N-(6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide | 1010120-56-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并吡啶类
• 英文名称: N-(6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide
• 英文别名: N-[6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]acetamide
• CAS: 1010120-56-5
• 化学式: C₁₄H₁₉BN₄O₃
• 分子量: 302.141
• InChiKey: VBRCDALYSNQXIV-UHFFFAOYSA-N

物化性质

• 密度：
  1.26±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.99
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  77.8
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  N-(6-bromo-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide 、 联硼酸频那醇酯 在 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 potassium acetate 作用下， 以 甲苯 为溶剂， 反应 16.0h， 以100%的产率得到N-(6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide
  参考文献：
  名称：

  [EN] AMINO TRIAZOLES AS PI3K INHIBITORS
  [FR] AMINOTRIAZOLES COMME INHIBITEURS DE P13K

  摘要：

  公开号：

  WO2009068482A8

文献信息

• TRIAZOLE DERIVATIVES AS KINASE INHIBITORS
  申请人：Wilson Francis

  公开号：US20100227800A1

  公开（公告）日：2010-09-09

  The invention relates to compounds of formula (I); wherein X and R 1 to R 5 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of Itk or PI3K, for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.

  本发明涉及式(I)的化合物；其中X和R1至R5的含义如所述及权利要求中所述。所述化合物可用作蛋白激酶抑制剂，特别是Itk或PI3K的抑制剂，用于治疗或预防免疫、炎症或过敏性疾病。本发明还涉及包括所述化合物的制药组合物，以及制备这些化合物的方法以及作为药物的生产和使用。
• Amino triazoles as PI3K inhibitors
  申请人：Ramsden Nigel

  公开号：US08865699B2

  公开（公告）日：2014-10-21

  The invention relates to compounds of formula (I) wherein X, T1 and R1 to R3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.

  该发明涉及公式（I）的化合物，其中X、T1和R1至R3的含义如说明书和权利要求书所述。所述化合物可用作蛋白激酶抑制剂，特别是PI3K的抑制剂，用于治疗或预防免疫、炎症、自身免疫或过敏性疾病。该发明还涉及包括所述化合物的制药组合物，以及制备此类化合物的方法以及作为药物的生产和使用。
• Triazole derivatives as kinase inhibitors
  申请人：Wilson Francis

  公开号：US08883820B2

  公开（公告）日：2014-11-11

  The invention relates to compounds of formula (I); wherein X and R1 to R5 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of Itk or PI3K, for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.

  本发明涉及公式(I)的化合物；其中X和R1到R5的含义如说明书和权利要求所述。所述化合物可用作蛋白激酶抑制剂，特别是Itk或PI3K的抑制剂，用于治疗或预防免疫、炎症或过敏性疾病。本发明还涉及包括所述化合物的制药组合物，以及制备此类化合物的方法以及其作为药物的生产和使用。
• AMINO TRIAZOLES AS PI3K INHIBITORS
  申请人：Ramsden Nigel

  公开号：US20110021497A1

  公开（公告）日：2011-01-27

  The invention relates to compounds of formula (I) wherein X, T 1 and R 1 to R 3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.

  本发明涉及式(I)的化合物，其中X、T1和R1至R3具有所述说明书和权利要求中所述的含义。所述化合物可用作蛋白激酶抑制剂，特别是PI3K的抑制剂，用于治疗或预防免疫、炎症、自身免疫或过敏性疾病。本发明还涉及包括所述化合物的制药组合物，以及制备此类化合物以及作为药物的生产和使用。
• [EN] AMINO TRIAZOLES AS PI3K INHIBITORS<br/>[FR] AMINOTRIAZOLES COMME INHIBITEURS DE P13K
  申请人：CELLZOME LTD

  公开号：WO2009068482A8

  公开（公告）日：2010-07-29