1H-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: 1H-quinazolin-5-one
• 化学式: C₈H₆N₂O
• mdl: MFCD19226338
• 分子量: 146.15
• InChiKey: FHBBETAOBPMWTJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  41.5
• 氢给体数：
  1
• 氢受体数：
  2

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：EP2666775A1

  公开（公告）日：2013-11-27

  The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their 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, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.

  本发明涉及通式（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，以及它们在治疗和/或预防与改变谷氨酸能信号和/或功能相关的疾病以及可以受到哺乳动物谷氨酸水平或信号改变影响的疾病中的用途，特别是在治疗和/或预防急性和慢性神经和/或精神障碍中的用途。
• [EN] SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP II METABOTROPIC GLUTAMATE RECEPTORS<br/>[FR] PYRAZOLOQUINAZOLINONES ET PYRROLOQUINAZOLINONES SUBSTITUÉES COMME MODULATEURS ALLOSTÉRIQUES DES RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE DE GROUPE II
  申请人：DOMAIN THERAPEUTICS

  公开号：WO2013174822A1

  公开（公告）日：2013-11-28

  The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their 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, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.

  本发明涉及一般式（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，以及它们在治疗和/或预防与改变谷氨酸能信号和/或功能相关的疾病以及/或在哺乳动物中可以受到谷氨酸水平或信号改变影响的疾病，特别是在治疗和/或预防急性和慢性神经和/或精神障碍中的应用。
• [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。
• SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP II METABOTROPIC GLUTAMATE RECEPTORS
  申请人：Domain Therapeutics

  公开号：US20150105381A1

  公开（公告）日：2015-04-16

  The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their 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, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.

  本发明涉及一般式(I)的吡唑喹唑酮和吡咯喹唑酮衍生物，以及包含它们的制药组合物，以及它们在治疗和/或预防与改变谷氨酸能信号和/或功能相关的疾病和/或在哺乳动物中可以受到谷氨酸水平或信号改变影响的疾病中的应用，特别是在治疗和/或预防急性和慢性神经和/或精神障碍方面的应用。
• TETRAHYDROQUINAZOLINE COMPOUNDS AND THEIR USE IN PREPARING MEDICAMENTS FOR TREATING AND PREVENTING VIROSIS
  申请人：Beijing Molecule Science and Technology Co., Ltd.

  公开号：EP2119708B1

  公开（公告）日：2013-08-14