4-(吡啶-2-基)哌啶-4-醇双盐酸盐 | 172734-32-6

• 物质功能分类: 医药中间体
• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 4-(吡啶-2-基)哌啶-4-醇双盐酸盐
• 英文名称: 4-(Pyridin-2-yl)piperidin-4-ol dihydrochloride
• 英文别名: 4-pyridin-2-ylpiperidin-4-ol;dihydrochloride
• CAS: 172734-32-6
• 化学式: C10H16Cl2N2O
• 分子量: 251.15
• InChiKey: BSSYDYGKBQCYJL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  45.2
• 氢给体数：
  4
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  4-(6-fluoropyridin-3-yl)-6,7-dimethoxycinnoline 、 4-(吡啶-2-基)哌啶-4-醇双盐酸盐 、 potassium carbonate 在 乙酸乙酯 、 水 、 氯化钠 、 magnesium sulfate 、 silica gel 、 甲醇 、 二氯甲烷 作用下， 以 二甲基亚砜 、 水 为溶剂， 反应 16.0h， 以to provide 1-(5-(6,7-dimethoxycinnolin-4-yl)pyridin-2-yl)-4-(pyridin-2-yl)piperidin-4-ol (0.1393 g, 55% yield, M+1=444.2)的产率得到1-(5-(6,7-dimethoxycinnolin-4-yl)pyridin-2-yl)-4-(pyridin-2-yl)piperidin-4-ol
  参考文献：
  名称：

  PHOSPHODIESTERASE 10 INHIBITORS

  摘要：

  本发明涉及一些有用的化合物，可作为磷酸二酯酶10（PDE10）抑制剂，其化学式为R1、R2、R3、R4、X、Y和Z，其中定义如下，以及含有这种化合物的制药组合物和制备这种化合物的方法。本发明还涉及治疗由PDE10介导的疾病的方法，例如肥胖症、非胰岛素依赖性糖尿病、精神分裂症、双相情感障碍、强迫症等。

  公开号：

  US20090062277A1

文献信息

• [EN] AMINOBENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS<br/>[FR] MODULATEURS ALLOSTÉRIQUES POSITIFS DU RÉCEPTEUR M1 À BASE D'AMINOBENZOQUINAZOLINONE
  申请人：MERCK SHARP & DOHME

  公开号：WO2011084371A1

  公开（公告）日：2011-07-14

  The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及式(I)的氨基苯并喹唑醌酮化合物，其为M1受体阳性变构调节剂，并且在治疗M1受体参与的疾病，如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍等方面有用。该发明还涉及包含这些化合物的药物组合物，以及在治疗M1受体介导的疾病中使用这些化合物和组合物。
• [EN] N-LINKED LACTAM M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS<br/>[FR] MODULATEURS ALLOSTÉRIQUES POSITIFS DU RÉCEPTEUR M1 CONTENANT DES LACTAMES LIÉS À N
  申请人：MERCK SHARP & DOHME

  公开号：WO2012158475A1

  公开（公告）日：2012-11-22

  The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及一般式（I）的N-连接内酰胺化合物，这些化合物是M1受体阳性变构调节剂，可用于治疗涉及M1受体的疾病，如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍。该发明还涉及包括这些化合物的药物组合物，以及在治疗由M1受体介导的疾病中使用这些化合物和组合物。
• Aminobenzoquinazolinone M1 Receptor Positive Allosteric Modulators
  申请人：Kuduk Scott D.

  公开号：US20120264761A1

  公开（公告）日：2012-10-18

  The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及式(I)的氨基苯并喹唑酮化合物，它们是M1受体正向变构调节剂，可用于治疗M1受体参与的疾病，如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍。本发明还涉及包含该化合物的制药组合物，以及在治疗M1受体介导的疾病中使用该化合物和组合物的方法。
• Aminobenzoquinazolinone M1 receptor positive allosteric modulators
  申请人：Kuduk Scott D.

  公开号：US08383638B2

  公开（公告）日：2013-02-26

  The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及公式（I）的氨基苯并喹唑酮化合物，其为M1受体正向变构调节剂，并且在治疗M1受体参与的疾病，如阿尔茨海默症、精神分裂症、疼痛或睡眠障碍方面有用。该发明还涉及包含这些化合物的制药组合物，以及使用这些化合物和组合物治疗由M1受体介导的疾病。
• N-LINKED LACTAM M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
  申请人：Kuduk Scott D.

  公开号：US20150065498A1

  公开（公告）日：2015-03-05

  The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及一般式（I）的N-连接内酰胺化合物，它们是M1受体正向变构调节剂，可用于治疗M1受体参与的疾病，例如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍。本发明还涉及包含这些化合物的药物组合物，以及在治疗M1受体介导的疾病中使用这些化合物和组合物的方法。