5-(4-fluorobenzyl)aminosalicylic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-(4-fluorobenzyl)aminosalicylic acid
• 英文别名: 5-[(4-fluorophenyl)methylamino]-2-hydroxybenzoic acid
• 化学式: C₁₄H₁₂FNO₃
• 分子量: 261.253
• InChiKey: YWRQYUUZJRYBKN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  69.6
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  5-氨基水杨酸 、 4-氟溴苄 以480 mg (44% yield) of 5-(4-fluorobenzyl)aminosalicylic acid was obtained as a white solid的产率得到5-(4-fluorobenzyl)aminosalicylic acid
  参考文献：
  名称：

  Compounds, compositions and methods for preventing neurodegeneration in acute and chronic injuries in the central nervous system

  摘要：

  本发明提供了预防和预防伴随有神经元死亡的神经系统疾病的组合物和方法。该发明包括合成5-苯甲基氨基水杨酸（BAS）及其衍生物。BAS及其衍生物可保护皮层神经元免受N-甲基-D-天门冬氨酸、Zn2+和活性氧物种的毒性损害。因此，本发明提供了用于治疗中风、创伤性脑和脊髓损伤、癫痫和神经退行性疾病的组合物和方法，这些疾病伴随着兴奋毒性、Zn2+神经毒性和自由基神经毒性引起的严重神经元损失。

  公开号：

  US20030097018A1

文献信息

• Compounds and compositions for treating neuronal death or neurological dysfunction
  申请人：Gwag Joo Byoung

  公开号：US20070298129A1

  公开（公告）日：2007-12-27

  The present invention relates to 2-hydroxy-alkylamino-benzoic acid derivatives and to a combination of cell necrosis inhibitor and lithium, process for the preparation of the derivatives or the combination, pharmaceutical formulation containing the derivatives or the combination, and use of the derivatives or the combination by either concomitant or sequential administration for improvement of treatment of neuronal death or neurological dysfunction. The derivatives and the combination of the present invention are useful for treating neurological diseases, such as amyotrophic lateral sclerosis (ALS, Lou Gehrig's disease), spinal muscular atrophy, Alzheimer's disease, Parkinson's disease, Huntington's disease, stroke, traumatic brain injury or spinal cord injury; and for treating ocular diseases such as glaucoma, diabetic retinopathy or macular degeneration.

  本发明涉及2-羟基-烷基氨基苯甲酸衍生物及细胞坏死抑制剂和锂的组合物，以及制备该衍生物或组合物的过程，含有该衍生物或组合物的制药配方，以及通过同时或顺序给药使用该衍生物或组合物以改善神经元死亡或神经功能障碍的治疗。本发明的衍生物和组合物对于治疗神经系统疾病，如肌萎缩侧索硬化症（ALS，路易·格里格病）、脊髓性肌萎缩症、阿尔茨海默病、帕金森病、亨廷顿病、中风、创伤性脑损伤或脊髓损伤；以及治疗眼科疾病，如青光眼、糖尿病性视网膜病变或黄斑变性有用。
• Method for reducing neuronal death in nervous system injuries resulting from amyotrophic lateral sclerosis
  申请人：Neurotech Pharmaceuticals Co., Ltd.

  公开号：US08211878B2

  公开（公告）日：2012-07-03

  The present invention provides methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death in a patient. The invention includes use of 5-benzylamino salicylic acid (BAS) and its derivatives. Thus, the present invention provides methods for reducing neuronal death in nervous system injuries resulting from amyotrophic lateral sclerosis.

  本发明提供了一种针对患者神经元死亡伴随的神经系统疾病进行预防和预防的方法。该发明包括使用5-苄氨基水杨酸（BAS）及其衍生物。因此，本发明提供了一种减少由肌萎缩性侧索硬化症引起的神经系统损伤中神经元死亡的方法。
• COMPOUNDS AND COMPOSITIONS FOR TREATING NEURONAL DEATH OR NEUROLOGICAL DYSFUNCTION
  申请人：GWAG Byoung Joo

  公开号：US20120301551A1

  公开（公告）日：2012-11-29

  The present invention relates to 2-hydroxy-alkylamino-benzoic acid derivatives and to a combination of cell necrosis inhibitor and lithium, process for the preparation of the derivatives or the combination, pharmaceutical formulation containing the derivatives or the combination, and use of the derivatives or the combination by either concomitant or sequential administration for improvement of treatment of neuronal death or neurological dysfunction. The derivatives and the combination of the present invention are useful for treating neurological diseases, such as amyotrophic lateral sclerosis (ALS, Lou Gehrig's disease), spinal muscular atrophy, Alzheimer's disease, Parkinson's disease, Huntington's disease, stroke, traumatic brain injury or spinal cord injury; and for treating ocular diseases such as glaucoma, diabetic retinopathy or macular degeneration.

  本发明涉及2-羟基-烷基氨基苯甲酸衍生物以及细胞坏死抑制剂和锂的组合物，制备衍生物或组合物的方法，含有衍生物或组合物的制药配方，以及通过同时或顺序给药使用衍生物或组合物来改善神经元死亡或神经功能障碍的治疗。本发明的衍生物和组合物对于治疗神经系统疾病非常有用，例如肌萎缩性侧索硬化症（ALS，路易·格里格氏病），脊髓肌肉萎缩症，阿尔茨海默病，帕金森病，亨廷顿病，中风，创伤性脑损伤或脊髓损伤；以及治疗眼科疾病，如青光眼，糖尿病性视网膜病变或黄斑变性。
• COSMETIC COMPOSITION COMPRISING 5-BENZYLAMINOSALICYLIC ACID DERIVATIVE AND LOCAL ADMINISTRATION METHOD THEREOF
  申请人：GNT Pharma Co., Ltd

  公开号：EP3998058A1

  公开（公告）日：2022-05-18

  The present invention relates to a composition comprising: a 5-benzyl aminosalicylic acid compound in chemical formula I or cosmetically acceptable salts thereof; and a cosmetically acceptable excipient suitable for local administration. The composition comprising the 5-benzyl aminosalicylic acid compound in chemical formula I or cosmetically acceptable salts thereof can be used for reducing or alleviating human skin aging by means of antioxidant, anti-inflammatory and whitening actions on the skin.

  本发明涉及一种组合物，该组合物包含：化学式 I 中的 5-苄基氨基水杨酸化合物或其美容上可接受的盐；以及适用于局部给药的美容上可接受的赋形剂。由化学式 I 中的 5-苄基氨基水杨酸化合物或其化妆品可接受盐组成的组合物可通过抗氧化、消炎和美白作用减少或缓解人体皮肤老化。
• COMPOUNDS, COMPOSITIONS AND METHODS FOR PREVENTING NEURODEGENERATION IN ACUTE AND CHRONIC INJURIES IN THE CENTRAL NERVOUS SYSTEM
  申请人：Neurotech Co., Ltd.

  公开号：EP1274675B1

  公开（公告）日：2004-09-01