2-Benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidine | 752259-62-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并间二氧杂环戊烯类
• 英文名称: 2-Benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidine
• 英文别名: 2-(1,3-benzodioxol-5-yl)-3-(6-methylpyridin-2-yl)imidazo[1,2-a]pyrimidine
• CAS: 752259-62-4
• 化学式: C₁₉H₁₄N₄O₂
• 分子量: 330.346
• InChiKey: PNWNZEIIYSUKRY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  61.5
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1,3,5-三嗪-2,4,6-三胺,N,N'''-1,2-乙二基二[N-[3-[[4,6-二[丁基(2,2,6,6-四甲基-4-哌啶基)氨基]-1,3,5-三嗪-2-基]氨基]丙基]-N,N''-二丁基-N,N''-二(2,2,6,6-四甲基-4-哌啶基)- 、 1-(苯并[d][1,3]二氧代-5-基)-2-溴-2-(6-甲基吡啶-2-基)乙酮 在 碳酸氢钠 作用下， 以 N-甲基乙酰胺 为溶剂， 以35%的产率得到2-Benzo[1,3]dioxol-5-yl-3-(6-methyl-pyridin-2-yl)-imidazo[1,2-a]pyrimidine
  参考文献：
  名称：

  Novel fused heteroaromatic compounds as transforming growth factor (TGF) inhibitors

  摘要：

  描述了新型融合杂芳化合物，包括其衍生物，以及用于其制备的中间体，含有它们的药物组合物以及它们的药用。本发明的化合物是转化生长因子（“TGF”）-β信号通路的有效抑制剂。它们在治疗各种与TGF相关的疾病状态中非常有用，包括癌症和纤维化疾病。

  公开号：

  US20040176390A1

文献信息

• NOVEL FUSED HETEROAROMATIC COMPOUNDS AS TRANSFORMING GROWTH FACTOR (TGF) INHIBITORS
  申请人：Blumberg Laura C.

  公开号：US20080275235A1

  公开（公告）日：2008-11-06

  Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)- signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

  本发明涉及融合的杂环化合物，包括其衍生物，以及制备它们的中间体，含有它们的制药组合物以及它们的药用用途。本发明的化合物是转化生长因子（“TGF”）信号通路的有效抑制剂。它们在治疗各种与TGF相关的疾病状态方面非常有用，包括癌症和纤维化疾病等。
• Imidazopyrimidines as transforming growth factor (TGF) inhibitors
  申请人：Pfizer Inc.

  公开号：US07417041B2

  公开（公告）日：2008-08-26

  Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-β signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

  本发明涉及新型融合杂环化合物，包括其衍生物，以及制备它们的中间体，含有它们的药物组合物以及它们的医药用途。本发明的化合物是转化生长因子（“TGF”）-β信号通路的有效抑制剂。它们可用于治疗各种与TGF相关的疾病状态，包括例如癌症和纤维化疾病。
• FUSED IMIDAZOLES AS TRANSFORMING GROWTH FACTOR (TGF) INHIBITORS
  申请人：Pfizer Products Inc.

  公开号：EP1601676A2

  公开（公告）日：2005-12-07
• US7417041B2
  申请人：——

  公开号：US7417041B2

  公开（公告）日：2008-08-26
• [EN] NOVEL FUSED HETEROAROMATIC COMPOUNDS AS TRANSFORMING GROWTH FACTOR (TGF) INHIBITORS<br/>[FR] NOUVEAUX COMPOSES HETEROAROMATIQUES CONDENSES AGISSANT COMME INHIBITEURS DU FACTEUR DE CROISSANCE TRANSFORMANT (TGF)
  申请人：PFIZER PROD INC

  公开号：WO2004078110A2

  公开（公告）日：2004-09-16

  Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor ('TGF')-ß signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.