5,7-dichloro-8-hydroxyquinoline-2-carboxylic acid [2-(1H-imidazol-4-yl)-ethyl]-amide

• 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: 5,7-dichloro-8-hydroxyquinoline-2-carboxylic acid [2-(1H-imidazol-4-yl)-ethyl]-amide
• 英文别名: PB-1038；5,7-dichloro-8-hydroxy-N-[2-(1H-imidazol-5-yl)ethyl]quinoline-2-carboxamide
• 化学式: C₁₅H₁₂Cl₂N₄O₂
• 分子量: 351.192
• InChiKey: NRMNXJVSVRPCJV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  90.9
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  5,7-Dichlor-8-hydroxy-chinolin-2-carbonsaeure 、 N,N'-二环己基碳二亚胺 、 1-羟基苯并三唑一水物 、 2-(1H-imidazol-3-ium-4-yl)ethanaminium dichloride 在 silica gel 、 Ethyl acetate 2-propanol water 、 5,7-dichloro-8-hydroxyquinoline-2-carboxylic acid [2-(1H-imidazol-4-yl)-ethyl]-amide 作用下， 以 三乙胺 为溶剂， 生成 5,7-dichloro-8-hydroxyquinoline-2-carboxylic acid [2-(1H-imidazol-4-yl)-ethyl]-amide
  参考文献：
  名称：

  8-Hydroxy quinoline derivatives

  摘要：

  本发明涉及一种用于治疗、改善和/或预防神经系统疾病的方法，特别是神经退行性疾病，该方法包括向需要治疗的受体中给予式（I）的化合物的有效量。本发明还涉及式（II）的化合物及其制备方法。

  公开号：

  US20060089380A1
• 作为试剂：
  描述：

  5,7-Dichlor-8-hydroxy-chinolin-2-carbonsaeure 、 N,N'-二环己基碳二亚胺 、 1-羟基苯并三唑一水物 、 2-(1H-imidazol-3-ium-4-yl)ethanaminium dichloride 在 silica gel 、 Ethyl acetate 2-propanol water 、 5,7-dichloro-8-hydroxyquinoline-2-carboxylic acid [2-(1H-imidazol-4-yl)-ethyl]-amide 作用下， 以 三乙胺 为溶剂， 生成 5,7-dichloro-8-hydroxyquinoline-2-carboxylic acid [2-(1H-imidazol-4-yl)-ethyl]-amide
  参考文献：
  名称：

  8-HYDROXY QUINOLINE DERIVATIVES

  摘要：

  本发明描述了一种治疗神经疾病的方法，包括向需要治疗的受试者注射一定疗效量的以下公式的化合物或其药学上可接受的盐、水合物或溶剂化物。

  公开号：

  US20150025108A1

文献信息

• [EN] 8-HYDROXY QUINOLINE DERIVATIVES<br/>[FR] DERIVES DE QUINOLINE 8-HYDROXY
  申请人：PRANA BIOTECHNOLOGY LTD

  公开号：WO2004007461A1

  公开（公告）日：2004-01-22

  The present invention relates to a method for the treatment, amelioration and/or prophylaxis of a neurological condition, in particular neurodegenerative disorders which comprises the administration of an effective amount of a compound of formula (I): to a subject in need thereof. The present invention also relates to a compound of formula (II) and processes for its preparation.

  本发明涉及一种用于治疗、改善和/或预防神经系统疾病，特别是神经退行性疾病的方法，包括向需要的受试者施用化合物(I)的有效量。本发明还涉及一种化合物(II)及其制备方法。
• 8-Hydroxy quinoline derivatives
  申请人：Barnham Jeffrey Kevin

  公开号：US20060089380A1

  公开（公告）日：2006-04-27

  The present invention relates to a method for the treatment, amelioration and/or prophylaxis of a neurological condition, in particular neurodegenerative disorders which comprises the administration of an effective amount of a compound of formula (I): to a subject in need thereof. The present invention also relates to a compound of formula (II) and processes for its preparation.

  本发明涉及一种用于治疗、改善和/或预防神经系统疾病的方法，特别是神经退行性疾病，该方法包括向需要治疗的受体中给予式（I）的化合物的有效量。本发明还涉及式（II）的化合物及其制备方法。
• Method of treating immunoglobulin light chain amyloidosis
  申请人：ALTERITY THERAPEUTICS LIMITED

  公开号：US11357770B2

  公开（公告）日：2022-06-14

  The present invention relates to the use of substituted quinoline compounds for treating immunoglobulin light chain (LC) amyloidosis (AL), especially cardiotoxicity associated with immunoglobulin LC AL. In particular, the substituted quinoline compounds useful in the treatment of cardiac LC amyloidosis are 5,7-dihalo-8-hydroxyquinoline derivatives, especially 5,7-dichloro-8-hydroxyquinoline derivatives.

  本发明涉及使用取代的喹啉化合物治疗免疫球蛋白轻链（LC）淀粉样变性（AL），特别是与免疫球蛋白LC AL相关的心脏毒性。特别是，用于治疗心脏LC淀粉样变性的取代喹啉化合物是5,7-二卤-8-羟基喹啉衍生物，尤其是5,7-二氯-8-羟基喹啉衍生物。
• METHOD OF TREATMENT AND AGENTS USEFUL FOR SAME
  申请人：Bush Ashley

  公开号：US20100069393A1

  公开（公告）日：2010-03-18

  The present invention relates generally to therapeutic agents, formulations comprising them and their use in the treatment, amelioration and/or prophylaxis of glioma brain tumours and related conditions. The therapeutic agent comprises two fused 6-membered rings with at least a nitrogen at position 1 and a hydroxyl at position 8.
• METHOD OF TREATMENT OF AGE-RELATED MACULAR DEGENERATION (AMD)
  申请人：Bush Ashley

  公开号：US20100144693A1

  公开（公告）日：2010-06-10

  The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions.