5-[2-Ethoxy-5-(1-methyl-2-imidazolyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-[2-Ethoxy-5-(1-methyl-2-imidazolyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
• 英文别名: 5-[2-ethoxy-5-(1-methylimidazol-2-yl)phenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-one
• 化学式: C₂₁H₂₄N₆O₂
• 分子量: 392.5
• InChiKey: GFVZTCIYHIUUJO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  86.3
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  正丁基锂 、 N-甲基咪唑 、 5-(5-bromo-2-ethoxyphenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one 、 乙二胺四乙酸 二钠盐 二水合物 、 disodium;carbonate 在 氯化锌 、 四(三苯基膦)钯 二氯甲烷 、 Sodium sulfate-III 、 silica gel 、 methanol-dichloromethane 、 甲醇 、 乙酸乙酯 作用下， 以 四氢呋喃 、 水 、 甲醇 为溶剂， 反应 78.45h， 以gave the title compound as an off-white solid (0.542 g, 53%), m.p. 199-202° C的产率得到5-[2-Ethoxy-5-(1-methyl-2-imidazolyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
  参考文献：
  名称：

  Method of treating a patient having precancerous lesions with phenyl purinone derivatives

  摘要：

  苯基嘌呤酮衍生物对于治疗患有癌前病变的患者非常有用。这些化合物还可以用于抑制肿瘤细胞的生长。

  公开号：

  US06200980B1

文献信息

• BRADYKININ RECEPTOR AGONISTS AND USES THEREOF TO TREAT OCULAR HYPERTENSION AND GLAUCOMA
  申请人：Combrink Keith D.

  公开号：US20120046285A1

  公开（公告）日：2012-02-23

  The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.

  这项发明提供了用于治疗和/或预防与眼内压增高相关的眼部疾病的组合物和方法。具体来说，这些化合物是激肽酶激动剂。
• Treatment of diabetic ulcers
  申请人：——

  公开号：US20030176442A1

  公开（公告）日：2003-09-18

  This invention relates to the use of cyclic guanosine 3′, 5′-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of diabetic ulcers, particularly diabetic foot ulcers.

  这项发明涉及使用环状鸟苷酸3′,5′-单磷酸磷酸二酯酶五型（cGMP PDE5）抑制剂，特别是硝苯地平这种化合物，用于治疗糖尿病溃疡，特别是糖尿病足溃疡。
• Phosphodiesterase type 5 (PDE5) inhibitors for the treatment of selective serotonin reuptake inhibitor (SSR) induced sexual dysfunction
  申请人：——

  公开号：US20030055070A1

  公开（公告）日：2003-03-20

  This invention is directed to the use phosphodiesterase type 5 (PDE5) inhibitors in the treatment of selective serotonin reuptake inhibitor (SSRI) induced sexual dysfunction. Specifically, this invention is directed to a method for treating an animal to cure; prevent or ameliorate SSRI induced sexual dysfunction which comprises administering to the animal an effective amount of the inhibitor. The animal may be a male or a female human. The invention also includes the use of such inhibitors in the manufacture of a medicament to prevent; cure or ameliorate SSRI induced sexual dysfunction. Moreover, the invention includes a kit comprising a SSRI, such as sertraline, fluoxetine, paroxetine, and a PDE5 inhibitor, such as sildenafil citrate, for the treatment or prevention of serotonergic associated disorders such as depression, obsessive compulsive disorder or panic disorder, while reducing or preventing sexual dysfunction.

  该发明涉及使用磷酸二酯酶-5（PDE5）抑制剂治疗选择性血清素再摄取抑制剂（SSRI）引起的性功能障碍。具体而言，该发明涉及一种治疗动物以治愈、预防或改善SSRI引起的性功能障碍的方法，包括向动物施用有效量的抑制剂。该动物可以是男性或女性人类。该发明还包括将这些抑制剂用于制造药物以预防、治愈或改善SSRI引起的性功能障碍。此外，该发明还包括一种套装，其中包括SSRI（如舍曲林、氟西汀、帕罗西汀）和PDE5抑制剂（如西地那非）用于治疗或预防血清素相关疾病，如抑郁症、强迫症或惊恐症，同时减少或预防性功能障碍。
• cGMP PDE 5 Inhibitors for inhalation in the treatment of sexual dysfunction
  申请人：——

  公开号：US20010055570A1

  公开（公告）日：2001-12-27

  Treatment of sexual dysfunction by inhalation of a cGMP PDE 5 inhibitor, especially 5-[2-ethoxy-5-(4-methylpiperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one, 4-phenylmethylamino-6-chloro-2-(1-imidazolyl) quinazoline, 4-phenylmethylamino-6-chloro-2-(3-pyridyl) quinazoline, 1,3-dimethyl-6-(2-propoxy-5-methanesulfonylamidophenyl)-1,5-dihydropyrazolo[3,4-d]pyrimidin-4-one or 1-cyclopentyl-3-ethyl-6-(3-ethoxy-4-pyridyl)-pyrazolo[3,4-d]pyrimidin-4-one.

  通过吸入cGMP PDE 5抑制剂治疗性功能障碍，特别是5-[2-乙氧基-5-(4-甲基哌嗪磺酰基)苯基]-1-甲基-3-正丙基-1,6-二氢-7H-吡唑并[4,3-d]嘧啶-7-酮、4-苯甲基氨基-6-氯-2-(1-咪唑基)喹唑啉、4-苯甲基氨基-6-氯-2-(3-吡啶基)喹唑啉、1,3-二甲基-6-(2-丙氧基-5-甲烷磺酰胺基苯基)-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮或1-环戊基-3-乙基-6-(3-乙氧基-4-吡啶基)-吡唑并[3,4-d]嘧啶-4-酮。
• cGMP PDE 5 inhibitors for inhalation in the treatment of sexual dysfunction
  申请人：——

  公开号：US20040214831A1

  公开（公告）日：2004-10-28

  Treatment of sexual dysfunction by inhalation of a cGMP PDE 5 inhibitor, especially 5-[2-ethoxy-5-(4-methylpiperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one, 4-phenylmethylamino-6-chloro-2-(1-imidazolyl) quinazoline, 4-phenylmethylamino-6-chloro-2-(3-pyridyl) quinazoline, 1,3-dimethyl-6-(2-propoxy-5-methanesulfonylamidophenyl)-1,5-dihydropyrazolo[3,4-d]pyrimidin-4-one or 1-cyclopentyl-3-ethyl-6-(3-ethoxy-4-pyridyl)-pyrazolo[3,4-d]pyrimidin-4-one.

  通过吸入cGMP PDE 5抑制剂治疗性功能障碍，特别是5-[2-乙氧基-5-(4-甲基哌嗪磺酰基)苯基]-1-甲基-3-正丙基-1,6-二氢-7H-吡唑并[4,3-d]嘧啶-7-酮，4-苯甲氨基-6-氯-2-(1-咪唑基)喹唑啉，4-苯甲氨基-6-氯-2-(3-吡啶基)喹唑啉，1,3-二甲基-6-(2-丙氧基-5-甲磺酰胺基苯基)-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮或1-环戊基-3-乙基-6-(3-乙氧基-4-吡啶基)-吡唑并[3,4-d]嘧啶-4-酮。