6-(2-fluoro-4-methoxyphenyl)pyridazin-3(2H)-one | 1219566-14-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-(2-fluoro-4-methoxyphenyl)pyridazin-3(2H)-one
• 英文别名: 3-(2-fluoro-4-methoxyphenyl)-1H-pyridazin-6-one
• CAS: 1219566-14-9
• 化学式: C₁₁H₉FN₂O₂
• mdl: MFCD16090095
• 分子量: 220.203
• InChiKey: UYMYEULBVQXUQF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  50.7
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 危险等级：
  IRRITANT

反应信息

• 作为反应物：
  描述：

  6-(2-fluoro-4-methoxyphenyl)pyridazin-3(2H)-one 在 三溴化硼 、 potassium carbonate 作用下， 以 二氯甲烷 、 丙酮 为溶剂， 生成
  参考文献：
  名称：

  Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity

  摘要：

  H3R structure-activity relationships on a novel class of pyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules with excellent target potency, selectivity and pharmacokinetic properties. Compounds 13 and 21 displayed potent functional H3R antagonism in vivo in the rat dipsogenia model and demonstrated robust wake activity in the rat EEG/EMG model. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.06.108
• 作为产物：
  描述：

  6-(2-Fluoro-4methoxyphenyl)-4,5-dihydro-3(2h)-pyridazinone 生成 6-(2-fluoro-4-methoxyphenyl)pyridazin-3(2H)-one
  参考文献：
  名称：

  Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity

  摘要：

  H3R structure-activity relationships on a novel class of pyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules with excellent target potency, selectivity and pharmacokinetic properties. Compounds 13 and 21 displayed potent functional H3R antagonism in vivo in the rat dipsogenia model and demonstrated robust wake activity in the rat EEG/EMG model. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.06.108

文献信息

• [EN] SUBSTITUTED PYRIDAZINONE FOR USE IN THE TREATMENT OF NEUROMUSCULAR DISEASES<br/>[FR] PYRIDAZINONE SUBSTITUÉE DESTINÉE À ÊTRE UTILISÉE DANS LE TRAITEMENT D'INFECTIONS NEUROMUSCULAIRE
  申请人：EDGEWISE THERAPEUTICS INC

  公开号：WO2021231630A1

  公开（公告）日：2021-11-18

  Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-α.

  本文披露了用于治疗神经肌肉疾病，如杜欣氏肌肉萎缩症（DMD）的吡啶并嗪酮化合物、结合物和药物组合物。所披露的化合物在治疗DMD和调节炎症抑制剂IL-1、IL-6或TNF-α等方面具有用处。
• Pyridazinone compounds and uses thereof
  申请人：Edgewise Therapeutics, Inc.

  公开号：US11390606B2

  公开（公告）日：2022-07-19

  Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-α.

  本文公开了用于治疗神经肌肉疾病（如杜氏肌肉萎缩症（DMD））的取代哒嗪酮化合物、共轭物和药物组合物。所公开的化合物除其他外，可用于治疗 DMD 和调节炎症抑制剂 IL-1、IL-6 或 TNF-α。
• WO2020097258A5
  申请人：——

  公开号：WO2020097258A5

  公开（公告）日：2022-11-14
• PYRIDAZINONE COMPOUNDS AND USES THEREOF
  申请人：EDGEWISE THERAPEUTICS, INC.

  公开号：EP3877367A1

  公开（公告）日：2021-09-15