8-difluoromethoxy-3-methyl-4-methylsulfonylamino-1-propyl-imidazo[1,5-a]pyrido[3,2-e]pyrazine

• 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: 8-difluoromethoxy-3-methyl-4-methylsulfonylamino-1-propyl-imidazo[1,5-a]pyrido[3,2-e]pyrazine
• 英文别名: N-[4-(difluoromethoxy)-11-methyl-13-propyl-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),5,7,10-tetraen-10-yl]methanesulfonamide
• 化学式: C₁₅H₂₁F₂N₅O₃S
• 分子量: 389.426
• InChiKey: IDUMJWOBOYQMGT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  85.9
• 氢给体数：
  1
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  3-methyl-4-methylsulfonylamino-1-propyl-imidazo[1,5-a]pyrido[3,2-e]pyrazin-8-ol 、 二氟氯乙酸 在 sodium hydroxide 作用下， 以 N-甲基乙酰胺 为溶剂， 生成 8-difluoromethoxy-3-methyl-4-methylsulfonylamino-1-propyl-imidazo[1,5-a]pyrido[3,2-e]pyrazine
  参考文献：
  名称：

  Methods of Treating Obesity and Metabolic Disorders

  摘要：

  本发明涉及使用PDE10抑制剂pyrido [3,2-e] pyrazines治疗或预防肥胖症、2型糖尿病、代谢综合征或葡萄糖不耐症的方法。本发明还涉及减少体脂肪或体重的方法。

  公开号：

  US20090143392A1

文献信息

• Pyrido[3,2-e]pyrazines, their use as inhibitors of phospohodiesterase 10, and processes for preparing them
  申请人：Hofgen Norbert

  公开号：US20090239874A1

  公开（公告）日：2009-09-24

  The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.

  本发明涉及吡啶并[3,2-e]吡嗪、其制备方法、含有该化合物的制药组合物以及将其作为磷酸二酯酶10的抑制剂的活性化合物，用于治疗哺乳动物包括人类的疾病，这些疾病可以通过使用本发明的化合物来抑制中枢神经系统中的磷酸二酯酶10活性来影响。具体而言，本发明涉及神经逻辑和精神障碍的治疗，例如精神病和包括认知缺陷症状的障碍。
• Pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
  申请人：Hofgen Norbert

  公开号：US20080027064A1

  公开（公告）日：2008-01-31

  The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.

  本发明涉及吡啶并[3,2-e]吡嗪类化合物、其制备方法、包含这些化合物的制药组合物以及这些化合物的制药用途。该化合物是磷酸二酯酶10的抑制剂，可用作治疗哺乳动物包括人类的疾病的活性成分，这些疾病可以通过使用本发明的化合物抑制中枢神经系统中的磷酸二酯酶10活性来影响。具体而言，本发明涉及治疗神经和精神障碍，例如包括认知缺陷症状的精神病和障碍的治疗。
• PYRIDO[3,2-e]PYRAZINES, THEIR USE AS INHIBITORS OF PHOSPHODIESTERASE 10, AND PROCESSES FOR PREPARING THEM
  申请人：Elbion Gmbh

  公开号：EP2021342A1

  公开（公告）日：2009-02-11
• US7550465B2
  申请人：——

  公开号：US7550465B2

  公开（公告）日：2009-06-23
• [EN] PYRIDO[3,2-e]PYRAZINES, THEIR USE AS INHIBITORS OF PHOSPHODIESTERASE 10, AND PROCESSES FOR PREPARING THEM<br/>[FR] PYRIDO[3,2-e]PYRAZINES, LEUR UTILISATION COMME INHIBITEURS DE LA PHOSPHODIESTÉRASE 10, ET LEURS MÉTHODES DE PRÉPARATION
  申请人：ELBION AG

  公开号：WO2007137820A1

  公开（公告）日：2007-12-06

  [EN] The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.
  [FR] L'invention concerne des pyrido[3,2-e]pyrazines, leurs méthodes de préparation, des préparations pharmaceutiques comprenant ces composés, et l'utilisation pharmaceutique de ces composés, qui sont des inhibiteurs de la phosphodiestérase 10, comme composés actifs destinés au traitement de maladies de mammifères, dont les êtres humains, maladies sur lesquelles les composés de l'invention peuvent agir par inhibition de l'activité de la phosphodiestérase 10 dans le système nerveux central. L'invention concerne plus particulièrement le traitement de troubles neurologiques et psychiatriques, tels que la psychose ou des troubles dont un des symptômes est le déficit cognitif.