Pyrazolo[3,4-d]pyrimidin-4-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: Pyrazolo[3,4-d]pyrimidin-4-one
• 化学式: C₅H₂N₄O
• 分子量: 134.1
• InChiKey: IUYQIJQHYDZUDF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  66.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  1-cyclopentyl-3-ethyl-5-amino-1H-pyrazole-4-carboxamide 、 3-[2-(二甲基氨基)乙氧基]苯甲醛 在 氯仿 、 水 、 Brine 、 magnesium sulfate 、 1-cyclopentyl-3-ethyl-6-[3-[2-dimethylamino)ethoxy]phenyl 作用下， 以 xylenes 为溶剂， 反应 16.0h， 以to afford, as an oil, 1-cyclopentyl-3-ethyl-6-[3-[2-dimethylamino)ethoxy]phenyl]pyrazolo[3,4-d]pyrimidin-4-one的产率得到Pyrazolo[3,4-d]pyrimidin-4-one
  参考文献：
  名称：

  6-aryl pyrazolo\x9b3,4-D! pyrimidin-4-ones and compositions and method of

  摘要：

  6-芳基吡唑并[3,4-d]嘧啶-4-酮衍生物，含有它们的制药组合物以及用于影响c-GMP-磷酸二酯酶抑制和治疗心力衰竭和/或高血压的方法。

  公开号：

  US05736548A1

文献信息

• 6-Substituted pyrazolo[3,4-d] pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
  申请人：——

  公开号：US20020013328A1

  公开（公告）日：2002-01-31

  The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): 1 that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

  本发明涉及合成一种新型类别的吡唑并[3,4-d]嘧啶-4-酮化合物，其化学式为(I)，或其互变异构体(II)：1，这些化合物是一类被称为细胞周期蛋白依赖性激酶抑制剂的强效抑制剂，与催化亚单位细胞周期蛋白依赖性激酶1-8及其调节亚单位细胞周期蛋白A-H、K、N和T有关。本发明还提供了一种新型的治疗癌症或其他增生性疾病的方法，通过给患者投与这些化合物或其药学上可接受的盐形式的治疗有效剂量。另外，也可以通过给患者投与本发明化合物中的一种和一种或多种其他已知的抗癌或抗增生剂的治疗有效组合来治疗癌症或其他增生性疾病。
• 6-substituted pyrazolo [3,4-d] pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
  申请人：DuPont Pharmaceuticals Company

  公开号：US06531477B1

  公开（公告）日：2003-03-11

  The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

  本发明涉及合成一种新型吡唑并［3,4-d］嘧啶-4-酮类化合物，其化学式为（I），或其互变异构体（II），这些化合物是强效的细胞周期蛋白依赖性激酶抑制剂，与催化亚基细胞周期蛋白依赖性激酶1-8及其调节亚基细胞周期蛋白A-H，K，N和T有关。本发明还提供了一种治疗癌症或其他增生性疾病的新方法，通过给予这些化合物或其药学上可接受的盐形式的治疗有效剂量。或者，可以通过给予本发明化合物之一和一种或多种其他已知的抗癌或抗增生剂的治疗有效组合来治疗癌症或其他增生性疾病。
• 6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
  申请人：DuPont Pharmaceuticals Company

  公开号：US06559152B2

  公开（公告）日：2003-05-06

  The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

  本发明涉及一种新型嘧唑并[3,4-d]嘧啶-4-酮类化合物，其化学式为(I)，或可用互变异构体(II)表示，该化合物是强效的细胞周期蛋白依赖性激酶抑制剂，与催化亚基细胞周期蛋白依赖性激酶1-8以及其调控亚基，即A-H，K，N和T有关。本发明还提供了一种治疗癌症或其他增殖性疾病的新方法，即通过给患者注射这些化合物或其药学上可接受的盐形式的治疗有效剂量。另外，也可以通过给患者注射本发明化合物和一种或多种其他已知的抗癌或抗增殖剂的治疗有效组合来治疗癌症或其他增殖性疾病。
• US05958929
  申请人：——

  公开号：——

  公开（公告）日：——
• 6-aryl pyrazolo\x9b3,4-D! pyrimidin-4-ones and compositions and method of
  申请人：Sanofi

  公开号：US05736548A1

  公开（公告）日：1998-04-07

  6-Aryl pyrazolo\x9b3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.

  6-芳基吡唑并[3,4-d]嘧啶-4-酮衍生物，含有它们的制药组合物以及用于影响c-GMP-磷酸二酯酶抑制和治疗心力衰竭和/或高血压的方法。