2-[3-(12-Cyclopropyl-7-methyl-2,4,5,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-3-yl)-4-methylphenyl]propan-2-ol | 1552287-30-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-[3-(12-Cyclopropyl-7-methyl-2,4,5,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-3-yl)-4-methylphenyl]propan-2-ol
• 英文别名: 2-[3-(12-cyclopropyl-7-methyl-2,4,5,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-3-yl)-4-methylphenyl]propan-2-ol
• CAS: 1552287-30-5
• 化学式: C₂₂H₂₃N₅O
• 分子量: 373.458
• InChiKey: JPJVFAWCZLFVAJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  76.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1-[3-(12-Cyclopropyl-7-methyl-2,4,5,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-3-yl)-4-methylphenyl]ethanone 在 manganese(IV) oxide 、 lithium aluminium tetrahydride 、 sodium hydroxide 作用下， 以 四氢呋喃 、 二氯甲烷 、 水 为溶剂， 反应 3.17h， 生成 2-[3-(12-Cyclopropyl-7-methyl-2,4,5,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-3-yl)-4-methylphenyl]propan-2-ol
  参考文献：
  名称：

  [EN] 4-METHYL-2,3,5,9,9B-PENTAAZA-CYCLOPENTA[A]NAPHTHALENES
  [FR] 4-MÉTHYL-2,3,5,9,9B-PENTAAZA-CYCLOPENTA[A]NAPHTALÈNES

  摘要：

  该发明涉及一般式(I)的4-甲基-2,3,5,9,9b-五氮杂-环戊[α]萘衍生物，它们是磷酸二酯酶2和/或10的抑制剂，可用于治疗中枢神经系统疾病和其他疾病。此外，该发明涉及制备药物组合物的方法，以及根据该发明制造化合物的方法。

  公开号：

  WO2014019979A1

文献信息

• 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes
  申请人：GIOVANNINI Riccardo

  公开号：US20140045856A1

  公开（公告）日：2014-02-13

  The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

  这项发明涉及一般式(I)的4-甲基-2,3,5,9,9b-五氮杂-环戊[α]萘衍生物，它们是磷酸二酯酶2和/或10的抑制剂，可用于治疗中枢神经系统疾病和其他疾病。此外，该发明涉及制备药物组合物的方法，以及根据该发明制造化合物的方法。
• Treatment of tachycardia
  申请人：OSLO UNIVERSITY HOSPITAL HF

  公开号：US11419874B2

  公开（公告）日：2022-08-23

  The invention provides compounds which are selective PDE2 inhibitors for use in the treatment of tachycardia or tachyarrhythmia Such compounds are particularly suitable for use in the treatment of any of the following conditions: atrial tachycardia, atrial fibrillation, atrial flutter, paroxysmal supraventricular tachycardia, premature ventricular contractions (PVCs), ventricular fibrillation and ventricular tachycardia, and may be used alone or in combination therapy with other conventional cardiovascular drugs, e.g. beta-blockers. In particular, the invention provides compounds which are selective PDE2 inhibitors for use in the treatment of ventricular tachycardia in patients who are suffering from, or who are at risk of suffering from heart failure, CPVT or long QT syndrome.

  本发明提供了用于治疗心动过速或心动过速性心律失常的选择性 PDE2 抑制剂化合物：心房性心动过速、心房颤动、心房扑动、阵发性室上性心动过速、室性早搏 （PVC）、心室颤动和室性心动过速，可单独使用或与其它常规心血管药物（如 β-受体阻滞剂）联合使用。如β-受体阻滞剂。特别是，本发明提供的化合物是选择性 PDE2 抑制剂，可用于治疗心力衰竭、CPVT 或长 QT 综合征患者的室性心动过速或有此风险的患者的室性心动过速。
• 4-METHYL-2,3,5,9,9B-PENTAAZA-CYCLOPENTA[A]NAPHTHALENES
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP2882749B1

  公开（公告）日：2018-04-04
• TREATMENT OF TACHYCARDIA
  申请人：OSLO UNIVERSITY HOSPITAL HF

  公开号：US20200345744A1

  公开（公告）日：2020-11-05

  The invention provides compounds which are selective PDE2 inhibitors for use in the treatment of tachycardia or tachyarrhythmia Such compounds are particularly suitable for use in the treatment of any of the following conditions: atrial tachycardia, atrial fibrillation, atrial flutter, paroxysmal supraventricular tachycardia, premature ventricular contractions (PVCs), ventricular fibrillation and ventricular tachycardia, and may be used alone or in combination therapy with other conventional cardiovascular drugs, e.g. beta-blockers. In particular, the invention provides compounds which are selective PDE2 inhibitors for use in the treatment of ventricular tachycardia in patients who are suffering from, or who are at risk of suffering from heart failure, CPVT or long QT syndrome.
• US9085584B2
  申请人：——

  公开号：US9085584B2

  公开（公告）日：2015-07-21