4-[8-(2,2-difluoroethylamino)-6-(5-fluoro-2-methylphenoxy)imidazo[1,2-b]pyridazin-3-yl]-N-ethyl-2-methylbenzamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-[8-(2,2-difluoroethylamino)-6-(5-fluoro-2-methylphenoxy)imidazo[1,2-b]pyridazin-3-yl]-N-ethyl-2-methylbenzamide
• 化学式: C₂₅H₂₄F₃N₅O₂
• 分子量: 483.5
• InChiKey: KFHPERPPLXIIRP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  80.6
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• [EN] COMBINATIONS FOR THE TREATMENT OF CANCER<br/>[FR] COMBINAISONS POUR LE TRAITEMENT DU CANCER
  申请人：BAYER PHARMA AG

  公开号：WO2014020041A1

  公开（公告）日：2014-02-06

  The present invention relates to combinations of at least two compounds A and B, compound A being an inhibitor of Mps-1 kinase, and compound B being an inhibitor of an anti-apoptotic protein of the Bcl-2 family. Another aspect of the present invention relates to the use of such combinations as described supra for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of cancer. Another aspect of the present invention relates to the use of an anti- apoptotic protein from the Bcl-2 family as a sensitizer of cells to Mps-1 inhibitors. Another aspect of the present invention relates to the use of the ratio of pro-apoptotic and anti-apoptotic proteins from the Bcl-2 family in a biological sample as a biomarker for a Mps-1 kinase inhibitor treatment.

  本发明涉及至少两种化合物A和B的组合，其中化合物A是Mps-1激酶的抑制剂，化合物B是Bcl-2家族抗凋亡蛋白的抑制剂。本发明的另一个方面涉及将这种组合用于制备用于治疗或预防疾病的药物，特别是用于癌症治疗。本发明的另一个方面涉及将Bcl-2家族的抗凋亡蛋白用作细胞对Mps-1抑制剂的敏感剂。本发明的另一个方面涉及将Bcl-2家族的促凋亡和抗凋亡蛋白的比例在生物样本中用作Mps-1激酶抑制剂治疗的生物标志物。
• SUBSTITUTED IMIDAZOPYRIDAZINES
  申请人：Bayer Intellectual Property GmbH

  公开号：EP2614063B1

  公开（公告）日：2016-01-13
• US9255100B2
  申请人：——

  公开号：US9255100B2

  公开（公告）日：2016-02-09