3-(3-pyridinyl)-5-(2-trifluoromethoxybenzyl)-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one | 521299-97-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 3-(3-pyridinyl)-5-(2-trifluoromethoxybenzyl)-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one
• 英文别名: 3-Pyridin-3-yl-5-[[2-(trifluoromethoxy)phenyl]methyl]-1,6-dihydropyrazolo[4,3-d]pyrimidin-7-one
• CAS: 521299-97-8
• 化学式: C₁₈H₁₂F₃N₅O₂
• 分子量: 387.321
• InChiKey: ZWURCJIAKXAOTE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  92.3
• 氢给体数：
  2
• 氢受体数：
  7

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。
• Treatment of insulin resistance syndrome and type 2 diabetes with PDE9 inhibitors
  申请人：——

  公开号：US20040023989A1

  公开（公告）日：2004-02-05

  This invention is directed to a method of treating insulin resistance syndrome (IRS), hypertension and/or type 2 diabetes in a mammal comprising administering to said mammal a cGMP PDE9 inhibitor or a pharmaceutical composition thereof. This invention is also directed to such methods wherein said cGMP PDE9 inhibitor is used in combination with other agents to treat IRS, hypertension and/or type 2 diabetes.

  本发明涉及一种治疗哺乳动物中胰岛素抵抗综合症（IRS）、高血压和/或2型糖尿病的方法，包括向该哺乳动物施用cGMP PDE9抑制剂或其制剂。本发明还涉及这样的方法，其中所述的cGMP PDE9抑制剂与其他药物联合使用以治疗IRS、高血压和/或2型糖尿病。
• TREATING AGENT OF UROPATHY
  申请人：Gotanda Kotaro

  公开号：US20100113484A1

  公开（公告）日：2010-05-06

  Disclosed is a treating agent of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria in benign prostatic hyperplasia or urolithiasis, which comprises a compound having PDE9-inhibiting activity as the active ingredient.

  本发明涉及一种治疗过度活跃膀胱综合症、排尿频繁、尿失禁、良性前列腺增生或泌尿结石引起的排尿困难的治疗剂，其包含一种具有PDE9抑制活性的化合物作为活性成分。
• THERAPEUTIC AGENT FOR URINARY TRACT DISEASE
  申请人：ASKA Pharmaceutical Co., Ltd.

  公开号：EP2123301A1

  公开（公告）日：2009-11-25

  Disclosed is a treating agent of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria in benign prostatic hyperplasia or urolithiasis, which comprises a compound having PDE9-inhibiting activity as the active ingredient.

  本发明公开了一种治疗膀胱过度活动症、花粉尿症、尿失禁、良性前列腺增生症排尿困难或尿路结石的药物，其活性成分包括一种具有 PDE9 抑制活性的化合物。
• PDE9 INHIBITORS FOR TREATING CARDIOVASCULAR DISORDERS
  申请人：Pfizer Limited

  公开号：EP1440073A1

  公开（公告）日：2004-07-28