3-(2-氨基-4-氯苯基)-4H-[1,2,4]噁二唑-5-酮 | 697278-41-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 3-(2-氨基-4-氯苯基)-4H-[1,2,4]噁二唑-5-酮
• 英文名称: 3-(2-amino-4-chlorophenyl)-4H-[1,2,4]oxadiazol-5-one
• 英文别名: 3-(2-Amino-4-chlorophenyl)-1,2,4-oxadiazol-5(2H)-one；3-(2-amino-4-chlorophenyl)-4H-1,2,4-oxadiazol-5-one
• CAS: 697278-41-4
• 化学式: C₈H₆ClN₃O₂
• 分子量: 211.608
• InChiKey: IGAVHJWKCUOTBA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  76.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  丙磺舒 、 3-(2-氨基-4-氯苯基)-4H-[1,2,4]噁二唑-5-酮 在 4-二甲氨基吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 以53%的产率得到N-[5-chloro-2-(5-oxo-2,5-dihydro-[1,2,4]oxadiazol-3-yl)-phenyl]-4-dipropylsulfamoyl-benzamide
  参考文献：
  名称：

  [EN] NOVEL BENZAMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS
  [FR] NOUVEAUX DÉRIVÉS DE BENZAMIDE UTILES EN TANT QUE MODULATEURS DES CANAUX POTASSIQUES

  摘要：

  这项发明涉及新型苯甲酰胺衍生物，发现它们是钾通道的有效调节剂，因此是治疗对钾通道调节敏感的疾病或疾病的有价值候选药物。

  公开号：

  WO2009068509A1
• 作为产物：
  描述：

  2-氨基-4-氯苯腈 在 盐酸羟胺 、 水 、 sodium ethanolate 、 potassium hydrogencarbonate 作用下， 以 乙醇 为溶剂， 反应 26.0h， 生成 3-(2-氨基-4-氯苯基)-4H-[1,2,4]噁二唑-5-酮
  参考文献：
  名称：

  [EN] ARYL UREIDO DERIVATIVES AND THEIR MEDICAL USE
  [FR] NOUVEAUX DERIVES D'ACIDE ARYL UREIDO BENZOIQUE ET LEUR UTILISATION

  摘要：

  公开号：

  WO2004046090A3

文献信息

• [EN] NOVEL PHENYL-ACETAMIDE AND PHENYL-PROPIONAMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS<br/>[FR] NOUVEAUX DERIVES DE PHENYL-ACETAMIDE ET DE PHENYL-PROPIONAMIDE UTILES EN TANT QUE MODULATEURS DES CANAUX POTASSIQUES
  申请人：NEUROSEARCH AS

  公开号：WO2009068557A1

  公开（公告）日：2009-06-04

  This invention relates to novel phenyl-acetamide and phenyl- propionamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.

  这项发明涉及新型苯乙酰胺和苯丙酰胺衍生物，发现它们是钾通道的有效调节剂，因此是治疗各种对钾通道调节敏感的疾病或紊乱的有价值候选药物。
• Novel aryl ureido benzoic acid derivatives and their use
  申请人：Valgeirsson Jon

  公开号：US20060069255A1

  公开（公告）日：2006-03-30

  This invention relates to novel aryl ureido benzoic acid derivatives useful as selective and non-competitive antagonists of the ionotropic GluR5 receptor. Due to their biological activity, the aryl ureido derivatives of the invention are considered useful for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.

  本发明涉及新型芳基脲基苯甲酸衍生物，可用作离子型GluR5受体的选择性和非竞争性拮抗剂。由于它们的生物活性，本发明的芳基脲基衍生物被认为对于治疗对天冬氨酸或谷氨酸受体调节敏感的疾病有用。此外，本发明提供了用于本发明的化学化合物，以及包含该化学化合物的药物组合物和治疗对天冬氨酸或谷氨酸受体调节敏感的疾病、障碍或状况的方法。
• Aryl ureido benzoic acid derivatives and their use
  申请人：Neurosearch

  公开号：US07521480B2

  公开（公告）日：2009-04-21

  This invention relates to novel aryl ureido benzoic acid derivatives useful as selective and non-competitive antagonists of the ionotropic GluR5 receptor. Due to their biological activity, the aryl ureido derivatives of the invention are considered useful for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.

  本发明涉及一种新型芳基脲基苯甲酸衍生物，可用作离子型GluR5受体的选择性和非竞争性拮抗剂。由于它们的生物活性，本发明的芳基脲基衍生物被认为对于治疗对天冬氨酸或谷氨酸受体调节敏感的疾病有用。此外，本发明还提供了用于本发明的化学化合物，以及包含该化学化合物的制药组合物和治疗对天冬氨酸或谷氨酸受体调节敏感的疾病、疾病或疾病的方法。
• NOVEL CINNAMIC AMIDE DERIVATIVES USEFUL AS ION CHANNEL MODULATORS
  申请人：Nardi Antonio

  公开号：US20100087496A1

  公开（公告）日：2010-04-08

  This invention relates to novel cinnamic amide derivatives that are found to be potent modulators of ion channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of ion channels.

  本发明涉及新型肉桂酰胺衍生物，发现它们是离子通道的强效调节剂，因此它们是治疗各种对离子通道调节有响应的疾病或疾病的有价值候选药物。
• NOVEL AROMATIC HETEROCYCLIC CARBOXYLIC ACID AMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS
  申请人：Nardi Antonio

  公开号：US20100137312A1

  公开（公告）日：2010-06-03

  This invention relates to novel aromatic heterocyclic carboxylic acid amide derivatives of formula (I) that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.

  本发明涉及一种新型芳香族杂环羧酸酰胺衍生物，其化学式为(I)，发现它们是有效的钾通道调节剂，因此是治疗各种对钾通道调节敏感的疾病或疾病的有价值的候选药物。