3-phenyl-6-(3-phenylazetidin-1-ylmethyl)-7H-imidazo-[1,5-a]pyrazin-8-one | 1430840-01-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-phenyl-6-(3-phenylazetidin-1-ylmethyl)-7H-imidazo-[1,5-a]pyrazin-8-one
• 英文别名: 3-phenyl-6-[(3-phenylazetidin-1-yl)methyl]-7H-imidazo[1,5-a]pyrazin-8-one
• CAS: 1430840-01-9
• 化学式: C₂₂H₂₀N₄O
• 分子量: 356.427
• InChiKey: UIIQLHYXQBZHDU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  50.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  5-氨基-3-甲氧基吡嗪-2-腈 在 4-二甲氨基吡啶 、 sodium tetrahydroborate 、 copper(l) iodide 、 氯化亚砜 、 palladium bis[bis(diphenylphosphino)ferrocene] dichloride 、 二碘甲烷 、 氨 、 氢气 、 三溴化硼 、 三乙胺 、 N,N-二异丙基乙胺 、 三氟乙酸 、 三氯氧磷 、 亚硝酸异戊酯 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 乙腈 为溶剂， 85.0 ℃ 、3.0 MPa 条件下， 反应 34.0h， 生成 3-phenyl-6-(3-phenylazetidin-1-ylmethyl)-7H-imidazo-[1,5-a]pyrazin-8-one
  参考文献：
  名称：

  [EN] PDE9I WITH IMIDAZO PYRAZINONE BACKBONE
  [FR] PDE9I AYANT UN SQUELETTE IMIDAZO PYRAZINONE

  摘要：

  该发明涉及一类PDE9酶抑制剂化合物。该发明提供了一种药物组合物，包括该发明化合物的治疗有效量和药用载体。本发明还提供了制备式(I)化合物的方法。本发明还提供了一种治疗患有神经退行性疾病的受试者的方法，包括向受试者投与式(I)化合物的治疗有效量。本发明还提供了一种治疗患有精神疾病的受试者的方法，包括向受试者投与式(I)化合物的治疗有效量。

  公开号：

  WO2013053690A1

文献信息

• PDE9i with imidazo pyrazinone backbone
  申请人：H. LUNDBECK A/S

  公开号：US20150274736A1

  公开（公告）日：2015-10-01

  This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).

  本发明涉及一种PDE9酶抑制剂化合物。该发明提供了一种药物组合物，包括本发明化合物的治疗有效量和药学可接受的载体。本发明还提供了制备式（I）化合物的方法。本发明还提供了一种治疗神经退行性疾病的方法，包括向患者投与式（I）化合物的治疗有效量。本发明还提供了一种治疗精神障碍的方法，包括向患者投与式（I）化合物的治疗有效量。
• PDE9 INHIBITOR WITH IMIDAZO PYRAZINONE BACKBONE
  申请人：H. Lundbeck A/S

  公开号：EP3121178A1

  公开（公告）日：2017-01-25

  This invention is directed to 6-[4-METHYL-1-(PYRlMIDIN-2-YLMETHYL)PYRROLIDIN-3-YL]-3-TETRAHYDROPYRAN-4-YL-7H-IMIDAZO[1,5-A]PYRAZIN-8-ONE and pharmaceutically acceptable acid addition salts thereof, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of invention. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of the invention. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).

  本发明涉及6-[4-甲基-1-(PYRlMIDIN-2-YLMEYTHL)PYRROLIDIN-3-YL]-3-四氢吡喃-4-YL-7H-IMIDAZO[1,5-A]PYRAZIN-8-ONE及其药学上可接受的酸加成盐，它们是PDE9酶抑制剂。本发明提供了一种药物组合物，其包含治疗有效量的本发明化合物和药学上可接受的载体。本发明还提供了制备本发明化合物的工艺。本发明进一步提供了一种治疗患有神经退行性疾病的受试者的方法，该方法包括向受试者施用治疗有效量的本发明化合物。本发明进一步提供了一种治疗精神疾病患者的方法，包括对该患者施用治疗有效量的式(I)化合物。
• PDE9I WITH IMIDAZO PYRAZINONE BACKBONE
  申请人：H. Lundbeck A/S

  公开号：EP2906562A1

  公开（公告）日：2015-08-19
• 6-[4-METHYL-1-(PYRIMIDIN-2-YLMETHYL)PYRROLIDIN-3-YL]-3-TETRAHYDROPYRAN-4-YL-7H-IMIDAZO[1,5-A]PYRAZIN-8-ONE AS PDE9 INHIBITOR
  申请人：H. Lundbeck A/S

  公开号：EP3121178B1

  公开（公告）日：2018-09-19
• SUBSTITUTED IMIDAZO[1,5-a]PYRAZINES AS PDE9 INHIBITORS
  申请人：H. LUNDBECK A/S

  公开号：US20170173018A1

  公开（公告）日：2017-06-22

  This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I) The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).