Tert-butyl 4-[4-[[5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl]amino]-2-fluorophenyl]piperazine-1-carboxylate | 1453212-49-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: Tert-butyl 4-[4-[[5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl]amino]-2-fluorophenyl]piperazine-1-carboxylate
• CAS: 1453212-49-1
• 化学式: C₂₈H₃₂F₃N₅O₅
• 分子量: 575.588
• InChiKey: JDQFOBJNWIVARQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  41
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  98.3
• 氢给体数：
  1
• 氢受体数：
  12

文献信息

• NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND
  申请人：Astellas Pharma Inc.

  公开号：EP2821402A1

  公开（公告）日：2015-01-07

  Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.

  本发明提供了一种可用于膀胱癌预防和/或治疗的化合物。 通过对具有 FGFR 抑制作用的化合物的研究，本发明人发现本发明的含氮芳香杂环化合物对 FGFR1、FGFR2 和/或 FGFR3，特别是突变型 FGFR3 具有抑制作用，从而完成了本发明。本发明的含氮芳香杂环化合物可用作与 FGFR1、FGFR2 和/或 FGFR3 有关的各种癌症的治疗剂，如肺癌和激素治疗耐药的乳腺癌、胃癌、三阴性乳腺癌、子宫内膜癌、膀胱癌和胶质母细胞瘤，尤其可用作突变型 FGFR3 阳性膀胱癌的预防和/或治疗剂。