1-benzyl-2,2,5,5-tetramethylpiperazine | 501653-34-5

• 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-benzyl-2,2,5,5-tetramethylpiperazine
• CAS: 501653-34-5
• 化学式: C₁₅H₂₄N₂
• 分子量: 232.369
• InChiKey: OYRHWKZRJAQUQH-UHFFFAOYSA-N

物化性质

• 沸点：
  303.6±22.0 °C(Predicted)
• 密度：
  0.934±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-benzyl-2,2,5,5-tetramethylpiperazine 、 6-(4-methoxymethoxyphenyl)-3-methyl-1-(tetrahydropyran-2-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid 在 2-bromo-1-ethylpyridin-1-ium tetrafluoroborate 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 以81%的产率得到(4-benzyl-2,2,5,5-tetramethylpiperazin-1-yl)-[6-(4-methoxymethoxyphenyl)-3-methyl-1-(tetrahydropyran-2-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl]methanone
  参考文献：
  名称：

  [EN] SUBSTITUTED 6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
  [FR] DÉRIVÉS DE 6-(4-HYDROXYPHÉNYL)-1H-PYRAZOLO[3,4-B]PYRIDINE SUBSTITUÉS UTILISÉS COMME INHIBITEURS DE KINASES

  摘要：

  本发明涉及一种式为pyrazolo[3,4-b]pyridine的化合物，其中R'、R2、R3、R4、R5和R6如下所示。公式I的化合物是蛋白激酶C（PKC）抑制剂，可用于治疗与糖尿病和糖尿病并发症相关的疾病，例如糖尿病肾病、糖尿病神经病和糖尿病视网膜病变。此外，本发明还涉及将该化合物用作药物的活性成分，以及包含它们的制药组合物。

  公开号：

  WO2013167403A1
• 作为产物：
  描述：

  6-benzyl-8,8-dimethyl-6,9-diazaspiro[4.5]decane 、 1,2-二氨基-2-甲基丙烷 、 丙酮氰醇 生成 1-benzyl-2,2,5,5-tetramethylpiperazine
  参考文献：
  名称：

  6-(4-hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors

  摘要：

  本发明涉及公式I的吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3、R4、R5、R6和R7如下所示。公式I的化合物是激酶抑制剂，适用于治疗与糖尿病和糖尿病并发症相关的疾病，例如糖尿病肾病、糖尿病神经病变和糖尿病视网膜病变。本发明还涉及公式I的化合物的用途，特别是作为药物活性成分以及包含它们的制药组合物。

  公开号：

  US08686150B2

文献信息

• 6-(4-Hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
  申请人：SANOFI

  公开号：US20130085128A1

  公开（公告）日：2013-04-04

  The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3、R4、R5、R6和R7如下所示。式I的化合物是激酶抑制剂，适用于治疗与糖尿病及糖尿病并发症相关的疾病，如糖尿病肾病、糖尿病神经病变和糖尿病视网膜病变等。此外，本发明还涉及式I的化合物的用途，特别是作为药物中的活性成分以及包含它们的药物组合物。
• [EN] 6-(4-HYDROXY-PHENYL)-3-ALKYL-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS D'AMIDE D'ACIDE 6-(4-HYDROXYPHÉNYL)-3-ALKYL-1H-PYRAZOLO[3,4-B] PYRIDINE-4-CARBOXYLIQUE UTILISÉS COMME INHIBITEURS DE KINASE
  申请人：SANOFI SA

  公开号：WO2013045413A1

  公开（公告）日：2013-04-04

  The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula (I), in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula (I) are protein kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式(I)的吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3、R4、R5、R6和R7如下所示。式(I)的化合物是蛋白激酶C（PKC）抑制剂，并且对于治疗与糖尿病和糖尿病并发症相关的疾病，例如糖尿病肾病、糖尿病神经病和糖尿病视网膜病变等，非常有用。此外，本发明还涉及使用该式化合物，特别是作为药物中的活性成分，以及包含它们的制药组合物。
• SUBSTITUTED 6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
  申请人：SANOFI

  公开号：US20150133432A1

  公开（公告）日：2015-05-14

  The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3、R4、R5和R6如下所示。式I的化合物是激酶抑制剂，用于治疗与糖尿病和糖尿病并发症相关的疾病，例如糖尿病肾病、糖尿病神经病和糖尿病视网膜病变。此外，本发明还涉及使用式I的化合物，特别是作为药物的活性成分以及包含它们的制药组合物。
• Substituted 6-(4-hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors
  申请人：SANOFI

  公开号：US09133181B2

  公开（公告）日：2015-09-15

  The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3、R4、R5和R6如下所示。式I的化合物是激酶抑制剂，可用于治疗与糖尿病和糖尿病并发症相关的疾病，例如糖尿病肾病、糖尿病神经病变和糖尿病视网膜病变。本发明还涉及使用式I的化合物，特别是作为制药活性成分以及包含它们的制药组合物。
• 6-(4-HYDROXY-PHENYL)-3-ALKYL-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS
  申请人：SANOFI

  公开号：EP2760862A1

  公开（公告）日：2014-08-06