Tert-butyl 6-[4-[[5-[(2,6-difluoro-3-methoxy-5-methylphenyl)methoxy]pyrimidin-2-yl]amino]-2-methoxyphenyl]-2,6-diazaspiro[3.3]heptane-2-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: Tert-butyl 6-[4-[[5-[(2,6-difluoro-3-methoxy-5-methylphenyl)methoxy]pyrimidin-2-yl]amino]-2-methoxyphenyl]-2,6-diazaspiro[3.3]heptane-2-carboxylate
• 英文别名: tert-butyl 6-[4-[[5-[(2,6-difluoro-3-methoxy-5-methylphenyl)methoxy]pyrimidin-2-yl]amino]-2-methoxyphenyl]-2,6-diazaspiro[3.3]heptane-2-carboxylate
• 化学式: C₃₀H₃₅F₂N₅O₅
• 分子量: 583.6
• InChiKey: OOQKXFTZGBOVAR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  42
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  98.3
• 氢给体数：
  1
• 氢受体数：
  11

文献信息

• NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND
  申请人：KOTOBUKI PHARMACEUTICAL CO., LTD.

  公开号：US20140142084A1

  公开（公告）日：2014-05-22

  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.

  提供了一种化合物，可作为膀胱癌的预防和/或治疗药物。通过对具有FGFR抑制作用的化合物进行研究，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FGFR3具有抑制作用，因此完成了本发明。本发明的含氮芳香杂环化合物可用作与FGFR1、FGFR2和/或FGFR3相关的各种癌症的治疗药物，如肺癌和激素治疗耐药性乳腺癌、胃癌、三阴性乳腺癌、子宫内膜癌、膀胱癌和胶质母细胞瘤，特别是作为突变FGFR3阳性膀胱癌的预防和/或治疗药物。
• US9464077B2
  申请人：——

  公开号：US9464077B2

  公开（公告）日：2016-10-11