1-methyl-5-(2-propoxy-5-[[1-benzyl-1-(2-hydroxyethyl)]amidosulfonyl]phenyl)-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | 936951-08-5

• 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-methyl-5-(2-propoxy-5-[[1-benzyl-1-(2-hydroxyethyl)]amidosulfonyl]phenyl)-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
• 英文别名: 1-methyl-5-{2-propoxy-5-[[1-benzyl-1-(2-hydroxyethyl)]amidosulfonyl]phenyl}-3-n-propyl-1,6-dihyro-7H-pyrazolol[4,3-d]pyrimidin-7-one；N-benzyl-N-(2-hydroxyethyl)-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide
• CAS: 936951-08-5
• 化学式: C₂₇H₃₃N₅O₅S
• 分子量: 539.656
• InChiKey: OBZXKHYLEPAQPO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  38
• 可旋转键数：
  12
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  135
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• PYRAZOLOPYRIMIDINONE DERIVATIVES, THEIR PREPARATION AND THEIR USE
  申请人：Topharman Shanghai Co., Ltd.

  公开号：EP1961753A1

  公开（公告）日：2008-08-27

  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吡唑嘧啶酮衍生物，其化学结构、制备方法和用途如下、 药理实验证明，上述吡唑嘧啶酮衍生物对 PDE5 具有很高的抑制活性，其中部分衍生物对 PDE5 的抑制作用比对 PDE6 的抑制作用强得多。大多数化合物的毒性较低。这些吡唑嘧啶酮衍生物可用于临床，缓解或治疗与心血管系统、泌尿系统有关的症状或疾病，特别是缓解或治疗勃起功能障碍。