1-[(2S)-butan-2-yl]-2-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide

• 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: 1-[(2S)-butan-2-yl]-2-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide
• 化学式: C₂₃H₂₉N₅O
• 分子量: 391.5
• InChiKey: LRLGMFTYSHZHPP-HNNXBMFYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  76.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• COMBINATION
  申请人：Glaxosmithkline LLC

  公开号：EP2934531A1

  公开（公告）日：2015-10-28
• [EN] COMBINATION<br/>[FR] COMBINAISON
  申请人：GLAXOSMITHKLINE LLC

  公开号：WO2014100080A1

  公开（公告）日：2014-06-26

  The present invention relates to a method of treating cancer and pre-cancerous syndromes in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering: (i) an EZH2 inhibitor selected from: N-[4,6-dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-[(1 S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide, or a pharmaceutically acceptable salt thereof; 1-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pryidinyl)methyl]-6-[2- (4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide, or a pharmaceutically acceptable salt thereof; and N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetahydro-2H-pyran-4-yl)amino)-4-mehtyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide, or a pharmaceutically acceptable salt thereof; and (ii) a Bcl-2 inhibitor, to a human in need thereof.