1,3-dimethyl-5-nitro-6-(piperidin-1-yl)-1H-indazole

• 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: 1,3-dimethyl-5-nitro-6-(piperidin-1-yl)-1H-indazole
• 英文别名: 1,3-Dimethyl-5-nitro-6-piperidin-1-ylindazole；1,3-dimethyl-5-nitro-6-piperidin-1-ylindazole
• 化学式: C₁₄H₁₈N₄O₂
• 分子量: 274.323
• InChiKey: OFGJUVKCZFYKTF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  66.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-氟-3-甲基-1H-吲唑 在 硫酸 、 sodium hydride 、 potassium nitrate 作用下， 以 四氢呋喃 为溶剂， 反应 6.0h， 生成 1,3-dimethyl-5-nitro-6-(piperidin-1-yl)-1H-indazole 、 2,3-dimethyl-5-nitro-6-(piperidin-1-yl)-2H-indazole
  参考文献：
  名称：

  Indazole Compounds as IRAK4 Inhibitors

  摘要：

  本发明提供了式（I）的吲唑化合物，作为激酶抑制剂在治疗上具有疗效，特别是IRAK4抑制剂，其中Z1、Z2、R1、R2、R3、'm'和'n'在规范中给出了含义，并且其药学上可接受的盐或立体异构体在治疗和预防疾病或疾病中有用，特别是它们在由激酶酶介导的疾病或疾病中的使用，特别是IRAK4酶。本发明还提供了包括至少一种式（I）化合物的药物组合物，以及药学上可接受的载体、稀释剂或赋形剂。

  公开号：

  US20160326151A1

文献信息

• [EN] INDAZOLE COMPOUNDS AS IRAK4 INHIBITORS<br/>[FR] COMPOSÉS D'IMIDAZOLE UTILISABLES EN TANT QU'INHIBITEURS DE L'IRAK4
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2015104662A1

  公开（公告）日：2015-07-16

  The present invention provides indazole compound of formula (I), which are therapeutically useful as kinase inhibitor, particularly IRAK4 inhibitors. wherein Z1, Z2, R1, R2, R3, 'm' and 'n' have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomers thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了式（I）的吲唑化合物，其在治疗中具有潜在的激酶抑制作用，特别是IRAK4抑制剂。其中Z1、Z2、R1、R2、R3、'm'和'n'的含义如规范中所述，并且其药学上可接受的盐或立体异构体在治疗和预防疾病或紊乱方面具有用处，特别是在由激酶酶介导的疾病或紊乱中的应用，特别是IRAK4酶。本发明还提供了包括至少一种式（I）化合物的药物组合物，以及药学上可接受的载体、稀释剂或赋形剂。
• Indazole compounds as IRAK4 inhibitors
  申请人：Aurigene Discovery Technologies Limited

  公开号：US10160753B2

  公开（公告）日：2018-12-25

  The present invention provides indazole compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors, wherein Z1, Z2, R1, R2, R3, ‘m’ and ‘n’ have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical compositions comprising at least one of the compounds of the compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.

  本发明提供了式(I)的吲唑化合物，其作为激酶抑制剂，特别是IRAK4抑制剂具有治疗作用，其中Z1、Z2、R1、R2、R3、'm'和'n'具有说明书中给出的含义，其药学上可接受的盐或立体异构体可用于治疗和预防疾病或紊乱，特别是其在激酶，特别是IRAK4酶介导的疾病或紊乱中的用途。本发明还提供了药物组合物，其包含至少一种式（I）化合物以及药学上可接受的载体、稀释剂或赋形剂。
• INDAZOLE COMPOUNDS AS IRAK4 INHIBITORS
  申请人：Aurigene Discovery Technologies Limited

  公开号：EP3092226A1

  公开（公告）日：2016-11-16
• Indazole Compounds as IRAK4 Inhibitors
  申请人：AURIGENE DISCOVERY TECHNOLOGIES LIMITED

  公开号：US20160326151A1

  公开（公告）日：2016-11-10

  The present invention provides indazole compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors, wherein Z 1 , Z 2 , R 1 , R 2 , R 3 , ‘m’ and ‘n’ have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical compositions comprising at least one of the compounds of the compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.

  本发明提供了式（I）的吲唑化合物，作为激酶抑制剂在治疗上具有疗效，特别是IRAK4抑制剂，其中Z1、Z2、R1、R2、R3、'm'和'n'在规范中给出了含义，并且其药学上可接受的盐或立体异构体在治疗和预防疾病或疾病中有用，特别是它们在由激酶酶介导的疾病或疾病中的使用，特别是IRAK4酶。本发明还提供了包括至少一种式（I）化合物的药物组合物，以及药学上可接受的载体、稀释剂或赋形剂。