(3R)-3-(3-methyl-1,2,4-oxadiazol-5-yl)piperidine | 1243306-94-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (3R)-3-(3-methyl-1,2,4-oxadiazol-5-yl)piperidine
• 英文别名: 3-methyI-5-(piperidin-3-yl)-1,2,4-oxadiazole；R-(-)-3-methyl-5-(piperidin-3-yl)-1,2,4-oxadiazole；3-methyl-5-[(3R)-piperidin-3-yl]-1,2,4-oxadiazole
• CAS: 1243306-94-6
• 化学式: C₈H₁₃N₃O
• 分子量: 167.211
• InChiKey: MPYNENJKQSNBDF-SSDOTTSWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  51
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (3R)-3-(3-methyl-1,2,4-oxadiazol-5-yl)piperidine 、 5’-methoxy-4H-spiro[cyclohexane-1,3'-indole]-2’,4(1’H)-dione 在 三乙胺 、 zinc(II) chloride 、 sodium cyanoborohydride 作用下， 以 甲醇 为溶剂， 反应 15.0h， 生成 5'-methoxy-4-[(3R)-3-(3-methyl-1,2,4-oxadiazol-5- yl)piperidin-1-yl]spiro[cyclohexane-1,3'-indol]-2'(1'H)-one
  参考文献：
  名称：

  PHARMACEUTICAL COMPOUNDS

  摘要：

  这项发明涉及激动毒蕈碱M1受体或M1和M4受体的化合物，这些化合物在治疗毒蕈碱M1或M1/M4受体介导的疾病中有用。还提供了含有这些化合物的药物组合物以及这些化合物的治疗用途。所提供的化合物的公式如下：其中Q4、Q5、R5、p、V、Q1、Q2、X1、X2和W在此处被定义。

  公开号：

  US20180105491A1
• 作为产物：
  描述：

  N-Boc-3-哌啶甲酸乙酯 在 盐酸 、 L-酒石酸 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲醇 、 乙腈 为溶剂， 反应 30.17h， 生成 (3R)-3-(3-methyl-1,2,4-oxadiazol-5-yl)piperidine
  参考文献：
  名称：

  PHARMACEUTICAL COMPOUNDS

  摘要：

  这项发明涉及激动毒蕈碱M1受体或M1和M4受体的化合物，这些化合物在治疗毒蕈碱M1或M1/M4受体介导的疾病中有用。还提供了含有这些化合物的药物组合物以及这些化合物的治疗用途。所提供的化合物的公式如下：其中Q4、Q5、R5、p、V、Q1、Q2、X1、X2和W在此处被定义。

  公开号：

  US20180105491A1

文献信息

• [EN] COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR AMÉLIORER LA FONCTION COGNITIVE, PROCÉDÉS DE FABRICATION ET MÉTHODES DE TRAITEMENT
  申请人：MITHRIDION INC

  公开号：WO2010102218A1

  公开（公告）日：2010-09-10

  Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.

  提供了用于刺激肌气受体并治疗认知障碍的肌气受体激动剂。还提供了合成这类激动剂的方法。还提供了用于增强人类等受试者认知功能的组合物，该组合物包括肌气受体激动剂或其药用适宜形式。还提供了通过给予这类组合物来治疗动物如人类的方法。
• [EN] COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR L'AMÉLIORATION DE LA COGNITION, LEURS PROCÉDÉS DE FABRICATION, ET MÉTHODES DE TRAITEMENT
  申请人：MITHRIDION INC

  公开号：WO2011085406A1

  公开（公告）日：2011-07-14

  Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.

  揭示了包括噻唑二唑衍生物在内的肌碱激动剂化合物，以及其组合物和制剂。还揭示了合成这种噻唑二唑化合物的方法。进一步揭示了使用这些肌碱激动剂或其药学适宜形式来增强认知功能的治疗方法。
• COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING
  申请人：Twose Trevor M.

  公开号：US20120046273A1

  公开（公告）日：2012-02-23

  Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.

  提供了用于刺激毒蕈碱受体和治疗认知障碍的毒蕈碱激动剂。还提供了合成这种激动剂的方法。还提供了用于增强人类等受试者认知功能的组合物，其中组合物包括毒蕈碱激动剂或其药学上适宜的形式。还提供了通过给予这样的组合物治疗人类等动物的方法。
• Cognition Enhancing Compounds and Compositions, Methods of Making, and Methods of Treating
  申请人：Mithridion, Inc.

  公开号：US20130274299A1

  公开（公告）日：2013-10-17

  The invention relates generally to muscarinic agonists, which are useful for stimulating muscarine receptors, and treating cognitive disorders. Included among the muscarinic agonists disclosed herein are oxadiazole derivatives, compositions, and preparations thereof. Methods of synthesizing oxadiazole compounds also are provided. This disclosure also relates in part to compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. This disclosure relates in part to methods of treating animals such as humans by administering such compositions.

  本发明涉及肌肉碱受体激动剂，其可用于刺激肌肉碱受体和治疗认知障碍。本文所披露的肌肉碱受体激动剂包括噁唑烷衍生物、组合物及其制备。还提供了合成噁唑烷化合物的方法。本公开还涉及用于增强人类等受试者认知功能的组合物，该组合物包括肌肉碱受体激动剂或其药学适宜形式。本公开还涉及通过给予该类组合物治疗动物，如人类的方法。
• Compounds and Compositions for Cognition-Enhancement, Methods of Making, and Methods of Treating
  申请人：NeuroSolis, Inc.

  公开号：US20150099765A1

  公开（公告）日：2015-04-09

  Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.

  本发明涉及包括噁唑烷衍生物在内的毒蕈碱受体激动剂化合物，以及其组合物和制备方法。本发明还涉及合成这种噁唑烷化合物的方法。本发明还涉及使用所述毒蕈碱受体激动剂或其药学适宜形式来增强认知功能的方法。