3-[2-(6-methoxypyridin)yl]-1-azabicyclo[2.2.1]heptane | 1238122-33-2

• 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: 3-[2-(6-methoxypyridin)yl]-1-azabicyclo[2.2.1]heptane
• 英文别名: 3-(6-Methoxypyridin-2-yl)-1-azabicyclo[2.2.1]heptane
• CAS: 1238122-33-2
• 化学式: C₁₂H₁₆N₂O
• 分子量: 204.272
• InChiKey: ZXZKCQRWYSXNGD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  25.4
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Substituted pyridine derivatives for use in the treatment of glaucoma
  申请人：MERCK SHARP & DOHME LTD.

  公开号：EP0492902A1

  公开（公告）日：1992-07-01

  The use of a compound of structural formula (I): or a pharmaceutically acceptable salt thereof or a prodrug thereof; wherein    R¹ represents a non-aromatic azabicyclic ring system having more than 5 ring atoms selected from: wherein the broken line represents an optional chemical bond;    the substituents R³ and R⁴ may be present at any position, including the point of attachment to the pyridine ring, and independently represent hydrogen, C₁₋₄ alkyl, halo, C₁₋₄ alkoxy, hydroxy, carboxy or C₁₋₄ alkoxycarbonyl; or R³ and R⁴ together represent carbonyl; and    R⁵represents hydrogen or C₁₋₄ alkyl;    provided that R¹ is attached to the pyridine ring other than at the 2′-carbon position of R¹; and    R² and R¹¹ independently represent hydrogen, halo, -CF₃, -OR⁶, -NR⁶R⁷, -CN, -COR⁸, C₁₋₈ alkyl or C₂₋₈ alkenyl; wherein R⁶ is hydrogen or C₁₋₆ alkyl; R⁷ is hydrogen or C₁₋₆ alkyl; and R⁸ represents -OR⁶ or -NR⁶R⁷; other than 3-hydroxy-3-(2-pyridinyl)-1-azabicyclo[2.2.2]-octane and 3-(2-pyridinyl)-1-azabicyclo[2.2.2]oct-2-ene; for the manufacture of a medicament for treating glaucoma and/or for reducing intraocular pressure.

  使用结构式(I)的化合物，其药学上可接受的盐或前药；其中R¹代表非芳香性的含有5个以上环原子的氮杂双环系统，选自：其中断裂的线表示可选的化学键；取代基R³和R⁴可以出现在任何位置，包括连接到吡啶环的位置，并且独立地表示氢、C₁₋₄烷基、卤素、C₁₋₄烷氧基、羟基、羧基或C₁₋₄烷氧羰基；或R³和R⁴一起表示羰基；而R⁵表示氢或C₁₋₄烷基；前提是R¹连接到吡啶环而不是R¹的2'-碳位置；而R²和R¹¹独立地表示氢、卤素、-CF₃、-OR⁶、-NR⁶R⁷、-CN、-COR⁸、C₁₋₈烷基或C₂₋₈烯基；其中R⁶表示氢或C₁₋₆烷基；R⁷表示氢或C₁₋₆烷基；而R⁸表示-OR⁶或-NR⁶R⁷；除了3-羟基-3-(2-吡啶基)-1-氮杂双环[2.2.2]辛烷和3-(2-吡啶基)-1-氮杂双环[2.2.2]辛-2-烯之外；用于制造治疗青光眼和/或降低眼内压的药物。
• Substituted pyridines, their preparation, formulations and use in dementia
  申请人：MERCK SHARP & DOHME LTD.

  公开号：EP0412798A2

  公开（公告）日：1991-02-13

  Pyridines, substituted by a non-aromatic azacyclic or non-fused azabicyclic ring system and a substituent of low lipophilicity or a hydrocarbon substituent, their salts and prodrugs, and formulations thereof are useful in the treatment of neurodegenerative disorders such as dementia. The compounds can be synthesised by methods analogous to these known in the art.

  由非芳香氮杂环或非融合氮杂环环系和低亲脂性取代基或烃类取代基取代的吡啶类化合物、其盐类和原药及其制剂可用于治疗神经退行性疾病，如痴呆症。这些化合物的合成方法类似于本领域已知的方法。
• US5346906A
  申请人：——

  公开号：US5346906A

  公开（公告）日：1994-09-13