(4R)-1-[5,5-dimethyl-2-(oxan-4-ylamino)-7H-pyrrolo[3,4-d]pyrimidin-6-yl]-4,5-dimethylhex-2-yn-1-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: (4R)-1-[5,5-dimethyl-2-(oxan-4-ylamino)-7H-pyrrolo[3,4-d]pyrimidin-6-yl]-4,5-dimethylhex-2-yn-1-one
• 化学式: C₂₁H₃₀N₄O₂
• 分子量: 370.5
• InChiKey: XEWILEORWYCPEV-HNNXBMFYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  67.4
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] DIHYDROPYRROLIDINO-PYRIMIDINES AS KINASE INHIBITORS<br/>[FR] DIHYDROPYRROLIDINOPYRIMIDINES COMME INHIBITEURS DE KINASE
  申请人：NOVARTIS AG

  公开号：WO2014047020A1

  公开（公告）日：2014-03-27

  The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof; as further described herein. The present invention further provides pharmaceutical compositions comprising these compounds, and combinations comprising these compounds combined with or used with a therapeutic co-agent, as well as therapeutic uses of these compounds and compositions. These are useful in the treatment of diseases such as cancer that are associated with activation of ERKl and/or ERK2, and especially for MAPK pathway dependent cancers showing resistance to Raf and/or MEK inhibitory cancer therapeutics

  本发明提供了式(I)的化合物及其药用盐；如本文所述。本发明进一步提供了包含这些化合物的药物组合物，以及与治疗协同剂结合或使用的这些化合物的组合物，以及这些化合物和组合物的治疗用途。这些在治疗与ERKl和/或ERK2激活相关的癌症等疾病方面非常有用，特别适用于对Raf和/或MEK抑制癌症治疗药物显示抵抗的MAPK信号通路依赖性癌症。