7-chloro-2,3-dihydro-10-hydroxypyridazino[4,5-b]quinoline-1,4-dione | 147493-44-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 7-chloro-2,3-dihydro-10-hydroxypyridazino[4,5-b]quinoline-1,4-dione
• 英文别名: Pyridazinediones-derivative-1；7-chloro-3,5-dihydro-2H-pyridazino[4,5-b]quinoline-1,4,10-trione
• CAS: 147493-44-5；219607-93-9
• 化学式: C₁₁H₆ClN₃O₃
• 分子量: 263.64
• InChiKey: QZWYCFYTWWTGQD-UHFFFAOYSA-N

物化性质

• 密度：
  1.657±0.06 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  18
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  87.3
• 氢给体数：
  3
• 氢受体数：
  4

制备方法与用途

生物活性

吡啶并咪唑衍生物-1适用于神经变性疾病的研宄。其ED50值为2.1 μM，能够抑制谷氨酸诱导的豚鼠回肠收缩。

反应信息

• 作为反应物：
  描述：

  7-chloro-2,3-dihydro-10-hydroxypyridazino[4,5-b]quinoline-1,4-dione 以 吡啶 、 甲醇 为溶剂， 生成 7-chloro-10-hydroxy-l-(3-phenylpropionyloxy)pyridazino[4,5-b]quinoline-4(3H)-one
  参考文献：
  名称：

  Pyridazinedione compounds useful in treating neurological disorders

  摘要：

  本发明涉及吡啶并[4,5-b]喹啉及其药用盐，它们是兴奋性氨基酸拮抗剂，在需要此类拮抗作用时非常有用，例如在治疗神经系统疾病时。该发明还提供含有吡啶并[4,5-b]喹啉作为活性成分的药物组合物，以及治疗神经系统疾病的方法。

  公开号：

  US05599814A1

文献信息

• Pyridazinedione compounds useful in the treating neurological disorders
  申请人：Imperial Chemical Industries PLC

  公开号：US05733910A1

  公开（公告）日：1998-03-31

  The present invention relates to pyridazino\x9b4,5-b!quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino\x9b4,5-b!quinolines as active ingredient, and methods for the treatment of neurological disorders.

  本发明涉及吡啶并[4,5-b]喹啉及其药用盐，其为兴奋性氨基酸拮抗剂，在需要这种拮抗作用时，如治疗神经系统疾病时，具有有用性。本发明还提供含有吡啶并[4,5-b]喹啉作为活性成分的制药组合物，以及治疗神经系统疾病的方法。
• Pyridazinediones and their use in the treatment of neurological disorders
  申请人：ZENECA LIMITED

  公开号：EP0516297A1

  公开（公告）日：1992-12-02

  The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.

  本发明涉及哒嗪并[4,5-b]喹啉、 及其药用盐，它们是兴奋性氨基酸拮抗剂，在治疗神经系统疾病等需要这种拮抗剂时非常有用。本发明进一步提供了含有哒嗪并[4,5-b]喹啉类活性成分的药物组合物，以及治疗神经系统疾病的方法。
• PYRIDAZINOQUINOLINE COMPOUNDS
  申请人：AstraZeneca AB

  公开号：EP0790996B1

  公开（公告）日：2002-03-27
• COMBINATIONS OF NMDAR MODULATING COMPOUNDS
  申请人：NORTHWESTERN UNIVERSITY

  公开号：US20170072005A1

  公开（公告）日：2017-03-16

  This disclosure features combinations of NMDAR modulating compounds. This disclosure features combinations that include one or more NMDAR antagonists and GLYX-13 (each of which is sometimes referred to herein as a ‘component”). The beneficial effects of the combination are based, in part, on the finding that administration of GLYX-13 (e.g., a single dose) can reverse and/or prevent NMDAR antagonist-induced cognitive impairment (e.g., NMDAR antagonist-induced impairment in novel object recognition; e.g., induced through repeated dosing of the NMDAR antagonist).
• US5599814A
  申请人：——

  公开号：US5599814A

  公开（公告）日：1997-02-04