PYRROLO[3,2-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-C]PYRIDINES AND THERAPEUTIC USES THEREOF<br/>[FR] 3-(1H-PYRROLO[3,2-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-C]PYRIDINES ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：SAMUMED LLC

  公开号：WO2017023984A1

  公开（公告）日：2017-02-09

  6-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 6-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6-氮杂吲唑化合物。更具体地，本公开涉及使用6-氮杂吲唑化合物或其类似物，治疗通过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、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。
• [EN] 3-(1H-PYRROLO[3,2-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF<br/>[FR] 3-(1H-PYRROLO[3,2-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-B]PYRIDINES ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：SAMUMED LLC

  公开号：WO2017023987A1

  公开（公告）日：2017-02-09

  7-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 7-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.

  7-氮杂吲唑化合物用于治疗各种疾病和病理已被披露。更具体地，本公开涉及使用7-氮杂吲唑化合物或其类似物，治疗通过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，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。
• [EN] OGA INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS D'OGA
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2019243535A1

  公开（公告）日：2019-12-26

  The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors of formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.

  本发明涉及式(I)的O-GIcNAc水解酶（OGA）抑制剂。该发明还涉及包含这种化合物的药物组合物，用于制备这种化合物和组合物的方法，以及利用这种化合物和组合物预防和治疗OGA抑制对其有益的疾病的应用，特别是τ蛋白病，如阿尔茨海默病或进行性核上性麻痹症；以及伴有τ病理的神经退行性疾病，特别是由C90RF72突变引起的肌萎缩侧索硬化和颞叶前叶痴呆症。
• 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
  申请人：Samumed, LLC

  公开号：US10206908B2

  公开（公告）日：2019-02-19

  6-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 6-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 6-氮杂吲唑化合物。更具体地说，本公开涉及 6-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 信号元件的突变或失调引起的遗传性疾病和神经状况/失调/疾病。此外，还提供了治疗 Wnt 相关疾病状态的方法。