(3-fluoro-4-hydroxy-phenyl)-(2-(S)-pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-methanone

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (3-fluoro-4-hydroxy-phenyl)-(2-(S)-pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-methanone
• 英文别名: (3-fluoro-4-hydroxy-phenyl)-((S)-2-pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-methanone；(3-Fluoro-4-hydroxy-phenyl)-(2-(S)-pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)methanone；(3-fluoro-4-hydroxyphenyl)-[(2S)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]methanone
• 化学式: C₁₆H₂₁FN₂O₂
• 分子量: 292.353
• InChiKey: UWFQJRPDHJLFQU-ZDUSSCGKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  43.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (3-fluoro-4-hydroxy-phenyl)-(2-(S)-pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-methanone 、 1-碘丁烷 在 caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 12.0h， 以26%的产率得到S-(4-butoxy-3-fluoro-phenyl)-(2-pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-methanone
  参考文献：
  名称：

  WO2006/101808

  摘要：

  公开号：

文献信息

• [EN] HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES<br/>[FR] AGENTS RECEPTEURS DE L'HISTAMINE H3, PREPARATION ET UTILISATIONS THERAPEUTIQUES
  申请人：LILLY CO ELI

  公开号：WO2005121080A1

  公开（公告）日：2005-12-22

  The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.

  本发明公开了化合物I式或其药学上可接受的盐的新颖化合物，其具有组胺-H3受体拮抗剂或反向激动剂活性，以及制备这些化合物的方法。在另一实施例中，本发明公开了包括化合物I式的药物组合物，以及使用这些组合物治疗肥胖症、认知缺陷、嗜睡病和其他组胺H3受体相关疾病的方法。
• Pyrrolidine Derivatives as Histamine H3 Receptor Antagonists
  申请人：Beavers Lisa Selsam

  公开号：US20080207732A1

  公开（公告）日：2008-08-28

  The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.

  本发明披露了公式（I）的新化合物或其药学上可接受的盐，具有组胺-H3受体拮抗剂或反向激动剂活性，以及制备这些化合物的方法和中间体。在另一种实施方式中，本发明披露了包含公式（I）化合物的药物组合物，以及使用它们治疗肥胖、认知障碍、嗜睡症和其他组胺H3受体相关疾病的方法。
• HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
  申请人：Beavers Lisa Selsam

  公开号：US20090118254A1

  公开（公告）日：2009-05-07

  The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.

  本发明披露了公式I的新化合物或其药学上可接受的盐，其具有组胺H3受体拮抗剂或反向激动剂活性，以及制备这些化合物的方法。在另一种实施方式中，本发明披露了包括公式I化合物的制药组合物，以及使用这些组合物治疗肥胖症、认知缺陷、嗜睡病和其他组胺H3受体相关疾病的方法。
• Histamine H3 receptor agents, preparation and therapeutic uses
  申请人：Eli Lilly and Company

  公开号：US07696234B2

  公开（公告）日：2010-04-13

  The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.

  本发明公开了一种新的化合物I或其药学上可接受的盐，其具有组胺H3受体拮抗剂或反向激动剂活性，以及制备这些化合物的方法。在另一种实施方式中，本发明公开了包含化合物I的药物组合物，以及使用这些组合物治疗肥胖症、认知缺陷、嗜睡病和其他组胺H3受体相关疾病的方法。
• PYRROLIDINE DERIVATIVES AS HISTAMINE H3 RECEPTOR ANTAGONISTS
  申请人：ELI LILLY AND COMPANY

  公开号：EP1861360A1

  公开（公告）日：2007-12-05