(1-benzyl-piperidin-4-yl)-(3-chloro-pyrazin-2-yl)-amine | 943019-00-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (1-benzyl-piperidin-4-yl)-(3-chloro-pyrazin-2-yl)-amine
• 英文别名: N-(1-benzylpiperidin-4-yl)-3-chloropyrazin-2-amine
• CAS: 943019-00-9
• 化学式: C₁₆H₁₉ClN₄
• 分子量: 302.807
• InChiKey: OMCIWTFQYKBTEU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  41
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (1-benzyl-piperidin-4-yl)-(3-chloro-pyrazin-2-yl)-amine 在 盐酸 、 水 作用下， 反应 16.0h， 以70%的产率得到3-[(1-benzylpiperidin-4-yl)amino]-1H-pyrazin-2-one
  参考文献：
  名称：

  WO2007/122173

  摘要：

  公开号：
• 作为产物：
  描述：

  2,3-二氯吡嗪 、 4-氨基-1-苄基哌啶 在 sodium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以74%的产率得到(1-benzyl-piperidin-4-yl)-(3-chloro-pyrazin-2-yl)-amine
  参考文献：
  名称：

  WO2007/122173

  摘要：

  公开号：

文献信息

• SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE AS A MEDICINE
  申请人：Andrés-Gil José Ignacio

  公开号：US20100105694A1

  公开（公告）日：2010-04-29

  The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in claim 1 , having selective 2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

  本发明涉及通式（I）的取代吡唑酮衍生物，其为药学上可接受的酸性或碱性盐、立体化学异构体形式、N-氧化物形式或季铵盐，其中变量在权利要求1中定义，具有选择性2C-肾上腺素受体拮抗剂活性。本发明还涉及它们的制备、包含它们的组合物及其用作药物。根据本发明的化合物对于预防和/或治疗中枢神经系统疾病、情绪障碍、焦虑症、与抑郁和/或焦虑有关的应激相关障碍、认知障碍、人格障碍、情感性精神病、帕金森病、阿尔茨海默病型痴呆、慢性疼痛症状、神经退行性疾病、成瘾障碍、情感障碍和性功能障碍方面具有用处。
• WO2007/71639
  申请人：——

  公开号：——

  公开（公告）日：——
• WO2008/43775
  申请人：——

  公开号：——

  公开（公告）日：——
• SUBSTITUTED PYRAZINONE DERIVATIVES AS ALPHA2C-ADRENORECEPTOR ANTAGONISTS
  申请人：Janssen Pharmaceutica N.V.

  公开号：EP1966191B1

  公开（公告）日：2010-03-17
• Substituted Pyrazinone Derivatives as Alpha2C-Adrenoreceptor Antagonists
  申请人：Andre-Gil Jose Ignacio

  公开号：US20080269251A1

  公开（公告）日：2008-10-30

  The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1 , having selective α 2C -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.