N-(1-(2-fluorobenzyl)-1H-pyrazol-4-yl)-5,5-dimethyl-2-((tetrahydro-2H-pyran-4-yl)amino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxamide | 1584146-96-2

• 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: N-(1-(2-fluorobenzyl)-1H-pyrazol-4-yl)-5,5-dimethyl-2-((tetrahydro-2H-pyran-4-yl)amino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxamide
• 英文别名: US9546173, cmpd 105；N-[1-[(2-fluorophenyl)methyl]pyrazol-4-yl]-5,5-dimethyl-2-(oxan-4-ylamino)-7H-pyrrolo[3,4-d]pyrimidine-6-carboxamide
• CAS: 1584146-96-2
• 化学式: C₂₄H₂₈FN₇O₂
• 分子量: 465.53
• InChiKey: OWRPUJHUSMEXQA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  97.2
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• DIHYDROPYRROLIDINO-PYRIMIDINES AS KINASE INHIBITORS
  申请人：DILLON Michael Patrick

  公开号：US20150274733A1

  公开（公告）日：2015-10-01

  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 ERK1 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）的化合物及其药学上可接受的盐；如本文所述。本发明还提供了包含这些化合物的制药组合物，并与治疗协同剂联合使用或与治疗协同剂一起使用的组合物，以及这些化合物和组合物的治疗用途。这些化合物和组合物在治疗与ERK1和/或ERK2激活相关的疾病，特别是对于显示对Raf和/或MEK抑制性癌症治疗药物耐药的MAPK通路依赖性癌症的治疗非常有用。
• US9546173B2
  申请人：——

  公开号：US9546173B2

  公开（公告）日：2017-01-17