2-(2-fluoropyridin-4-yl)-7-methoxy-4-methyl-4H-pyrazolo[1,5-a]quinazolin-5-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 2-(2-fluoropyridin-4-yl)-7-methoxy-4-methyl-4H-pyrazolo[1,5-a]quinazolin-5-one
• 英文别名: 2-(2-Fluoropyridin-4-yl)-7-methoxy-4-methylpyrazolo[1,5-a]quinazolin-5-one；2-(2-fluoropyridin-4-yl)-7-methoxy-4-methylpyrazolo[1,5-a]quinazolin-5-one
• 化学式: C₁₇H₁₃FN₄O₂
• 分子量: 324.314
• InChiKey: KMDUYAHVKHNBJR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  60.2
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2,2,2-三氟乙醇 、 2-(2-fluoropyridin-4-yl)-7-methoxy-4-methyl-4H-pyrazolo[1,5-a]quinazolin-5-one 在 sodium hydride 作用下， 以 N,N-二甲基乙酰胺 为溶剂， 反应 1.0h， 以60%的产率得到7-methoxy-4-methyl-2-[2-(2,2,2-trifluoroethoxy)-pyridin-4-yl]-4H-pyrazolo[1,5-a]quinazolin-5-one
  参考文献：
  名称：

  [EN] SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP IIMETABOTROPIC GLUTAMATE RECEPTORS
  [FR] PYRAZOLOQUINAZOLINONES ET PYRROLOQUINAZOLINONES SUBSTITUÉES EN TANT QUE MODULATEURS ALLOSTÉRIQUES DES RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE DU GROUPE II

  摘要：

  本发明提供了通式(I)的吡唑并喹唑啉酮和吡咯并喹唑啉酮衍生物以及含有它们的药物组合物。此外，式(I)的化合物及其组合物被提供用于治疗和/或预防与谷氨酸能信号传导和/或功能改变相关的病症，以及可以通过改变哺乳动物中的谷氨酸水平或信号传导而受影响的病症。这些通式(I)的吡唑并喹唑啉酮和吡咯并喹唑啉酮衍生物可以作为神经系统中对谷氨酸敏感的受体调节剂，特别是作为代谢型谷氨酸受体(mGluRs)的调节剂，这使得它们特别适合用于治疗和/或预防急性和慢性神经和/或精神疾病。

  公开号：

  WO2016046404A1

文献信息

• Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
  申请人：Domain Therapeutics

  公开号：EP3000814A1

  公开（公告）日：2016-03-30

  The present invention provides pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I) and pharmaceutical compositions containing them. Moreover, the compounds of formula (I) and the compositions containing them are provided for use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. These pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I) can act as modulators of nervous system receptors sensitive to glutamate, in particular as modulators of metabotropic glutamate receptors (mGluRs), which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.

  本发明提供通式（I）的吡唑喹唑啉酮和吡咯喹唑啉酮衍生物以及含有它们的药物组合物。此外，本发明提供的式(I)化合物和含有它们的组合物可用于治疗和/或预防与谷氨酸能信号传导和/或功能改变有关的疾病，和/或可受哺乳动物体内谷氨酸水平或信号传导改变影响的疾病。这些通式（I）的吡唑并喹唑啉酮和吡咯并喹唑啉酮衍生物可作为对谷氨酸敏感的神经系统受体的调节剂，特别是作为代谢型谷氨酸受体（mGluRs）的调节剂，这使它们特别适用于治疗和/或预防急性和慢性神经和/或精神疾病。
• SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP IIMETABOTROPIC GLUTAMATE RECEPTORS
  申请人：Domain Therapeutics

  公开号：EP3197897A1

  公开（公告）日：2017-08-02
• SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP II METABOTROPIC GLUTAMATE RECEPTORS
  申请人：DOMAIN THERAPEUTICS

  公开号：US20170305913A1

  公开（公告）日：2017-10-26

  The present invention provides pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I) and pharmaceutical compositions containing them. Moreover, the compounds of formula (I) and the compositions containing them are provided for use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. These pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I) can act as modulators of nervous system receptors sensitive to glutamate, in particular as modulators of metabotropic glutamate receptors (mGluRs), which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.
• [EN] SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP IIMETABOTROPIC GLUTAMATE RECEPTORS<br/>[FR] PYRAZOLOQUINAZOLINONES ET PYRROLOQUINAZOLINONES SUBSTITUÉES EN TANT QUE MODULATEURS ALLOSTÉRIQUES DES RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE DU GROUPE II
  申请人：DOMAIN THERAPEUTICS

  公开号：WO2016046404A1

  公开（公告）日：2016-03-31

  The present invention provides pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I) and pharmaceutical compositions containing them. Moreover, the compounds of formula (I) and the compositions containing them are provided for use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. These pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I) can act as modulators of nervous system receptors sensitive to glutamate, in particular as modulators of metabotropic glutamate receptors (mGlu Rs), which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.

  本发明提供了通式(I)的吡唑并喹唑啉酮和吡咯并喹唑啉酮衍生物以及含有它们的药物组合物。此外，式(I)的化合物及其组合物被提供用于治疗和/或预防与谷氨酸能信号传导和/或功能改变相关的病症，以及可以通过改变哺乳动物中的谷氨酸水平或信号传导而受影响的病症。这些通式(I)的吡唑并喹唑啉酮和吡咯并喹唑啉酮衍生物可以作为神经系统中对谷氨酸敏感的受体调节剂，特别是作为代谢型谷氨酸受体(mGluRs)的调节剂，这使得它们特别适合用于治疗和/或预防急性和慢性神经和/或精神疾病。