8-amino-1-methyl-4,5-dihydro-1H-1,7,9-triaza-cyclopenta[a]naphthalene-3-carboxylic acid amide | 1031441-25-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 8-amino-1-methyl-4,5-dihydro-1H-1,7,9-triaza-cyclopenta[a]naphthalene-3-carboxylic acid amide
• 英文别名: 2-amino-9-methyl-6,9-dihydro-5H-pyrrolo[3,2-h]quinazoline-7-carboxamide；2-amino-9-methyl-5,6-dihydropyrrolo[3,2-h]quinazoline-7-carboxamide
• CAS: 1031441-25-4
• 化学式: C₁₂H₁₃N₅O
• 分子量: 243.268
• InChiKey: UXWNPSLXAXDXKK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  99.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  8-amino-1-methyl-4,5-dihydro-1H-1,7,9-triaza-cyclopenta[a]naphthalene-3-carboxylic acid 在 1-羟基-1H-苯并三唑铵盐 、 O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 以55%的产率得到8-amino-1-methyl-4,5-dihydro-1H-1,7,9-triaza-cyclopenta[a]naphthalene-3-carboxylic acid amide
  参考文献：
  名称：

  WO2008/65054

  摘要：

  公开号：

文献信息

• [EN] TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS PYRROLO TRICYCLIQUES, LEUR PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION À TITRE D'INHIBITEURS DE KINASES
  申请人：NERVIANO MEDICAL SCIENCES SRL

  公开号：WO2012101032A1

  公开（公告）日：2012-08-02

  The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.

  本发明涉及式（I）的三环吡咯衍生物，其调节蛋白激酶的活性，因此在治疗由失调的蛋白激酶活性引起的疾病方面具有用途。本发明还提供了制备这些化合物的方法、包含这些化合物的药物组合物以及利用这些化合物或含有它们的药物组合物治疗疾病的方法。
• TRICYCLIC INDOLES AND (4,5-DIHYDRO) INDOLES
  申请人：Vanotti Ermes

  公开号：US20100075998A1

  公开（公告）日：2010-03-25

  The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R 1 , R 2 and R 3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.

  本发明提供了三环吲哚和（4,5-二氢）吲哚的公式（I）或其药学上可接受的盐：其中环A代表融合的吡唑、吡啶或嘧啶，表示单重或双重碳-碳键，R1、R2和R3如规范中所定义。本发明的进一步目标是公式（I）化合物的制备方法，包含它们的制药组合物以及治疗细胞增殖性疾病的方法。事实上，公式（I）化合物在治疗与失调的蛋白激酶活性有关的疾病，特别是Cdc7和AKT激酶活性，如癌症方面非常有用。
• Tricyclic indoles and (4,5-dihydro) indoles
  申请人：Nerviano Medical Sciences S.R.L.

  公开号：US08207180B2

  公开（公告）日：2012-06-26

  The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.

  本发明提供了式(I)或其药学上可接受的盐的三环吲哚和(4,5-二氢)吲哚，其中环A代表融合的吡唑、吡啶或嘧啶，表示单一或双重碳-碳键，而R1、R2和R3如规范中所定义。本发明的进一步目的是提供式(I)化合物的制备方法、包含它们的制药组合物以及治疗细胞增殖障碍的方法。事实上，式(I)化合物在治疗与蛋白激酶活性失调有关的疾病，特别是Cdc7和AKT激酶活性，如癌症方面是有用的。
• TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
  申请人：Caldarelli Marina

  公开号：US20130296305A1

  公开（公告）日：2013-11-07

  The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.

  本发明涉及式（I）的三环吡咯衍生物，其调节蛋白激酶的活性，因此在治疗由失调的蛋白激酶活性引起的疾病方面有用。本发明还提供了制备这些化合物的方法，包括这些化合物的制药组合物以及利用这些化合物或含有它们的制药组合物治疗疾病的方法。
• US8207180B2
  申请人：——

  公开号：US8207180B2

  公开（公告）日：2012-06-26