5-(4-amino-2-methoxyphenyl)-1-cyclohexyl-3-methyl-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 - 吡唑并嘧啶类
• 英文名称: 5-(4-amino-2-methoxyphenyl)-1-cyclohexyl-3-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
• 英文别名: 5-(4-amino-2-methoxyphenyl)-1-cyclohexyl-3-methyl-6H-pyrazolo[4,3-d]pyrimidin-7-one
• 化学式: C₁₉H₂₃N₅O₂
• 分子量: 353.424
• InChiKey: BBEQXRUPYAKWEQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  94.5
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  四氢吡喃酮 、 5-(4-amino-2-methoxyphenyl)-1-cyclohexyl-3-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one 、 1,2-二氯乙烷 在 三乙酰氧基硼氢化钠 、 溶剂黄146 、 碳酸氢钠 作用下， 以 水 为溶剂， 反应 46.5h， 以49%的产率得到1-cyclohexyl-5-[2-methoxy-4-(tetrahydro-2H-pyran-4-ylamino)phenyl]-3-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
  参考文献：
  名称：

  PYRAZOLOPYRIMIDINONE DERIVATIVES HAVING PDE7-INHIBITORY ACTIVITY

  摘要：

  公开号：

  EP1454897B1

文献信息

• Pyrazolopyrimidinone derivatives having PDE7 inhibiting action
  申请人：Inoue Hidekazu

  公开号：US20050148604A1

  公开（公告）日：2005-07-07

  Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): and the following general formula (IA′) or (IB′): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds have the action of selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, they are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.

  本发明提供了以下通式(IA)或(IB)所表达的吡唑并嘧啶酮衍生物，以及以下通式(IA′)或(IB′)所表达的吡唑并嘧啶酮衍生物：其中所述符号如本说明书所披露的那样，作为所需的化合物提供。这些化合物具有选择性地抑制PDE7的作用，从而增加细胞内cAMP水平并抑制T细胞的活化。因此，它们对于预防和治疗各种过敏性疾病和炎症或免疫性疾病是有用的。
• Treatment of Addiction and Impulse-Control Disorders Using PDE7 Inhibitors
  申请人：OMEROS CORPORATION

  公开号：US20130267502A1

  公开（公告）日：2013-10-10

  This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.

  本公开涉及使用磷酸二酯酶7（PDE7）抑制剂，单独或与其他治疗药物联合治疗成瘾和原发性冲动控制障碍。
• USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS
  申请人：Omeros Corporation

  公开号：US20160015715A1

  公开（公告）日：2016-01-21

  A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.

  本发明涉及一种治疗神经运动障碍病理学相关的运动异常的方法，例如帕金森病或不宁腿综合症，通过给予治疗有效量的PDE7抑制剂。本发明的一个方面提供了与多巴胺激动剂或前体（例如左旋多巴）一起给予PDE7抑制剂的治疗方法。在本发明的另一个方面，PDE7抑制剂可以选择性地作用于PDE7，而相对于其他分子靶点（i）已知与帕金森病的病理学有关或（ii）其他治疗帕金森病的药物作用的靶点。
• PYRAZOLOPYRIMIDINONE DERIVATIVES HAVING PDE7−INHIBITORY ACTIVITY
  申请人：Daiichi Suntory Pharma Co., Ltd.

  公开号：EP1454897A1

  公开（公告）日：2004-09-08

  Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): and the following general formula (IA') or (IB'): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds have the action of selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, they are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.

  由以下通式（IA）或（IB）表示的吡唑嘧啶酮衍生物： 和以下通式（IA'）或（IB'）表示的吡唑嘧啶酮衍生物： 其中的符号如说明书中所披露的，作为所需的化合物提供。 这些化合物具有选择性抑制 PDE7 的作用，从而提高细胞内 cAMP 水平并抑制 T 细胞的活化。因此，它们可用于预防和治疗各种过敏性疾病和炎症性或免疫性疾病。
• Treatment of addiction and impulse-control disorders using PDE7 inhibitors
  申请人：Omeros Corporation

  公开号：US11207275B2

  公开（公告）日：2021-12-28

  This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.

  本公开内容涉及使用磷酸二酯酶 7 (PDE7) 抑制剂单独或与其他治疗剂联合治疗成瘾症和原发性冲动控制障碍。