2-[[3-(3-chloro-4-fluorophenyl)imidazo[1,2-b]pyridazin-6-yl]amino]butan-1-ol

• 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-[[3-(3-chloro-4-fluorophenyl)imidazo[1,2-b]pyridazin-6-yl]amino]butan-1-ol
• 化学式: C₁₆H₁₆ClFN₄O
• 分子量: 334.781
• InChiKey: KWWMCDVDRSJVAC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  62.4
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments
  申请人：Prien Olaf

  公开号：US20070093490A1

  公开（公告）日：2007-04-26

  The invention relates to novel inhibitors of kinases, methods for preparing such inhibitors, intermediates for the preparation of such inhibitors and uses of such inhibitors.

  这项发明涉及新型激酶抑制剂，制备这种抑制剂的方法，制备这种抑制剂的中间体以及这种抑制剂的用途。
• PIM kinase inhibitors in combination with RNA splicing modulators/inhibitors for treatment of cancers
  申请人：UNIVERSITY OF MARYLAND, BALTIMORE COUNTY

  公开号：US10842785B2

  公开（公告）日：2020-11-24

  The present invention provides for a method of treating cancer and/or reducing proliferation of cancer cells, the method comprising administering to a subject in need of such treatment a composition comprising a PIM kinase inhibitor that exhibits changes of mRNA splicing in combination with a compound that modulates/inhibits activity of an RNA splicing factor protein. Further, changes in splicing of mRNAs and phosphorylation of RNA splicing factors can be used as biomarkers for patient responsiveness to anti-PIM treatment and also suggest effective combinatorial therapies, including synergistic combination.

  本发明提供了一种治疗癌症和/或减少癌细胞增殖的方法，该方法包括向需要这种治疗的受试者施用一种组合物，该组合物包含一种PIM激酶抑制剂，该PIM激酶抑制剂与一种调节/抑制RNA剪接因子蛋白活性的化合物相结合，可显示出mRNA剪接的变化。此外，mRNA 的剪接变化和 RNA 剪接因子的磷酸化可用作患者对抗 PIM 治疗反应性的生物标志物，还可提示有效的组合疗法，包括协同组合疗法。
• PIM kinase inhibitors in combination with autophagy inhibitors for treatment of cancers
  申请人：UNIVERSITY OF MARYLAND, BALTIMORE COUNTY

  公开号：US11389440B2

  公开（公告）日：2022-07-19

  The present invention provides for a method of treating cancer and/or reducing proliferation of cancer cells, the method comprising administering to a subject in need of such treatment a composition comprising a PIM kinase inhibitor that exhibits changes in expressed RNA or ribosomal binding proteins in combination with a compound that inhibits autophagy.

  本发明提供了一种治疗癌症和/或减少癌细胞增殖的方法，该方法包括向需要这种治疗的受试者施用一种组合物，该组合物包含一种 PIM 激酶抑制剂，该抑制剂与一种抑制自噬的化合物结合使用，后者在表达的 RNA 或核糖体结合蛋白中显示出变化。
• PEPTIDE EPOXYKETONE PROTEASOME INHIBITORS IN COMBINATION WITH PIM KINASE INHIBITORS FOR TREATMENT OF CANCERS
  申请人：Onyx Therapeutics, Inc.

  公开号：EP3021862A2

  公开（公告）日：2016-05-25
• PIM KINASE INHIBITORS IN COMBINATION WITH RNA SPLICING MODULATORS/INHIBITORS FOR TREATMENT OF CANCERS
  申请人：University of Maryland, Baltimore County

  公开号：EP3432886B1

  公开（公告）日：2021-06-02