6-(2,4-difluorophenoxy)nicotinic acid | 862088-72-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 6-(2,4-difluorophenoxy)nicotinic acid
• 英文别名: 6-(2,4-difluorophenoxy)pyridine-3-carboxylic acid
• CAS: 862088-72-0
• 化学式: C₁₂H₇F₂NO₃
• mdl: MFCD09737159
• 分子量: 251.189
• InChiKey: VVOBPLOEWWRDOQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  59.4
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• 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。
• NOVEL BENZOFURAN DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND USES OF THESE
  申请人：Nakamura Tetsuya

  公开号：US20090239860A1

  公开（公告）日：2009-09-24

  The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R 1 is hydrogen or lower alkyl; R 2 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, aryl, aralkyl, arylalkenyl, aryloxy-lower alkyl, heteroaryl, heteroaryl-lower alkyl, etc; R 3 , R 4 , R 5 and R 6 are each hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, lower alkoxy, hydroxy, aryl, etc; provided that at least one of R 3 , R 4 , R 5 and R 6 is other than hydrogen. Compound (I) of the present invention shows a potent adenosine A 2A receptor antagonistic activity, and are useful for treating or preventing a disease mediated by adenosine A 2A receptors such as motor function disorders, depression, anxiety disorders, cognitive function disorders, cerebral ischemia disorders, restless legs syndrome and the like.

  本发明提供了通式(I)所表示的化合物或其药物可接受的盐，其中R1是氢或低碳基；R2是低碳基，卤代低碳基，环烷基，杂环烷基，芳基，芳基烷基，芳基烯基，芳氧基-低碳基，杂芳基，杂芳基-低碳基等；R3、R4、R5和R6均为氢、卤素、氰基、低碳基、卤代低碳基、低碳氧基、羟基、芳基等；其中至少有一个R3、R4、R5和R6不是氢。本发明的化合物(I)表现出强大的腺苷A2A受体拮抗活性，并且可用于治疗或预防由腺苷A2A受体介导的疾病，例如运动功能障碍、抑郁症、焦虑症、认知功能障碍、脑缺血性疾病、不宁腿综合征等。
• US7951826B2
  申请人：——

  公开号：US7951826B2

  公开（公告）日：2011-05-31