2-(azetidin-3-yloxy)pyrazine | 1343323-27-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(azetidin-3-yloxy)pyrazine
• CAS: 1343323-27-2
• 化学式: C₇H₉N₃O
• 分子量: 151.168
• InChiKey: GNPOUHBTAAICIH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  47
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  benzyl 3-(3-chloropyrazin-2-yloxy)azetidine-1-carboxylate 在 钯 氮气 、 氢气 、 乙酸乙酯 作用下， 以 乙醇 为溶剂， 反应 16.52h， 以to give crude 2-(azetidin-3-yloxy)pyrazine (0.188 g, 181% yield)的产率得到2-(azetidin-3-yloxy)pyrazine
  参考文献：
  名称：

  HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS

  摘要：

  杂环氧基杂环芳基化合物，以及含有它们的组合物和制备这些化合物的方法。此外，本文还提供了治疗可通过PDE10抑制治疗的疾病或疾病的方法，例如肥胖症、非胰岛素依赖性糖尿病、精神分裂症、亨廷顿病、双相障碍、强迫症等。

  公开号：

  US20130253186A1

文献信息

• POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4
  申请人：Vanderbilt University

  公开号：US20170369505A1

  公开（公告）日：2017-12-28

  Disclosed herein are tricyclic compounds, including pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine-8-amine, pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine-4-amine, pyrazino[2′,3′:4,5]thieno[3,2-d]pyrimidin-4-amine, pyrido[3′,2′:4,5]furo[3, 2-d]pyrimidin-4-amine, and pyrimido[4′,5′:4,5]furo[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

  本文披露了三环化合物，包括嘧啶并[4′,5′:4,5]噻吩并[2,3-c]吡啶嗪-8-胺，吡啶并[3′,2′:4,5]噻吩并[3,2-d]嘧啶-4-胺，吡嗪并[2′,3′:4,5]噻吩并[3,2-d]嘧啶-4-胺，吡啶并[3′,2′:4,5]呋喃[3,2-d]嘧啶-4-胺，以及嘧啶并[4′,5′:4,5]呋喃[2,3-c]吡啶嗪-8-胺化合物，这些化合物可能作为肌胆碱受体M4（mAChR M4）的正向变构调节剂而有用。本文还披露了制备这些化合物的方法，包括这些化合物的药物组合物，以及使用这些化合物和组合物治疗与肌胆碱受体功能障碍相关的神经和精神疾病的方法。
• [EN] HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS<br/>[FR] COMPOSÉS D'HÉTÉROARYLOXYHÉTÉROCYCLYLE CONVENANT COMME INHIBITEURS DE LA PDE10
  申请人：AMGEN INC

  公开号：WO2011143495A1

  公开（公告）日：2011-11-17

  Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.

  杂芳基氧杂环基化合物，以及含有它们的组合物，以及制备这类化合物的方法。本文还提供了通过抑制PDE10治疗可治疗的疾病或病症的方法，例如肥胖症、非胰岛素依赖型糖尿病、精神分裂症、亨廷顿病、双相情感障碍、强迫症等。
• HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS
  申请人：Allen Jennifer R.

  公开号：US20110306588A1

  公开（公告）日：2011-12-15

  Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.

  本文提供了杂环氧杂芳基化合物及其组合物，以及制备这种化合物的方法。此外，还提供了治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症、非胰岛素依赖型糖尿病、精神分裂症、亨廷顿病、双相情感障碍、强迫症等。
• 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。
• Positive allosteric modulators of the muscarinic acetylcholine receptor M4
  申请人：Vanderbilt University

  公开号：US10239887B2

  公开（公告）日：2019-03-26

  Disclosed herein are tricyclic compounds, including pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine-8-amine, pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine-4-amine, pyrazino[2′,3′:4,5]thieno[3,2-d]pyrimidin-4-amine, pyrido[3′,2′:4,5]furo[3,2-d]pyrimidin-4-amine, and pyrimido[4′,5′:4,5]furo[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

  本文公开的三环化合物包括嘧啶并[4′,5′:4,5]噻吩并[2,3-c]哒嗪-8-胺、吡啶并[3′,2′：4,5]噻吩并[3,2-d]嘧啶-4-胺、吡嗪并[2′,3′:4,5]噻吩并[3,2-d]嘧啶-4-胺、吡啶并[3′,2′：4,5]呋喃并[3,2-d]嘧啶-4-胺和嘧啶并[4′,5′:4,5]呋喃并[2,3-c]哒嗪-8-胺化合物，这些化合物可用作毒蕈碱乙酰胆碱受体M4（mAChR M4）的正异位调节剂。本文还公开了制造这些化合物的方法、包含这些化合物的药物组合物，以及使用这些化合物和组合物治疗与毒蕈碱乙酰胆碱受体功能障碍相关的神经和精神疾病的方法。