1-((4-methyl-1-(5-methyl-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-yl)-1H-pyrrol-3-yl)methyl)azetidin-3-ol | 1307802-44-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-((4-methyl-1-(5-methyl-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-yl)-1H-pyrrol-3-yl)methyl)azetidin-3-ol
• 英文别名: 1-[[4-methyl-1-[5-methyl-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]pyrrol-3-yl]methyl]azetidin-3-ol
• CAS: 1307802-44-3
• 化学式: C₂₃H₂₉N₅O₄
• 分子量: 439.514
• InChiKey: GMJJAPQIVNJPBZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  32
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  93.9
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  1-((4-methyl-1-(5-methyl-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-yl)-1H-pyrrol-3-yl)methyl)azetidin-3-ol 、 三甲基乙酸酐 在 4-二甲氨基吡啶 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以55%的产率得到1-((4-methyl-1-(5-methyl-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-yl)-1H-pyrrol-3-yl)methyl)azetidin-3-yl pivalate
  参考文献：
  名称：

  [EN] KINASE INHIBITORS
  [FR] INHIBITEURS DE KINASES

  摘要：

  公开号：

  WO2011060295A8

文献信息

• Kinase Inhibitors
  申请人：Lee Jaekyoo

  公开号：US20110281841A1

  公开（公告）日：2011-11-17

  The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.

  本发明提供了一种新的蛋白激酶抑制剂群，包括吡咯嘧啶和吡唑嘧啶衍生物，以及其药学上可接受的盐和前药，用于治疗细胞增殖性疾病和疾病，例如癌症、自身免疫性疾病、感染、心血管疾病和神经退行性疾病。本发明提供了合成和给药蛋白激酶抑制剂化合物的方法。本发明还提供了包含至少一种蛋白激酶抑制剂化合物和药学上可接受的载体、稀释剂或赋形剂的制剂。本发明还提供了在合成吡咯嘧啶和吡唑嘧啶衍生物的过程中产生的有用中间体。
• Kinase inhibitors
  申请人：Lee Jaekyoo

  公开号：US08629132B2

  公开（公告）日：2014-01-14

  The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.

  本发明提供了一种新的蛋白激酶抑制剂群，即吡啶并嘧啶和吡唑并嘧啶衍生物，以及其药学上可接受的盐和前药，这些化合物可用于治疗细胞增殖性疾病和疾病，如癌症、自身免疫性疾病、感染、心血管疾病和神经退行性疾病。本发明提供了合成和给药蛋白激酶抑制剂化合物的方法。本发明还提供了包含至少一种蛋白激酶抑制剂化合物和药学上可接受的载体、稀释剂或辅料的制剂。本发明还提供了在合成吡啶并嘧啶和吡唑并嘧啶衍生物过程中产生的有用中间体。
• KINASE INHIBITORS
  申请人：Genosco

  公开号：EP2498607B1

  公开（公告）日：2016-02-17
• US8629132B2
  申请人：——

  公开号：US8629132B2

  公开（公告）日：2014-01-14
• [EN] KINASE INHIBITORS<br/>[FR] INHIBITEURS DE KINASES
  申请人：GENOSCO

  公开号：WO2011060295A8

  公开（公告）日：2011-10-27