3-(4-cyclopropyl-1H-imidazol-1-yl)-N-(6-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)benzamide | 1262041-59-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-(4-cyclopropyl-1H-imidazol-1-yl)-N-(6-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)benzamide
• 英文别名: USRE48711, Example 192；3-(4-cyclopropylimidazol-1-yl)-N-[6-(4-cyclopropyl-1,2,4-triazol-3-yl)pyridin-2-yl]benzamide
• CAS: 1262041-59-7
• 化学式: C₂₃H₂₁N₇O
• 分子量: 411.466
• InChiKey: WUSUSCGYDUUQMW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  31
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  90.5
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS
  申请人：Corkey Britton

  公开号：US20110009410A1

  公开（公告）日：2011-01-13

  The present invention relates to compounds of Formula (I): where in X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , R 1 , R 2 , R 3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

  本发明涉及式(I)的化合物： 其中X 1 、X 2 、X 3 、X 4 、X 5 、X 6 、X 7 、X 8 、R 1 、R 2 、R 3 如上所定义。这些化合物具有凋亡信号调节激酶（“ASK1”）抑制活性，因此在治疗ASK1介导的疾病，包括自身免疫性疾病、炎症性疾病、心血管疾病和神经退行性疾病方面具有用途。该发明还涉及包含一种或多种式(I)化合物的药物组合物，以及制备式(I)化合物的方法。
• Apoptosis signal-regulating kinase inhibitors
  申请人：GILEAD SCIENCES, INC.

  公开号：EP2933252A1

  公开（公告）日：2015-10-21

  The present invention relates to compounds of Formula (I): where in X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase ("ASK1") inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

  本发明涉及式（I）化合物：其中 X1、X2、X3、X4、X5、X6、X7、X8、R1、R2、R3 如上定义。这些化合物具有抑制细胞凋亡信号调节激酶（"ASK1"）的活性，因此可用于治疗 ASK1 介导的疾病，包括自身免疫性疾病、炎症性疾病、心血管疾病和神经退行性疾病。本发明还涉及包含一种或多种式（I）化合物的药物组合物，以及制备式（I）化合物的方法。
• ORAL DOSAGE FORM OF APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS
  申请人：Gilead Sciences, Inc.

  公开号：EP3363797A1

  公开（公告）日：2018-08-22

  The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase ("ASK1") inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

  本发明涉及式（I）化合物：其中 X1、X2、X3、X4、X5、X6、X7、X8、R1、R2、R3 如上文所定义。这些化合物具有抑制细胞凋亡信号调节激酶（"ASK1"）的活性，因此可用于治疗 ASK1 介导的疾病，包括自身免疫性疾病、炎症性疾病、心血管疾病和神经退行性疾病。本发明还涉及包含一种或多种式（I）化合物的药物组合物，以及制备式（I）化合物的方法。
• COMBINATION THERAPIES FOR TREATING CANCERS
  申请人：GILEAD SCIENCES, INC.

  公开号：US20180311247A1

  公开（公告）日：2018-11-01

  Provided herein are methods that relate to a therapeutic strategy for treatment of cancer, and allergic, autoimmune, and inflammatory disorders including hematological malignancies. In particular, the methods include administration of a BTK inhibitor and with one or more inhibitor. For example, the one or more inhibitor may be a JAK inhibitor, a ASK1 inhibitor, a BRD4 inhibitor or an MMP9 inhibitor.
• US8378108B2
  申请人：——

  公开号：US8378108B2

  公开（公告）日：2013-02-19