4-(5-Methyl-oxazolo[4,5-b]pyridin-2-yl)-1,4-diaza-bicyclo[3.2.2]nonane | 439608-12-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶唑并吡啶类
• 英文名称: 4-(5-Methyl-oxazolo[4,5-b]pyridin-2-yl)-1,4-diaza-bicyclo[3.2.2]nonane
• 英文别名: CP-810123；4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane；2-(1,4-diazabicyclo[3.2.2]non-4-yl)-5-methyloxazolo[4,5-b]pyridine；CP-810,123；4-(5-methyl-oxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane；1,4-Diazabicyclo(3.2.2)nonane, 4-(5-methyloxazolo(4,5-b)pyridin-2-yl)-；2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-methyl-[1,3]oxazolo[4,5-b]pyridine
• CAS: 439608-12-5
• 化学式: C₁₄H₁₈N₄O
• 分子量: 258.323
• InChiKey: BSNKYWSMUAGMDO-UHFFFAOYSA-N

物化性质

• 沸点：
  392.9±52.0 °C(Predicted)
• 密度：
  1.29±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  45.4
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-(5-Methyl-oxazolo[4,5-b]pyridin-2-yl)-1,4-diaza-bicyclo[3.2.2]nonane 在 盐酸 作用下， 以 乙酸乙酯 为溶剂， 反应 0.5h， 以80%的产率得到CP-810123 hydrochloride
  参考文献：
  名称：

  ANTIPRURITIC AGENT

  摘要：

  一种抗瘙痒药物，基于新颖的作用机制发挥抗瘙痒作用，并对瘙痒有效。该抗瘙痒药物含有一种有效成分，该成分可以激活中枢型尼古丁乙酰胆碱受体。

  公开号：

  US20140128606A1
• 作为产物：
  描述：

  5-甲基-3H-恶唑并[4,5-B]吡啶-2-硫酮 在 potassium carbonate 作用下， 生成 4-(5-Methyl-oxazolo[4,5-b]pyridin-2-yl)-1,4-diaza-bicyclo[3.2.2]nonane
  参考文献：
  名称：

  Pharmaceutical compositions for CNS and other disorders

  摘要：

  公开号：

  EP1219622B1

文献信息

• Pharmaceutical composition for the treatment of CNS and other disorders
  申请人：——

  公开号：US20020086871A1

  公开（公告）日：2002-07-04

  The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant &agr;7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant &agr;7 nicotinic receptor agonist.

  本发明涉及一种治疗哺乳动物中枢神经系统（CNS）和其他疾病的方法，包括人类，在哺乳动物中给予一种穿透中枢神经系统的α7烟碱受体激动剂。同时涉及含有药用可接受载体和穿透中枢神经系统的α7烟碱受体激动剂的药物组合物。
• Benzoate salt of 4-(5-methyl-oxazolo[4,5-b]-pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane
  申请人：Duplantier Allen J.

  公开号：US20080045512A1

  公开（公告）日：2008-02-21

  The present invention provides a benzoate salt of Formula I: Formula I is also known as 4-(5-methyloxazolo[4,5-b]pyridine-2-yl)-1,4-diazabicyclo[3.2.2]nonane. The benzoate salt of the invention is useful in the treatment of schizophrenia and Alzheimer's Disease. It is particularly of use in the treatment of cognitive deficits associated with schizophrenia, cognitive and attention deficit symptoms of Alzheimer's Disease, and neurodegeneration associated with Alzheimer's Disease.

  本发明提供了一种公式I的苯甲酸盐： 公式I也被称为4-(5-甲氧噁唑[4,5-b]吡啶-2-基)-1,4-二氮杂双环[3.2.2]壬烷。该发明的苯甲酸盐在治疗精神分裂症和阿尔茨海默病方面非常有用。它特别适用于治疗与精神分裂症相关的认知缺陷，阿尔茨海默病的认知和注意力缺陷症状，以及与阿尔茨海默病相关的神经退行性。
• Azabenzoxazoles for the treatment of CNS disorders
  申请人：Rogers N. Bruce

  公开号：US20060166974A1

  公开（公告）日：2006-07-27

  The present invention relates to α7 nicotinic receptor agonists of formula I as described herein and to a method for treating disorders of the Central Nervous System (CNS) such as cognitive deficits in schizophrenia, by administering to a mammal an α7 nicotinic receptor agonist of formula I as shown herein.

  本发明涉及如下式所述的α7烟碱受体激动剂，以及通过向哺乳动物施用本文所示的α7烟碱受体激动剂来治疗中枢神经系统（CNS）疾病，如精神分裂症中的认知缺陷的方法。
• PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF CNS AND OTHER DISORDERS
  申请人：O'Neill Thomas Brian

  公开号：US20070099904A1

  公开（公告）日：2007-05-03

  The present invention relates to compounds of formula I The substituent designations are as disclosed. At least one of B Q, D and E is nitrogen. The present invention also provides a method of treating disorders of the Central Nervous System such as schizophrenia and cognitive dysfunction.

  本发明涉及I式化合物。取代基的标识如所披露的那样。B、Q、D和E中至少有一个是氮。本发明还提供了一种治疗中枢神经系统疾病，如精神分裂症和认知功能障碍的方法。
• Biomarkers predictive of responsiveness to alpha 7 nicotinic acetylcholine receptor activator treatment
  申请人：Novartis AG

  公开号：US11359241B2

  公开（公告）日：2022-06-14

  The invention provides methods for predicting therapeutic responsiveness of a subject suffering from cognitive impairments or dysfunctions, psychotic and/or neurodegenerative disorders to an alpha 7 nicotinic acetylcholine receptor activator treatment.

  本发明提供了预测患有认知障碍或功能障碍、精神病和/或神经退行性疾病的受试者对α7烟碱乙酰胆碱受体激活剂治疗反应性的方法。