2-(4-(((3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-yl)amino)methyl)piperidin-1-yl)ethanol | 1361951-12-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-(4-(((3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-yl)amino)methyl)piperidin-1-yl)ethanol
• 英文别名: 2-[4-[[[3-[3-(Trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-yl]amino]methyl]piperidin-1-yl]ethanol；2-[4-[[[3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-yl]amino]methyl]piperidin-1-yl]ethanol
• CAS: 1361951-12-3
• 化学式: C₂₁H₂₄F₃N₅O₂
• 分子量: 435.449
• InChiKey: DQINITVVKFIKIO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  74.9
• 氢给体数：
  2
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  3-溴-6-氯咪唑并[1,2-b]哒嗪 在 四(三苯基膦)钯 、 potassium carbonate 、 N,N-二异丙基乙胺 、 cesium fluoride 作用下， 以 1,4-二氧六环 、 水 、 二甲基亚砜 为溶剂， 反应 5.0h， 生成 2-(4-(((3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-yl)amino)methyl)piperidin-1-yl)ethanol
  参考文献：
  名称：

  Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors

  摘要：

  本发明提供具有以下结构之一的蛋白激酶（I）、（II）或（III）：或其立体异构体、前药、互变异构体或药用可接受盐，其中R、R1、R2和X如本文所定义。还公开了在治疗癌症、自身免疫、炎症和其他Pim激酶相关疾病中使用这些组合物和方法。

  公开号：

  US09416132B2

文献信息

• [EN] HETEROCYCLIC PROTEIN KINASE INHIBITORS<br/>[FR] INHIBITEURS DE PROTÉINE KINASE HÉTÉROCYCLIQUES
  申请人：TOLERO PHARMACEUTICALS INC

  公开号：WO2013013188A1

  公开（公告）日：2013-01-24

  The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.

  本发明提供具有以下结构之一的蛋白激酶（I）、（II）或（III）：或其立体异构体、前药、互变异构体或药用可接受盐，其中R、R1、R2和X如本文所定义。还公开了在治疗癌症、自身免疫、炎症和其他Pim激酶相关疾病中使用这些蛋白激酶的组合物和方法。
• IMIDAZO[1,2-B]PYRIDAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS
  申请人：Xu Yong

  公开号：US20120058997A1

  公开（公告）日：2012-03-08

  The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R 1 , R 2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.

  本发明提供了蛋白激酶抑制剂，包括以下结构（I）和（II）的咪唑[1,2-b]吡啶和吡唑[1,5-a]嘧啶化合物或其立体异构体、前药或药物可接受的盐，其中R、R1、R2和X如本文所定义。还公开了将其用于治疗癌症和其他Pim激酶相关疾病的组合物和方法。
• HETEROCYCLIC PROTEIN KINASE INHIBITORS
  申请人：Xu Yong

  公开号：US20140329807A1

  公开（公告）日：2014-11-06

  The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R 1 , R 2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.

  本发明提供具有以下结构之一（I），（II）或（III）的蛋白激酶：或其立体异构体，前药，互变异构体或药学上可接受的盐，其中R，R1，R2和X如本文所定义。还公开了在治疗癌症，自身免疫，炎症和其他Pim激酶相关疾病中使用相同的组合物和方法。
• Substituted imidazo[1,2-B]pyridazines as protein kinase inhibitors
  申请人：Tolero Pharmaceuticals, Inc.

  公开号：US10392392B2

  公开（公告）日：2019-08-27

  The present invention provides substituted imidazo[1,2-b]pyridazines that are useful as protein kinase inhibitors and have one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. For example, a compound having the following structure: Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.

  本发明提供了可用作蛋白激酶抑制剂的取代咪唑并[1,2-b]哒嗪，它们具有以下结构之一 (I)、(II) 或 (III)： 或其立体异构体、原药、同系物或药学上可接受的盐，其中 R、R1、R2 和 X 如本文所定义。例如，具有以下结构的化合物： 此外，还公开了用于治疗癌症、自身免疫性疾病、炎症和其他与 Pim 激酶相关的疾病的组合物和方法。
• SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINES AS PROTEIN KINASE INHIBITORS
  申请人：Tolero Pharmaceuticals, Inc.

  公开号：US20170002014A1

  公开（公告）日：2017-01-05

  The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R 1 , R 2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.