5-[4-(diethylamino)benzyl]-1-methyl-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-one | 223430-04-4

• 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: 5-[4-(diethylamino)benzyl]-1-methyl-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-one
• 英文别名: 5-(4-Diethylamino-benzyl)-1-methyl-3-propyl-1,6-dihydro-pyrazolo[4,3-D]pyrimidin-7-one；5-[[4-(diethylamino)phenyl]methyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-one
• CAS: 223430-04-4
• 化学式: C₂₀H₂₇N₅O
• 分子量: 353.467
• InChiKey: ORMBCFWPACLYFR-UHFFFAOYSA-N

物化性质

• 密度：
  1.18±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  26
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  62.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  N-ethyl-N-{4-[(1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)methyl]phenyl}acetamide 以45%的产率得到5-[4-(diethylamino)benzyl]-1-methyl-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-one
  参考文献：
  名称：

  5-substituted pyrazolo[4,3-D]pyrimidin-7-ones

  摘要：

  抑制PDE1的化合物已被披露。这些化合物的化学式如下：

  公开号：

  US06235742B1

文献信息

• PDE9 inhibitors for treating cardiovascular disorders
  申请人：Pfizer Inc.

  公开号：US20030195205A1

  公开（公告）日：2003-10-16

  The invention relates to PDE9 inhibitors for treating cardiovascular disorders. Preferred PDE9 inhibitors are compounds of formula I wherein R 1 is H or C 1-6 alkyl, wherein R 1 is attached to either N 1 or N 2 ; R 2 is C 1-6 alkyl optionally substituted by hydroxy or alkoxy; C 3-7 cycloalkyl optionally substituted by alkyl, hydroxy or alkoxy; a saturated 5-6-membered heterocycle optionally substituted by alkyl, hydroxy or alkoxy; het1 or Ar 1 ; R 3 is C 1-6 alkyl optionally substituted by 1 or 2 groups independently selected from: Ar 2 ; C 3-7 cycloalkyl optionally substituted by C 1-6 alkyl; OAr 2 ; SAr 2 ; NHC(O)C 1-6 alkyl; het 2 ; xanthene; and naphthalene. 1

  该发明涉及用于治疗心血管疾病的PDE9抑制剂。首选的PDE9抑制剂是具有以下结构的化合物，其中R1是H或C1-6烷基，其中R1连接到N1或N2中的任一者；R2是C1-6烷基，可选择地被羟基或烷氧基取代；C3-7环烷基，可选择地被烷基、羟基或烷氧基取代；饱和的5-6成员杂环，可选择地被烷基、羟基或烷氧基取代；het1或Ar1；R3是C1-6烷基，可选择地被从Ar2中独立选择的1或2个基团取代；C3-7环烷基，可选择地被C1-6烷基取代；OAr2；SAr2；NHC(O)C1-6烷基；het2；黄酮；和萘。
• Phosphodiesterase inhibitors for the treatment of female sexual dysfunction
  申请人：Pfizer Limited

  公开号：EP1097706A1

  公开（公告）日：2001-05-09

  A method of treating a female suffering from femal sexual dysfunction (FSD), in particular femal sexual arousal dysfunction (FSAD), is described. The method comprises delivering to the female an agent that is capable of potentiating cAMP in the sexual genitalia; wherein the agent is in an amount to cause potentiation of cAMP in the sexual genitalia of the female. The agent may be admixed with a pharmaceutically acceptable carrier, diluent or excipient. Said agent is a phosphodiesterase (PDE) inhibitor wherein said PDE is a cAMP hydrolysing PDE (and optionally cGMP hydroysing).

  描述了一种治疗女性性功能障碍（FSD），特别是女性性唤醒功能障碍（FSAD）的方法。该方法包括向女性提供一种能够增强性生殖器内环磷酸腺苷（cAMP）的药物；其中，该药物的量足以引起女性性生殖器内cAMP的增强。该药物可以与药用可接受的载体、稀释剂或赋形剂混合。所述药物是一种磷酸二酯酶（PDE）抑制剂，其中所述PDE是一种cAMP水解PDE（可选地为cGMP水解）。
• Compounds for the treatment of female sexual dysfunction
  申请人：Pfizer Inc

  公开号：US20040254153A1

  公开（公告）日：2004-12-16

  A method of treating a female suffering from FSD, in particular FSAD, is described. The method comprises delivering to the female an agent that is capable of potentiating cAMP in the sexual genitalia; wherein the agent is in an amount to cause potentiation of cAMP in the sexual genitalia of the female. The agent may be admixed with a pharmaceutically acceptable carrier, diluent or excipient.

  本发明描述了一种治疗患有女性性功能障碍（FSD），特别是女性性唤起障碍（FSAD）的方法。该方法包括向女性输送一种能够在性生殖器中增强cAMP的药剂；其中该药剂的量足以在女性的性生殖器中引起cAMP的增强。该药剂可以与药学上可接受的载体、稀释剂或赋形剂混合。
• NEP inhibitors for the treatment of female sexual dysfunction
  申请人：Pfizer Limited

  公开号：EP1097719A1

  公开（公告）日：2001-05-09

  A method of treating a female suffering from female sexual dysfunction (FSD), in particular female sexual arousal dysfunction (FSAD), is described. The method comprises delivering to the female an agent that is capable of potentiating cAMP in the sexual genitalia; wherein the agent is in an amount to cause potentiation of cAMP in the sexual genitalia of the female. The agent may be admixed with a pharmaceutically acceptable carrier, diluent or excipient. Said agent is an inhibitor of NEP.

  描述了一种治疗女性性功能障碍（FSD），特别是女性性唤起功能障碍（FSAD）的方法。该方法包括向该女性提供一种能使性器官中的 cAMP 增效的药剂；其中药剂的用量能使该女性性器官中的 cAMP 增效。药剂可与药学上可接受的载体、稀释剂或赋形剂混合。所述药剂是 NEP 的抑制剂。
• Treatment of female sexual dysfunction
  申请人：Pfizer Limited

  公开号：EP1097707A1

  公开（公告）日：2001-05-09

  A method of treating a female suffering from female sexual dysfunction (FSD), in particular female sexual arousal dysfunction (FSAD), is described. The method comprises delivering to the female an agent that is capable of potentiating cAMP in the sexual genitalia; wherein the agent is in an amount to cause potentiation of cAMP in the sexual genitalia of the female. The agent may be admixed with a pharmaceutically acceptable carrier, diluent or excipient.

  描述了一种治疗女性性功能障碍（FSD），特别是女性性唤起功能障碍（FSAD）的方法。该方法包括向该女性提供一种能使性器官中的 cAMP 增效的药剂；其中药剂的用量能使该女性性器官中的 cAMP 增效。药剂可与药学上可接受的载体、稀释剂或赋形剂混合。