1-methyl-5-(2-propoxy-5-[[1-methyl-1-(2-nicotinoyloxyethyl)]amidosulfonyl]phenyl)-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | 936950-70-8

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 1-methyl-5-(2-propoxy-5-[[1-methyl-1-(2-nicotinoyloxyethyl)]amidosulfonyl]phenyl)-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
• 英文别名: 2-[methyl-[3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenyl]sulfonylamino]ethyl pyridine-3-carboxylate
• CAS: 936950-70-8
• 化学式: C₂₇H₃₂N₆O₆S
• 分子量: 568.654
• InChiKey: DQKFACBHVXZDOY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  40
• 可旋转键数：
  13
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  154
• 氢给体数：
  1
• 氢受体数：
  9

文献信息

• Pyrazolopyrimidinone Derivatives, Their Preparation And Their Use
  申请人：Tian Guanghui

  公开号：US20080318949A1

  公开（公告）日：2008-12-25

  The invention discloses a series of pyrazolopyrimidinone derivatives, which have the following chemical structure, their preparation methods and use, It has been proved by pharmacological experiment that the said pyrazolopyrimidinone derivatives have high inhibitory activity against PDE5, and parts of them have a much stronger potency against PDE5 than against PDE6. Most of the compounds show low toxicity. The pyrazolopyrimidinone derivatives can be used in clinics for the palliative or curative treatment of symptoms or diseases relating to cardiovascular system, urinary system, especially for the palliative or curative treatment of erectile dysfunction.

  本发明公开了一系列嘧唑吡咯啉酮衍生物，其化学结构如下，以及它们的制备方法和用途。经过药理实验证明，所述嘧唑吡咯啉酮衍生物对PDE5具有高抑制活性，其中部分化合物对PDE5的抑制活性比对PDE6更强。大多数化合物显示出低毒性。这些嘧唑吡咯啉酮衍生物可用于临床上缓解或治疗与心血管系统、泌尿系统有关的症状或疾病，特别是用于缓解或治疗勃起功能障碍。