6-bromo-3-fluoro-1H-indole-2-carboxylic acid | 2116286-77-0

• 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: 6-bromo-3-fluoro-1H-indole-2-carboxylic acid
• CAS: 2116286-77-0
• 化学式: C₉H₅BrFNO₂
• 分子量: 258.047
• InChiKey: RGHRHWXLBYZXIS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  53.1
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  ethyl 6-bromo-3-fluoro-1H-indole-2-carboxylate 在 lithium hydroxide monohydrate 、 水 作用下， 以 四氢呋喃 为溶剂， 反应 5.0h， 生成 6-bromo-3-fluoro-1H-indole-2-carboxylic acid
  参考文献：
  名称：

  [EN] COMPOUNDS USEFUL AS RET INHIBITORS
  [FR] COMPOSÉS UTILISÉS COMME INHIBITEURS DE RET

  摘要：

  本发明涉及式I的化合物，其作为RET（重排转录）激酶酶活性的抑制剂：式I其中HET，键a，b，c和d，X1，X2，X3，X4，R2和R3在此均有所定义。本发明还涉及制备这些化合物的过程，包括它们的制药组合物，以及它们在治疗增殖性疾病（如癌症）以及其他涉及RET激酶活性的疾病或病况中的应用。

  公开号：

  WO2018189553A1

文献信息

• PYRAZOLOPYRIMIDINE COMPOUNDS USEFUL AS RET INHIBITORS
  申请人：Cancer Research Technology Limited

  公开号：EP4105219A1

  公开（公告）日：2022-12-21

  The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.

  本发明涉及作为 RET（转染过程中重排）激酶酶活性抑制剂的式 I 化合物： 其中HET、键a、b、c和d、X1、X2、X3、X4、R2和R3各自如本文所定义。本发明还涉及这些化合物的制备工艺、包含这些化合物的药物组合物，以及它们在治疗增殖性疾病（如癌症）和其他涉及 RET 激酶活性的疾病或病症中的用途。
• Inhibitors of cysteine proteases and methods of use thereof
  申请人：Pardes Biosciences, Inc.

  公开号：US11174231B1

  公开（公告）日：2021-11-16

  The disclosure provides compounds with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.

  本公开提供了带有弹头的化合物及其在治疗医学疾病或失调（如病毒感染）中的用途。提供了药物组合物和制造各种带弹头化合物的方法。这些化合物可用于抑制蛋白酶，如 3C、CL 或 3CL 样蛋白酶。
• Compounds useful as RET inhibitors
  申请人：Cancer Research Technology Limited

  公开号：US11352361B2

  公开（公告）日：2022-06-07

  The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.

  本发明涉及作为 RET（转染过程中重排）激酶酶活性抑制剂的式 I 化合物： 其中HET、键a、b、c和d、X1、X2、X3、X4、R2和R3各自如本文所定义。本发明还涉及这些化合物的制备工艺、包含这些化合物的药物组合物，以及它们在治疗增殖性疾病（如癌症）和其他涉及 RET 激酶活性的疾病或病症中的用途。
• COMPOUNDS USEFUL AS RET INHIBITORS
  申请人：Cancer Research Technology Limited

  公开号：EP3609898A1

  公开（公告）日：2020-02-19
• Compounds Useful as RET Inhibitors
  申请人：Cancer Research Technology Limited

  公开号：US20200157107A1

  公开（公告）日：2020-05-21

  The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X 1 , X 2 , X 3 , X 4 , R 2 , and R 3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.