5-[3-(4-nitrophenyl)-n-propyl]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-[3-(4-nitrophenyl)-n-propyl]aminosalicylic acid
• 英文别名: 2-hydroxy-5-[3-(4-nitrophenyl)propylamino]benzoic acid
• 化学式: C₁₆H₁₆N₂O₅
• 分子量: 316.313
• InChiKey: AEDBPOPSLDSBMP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  115
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  5-氨基水杨酸 、 1-(3-溴丙基)-4-硝基苯 以520 mg (50% yield) of 5-[3-(4-nitrophenyl)-n-propyl]aminosalicylic acid was obtained as a pale yellow solid的产率得到5-[3-(4-nitrophenyl)-n-propyl]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, 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：US20030045575A1

  公开（公告）日：2003-03-06

  The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn 2+ , and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn 2+ neurotoxicity, and free radical neurotoxicity.

  本发明提供了用于预防和预防伴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5-苄氨基水杨酸（BAS）及其衍生物的合成。BAS及其衍生物通过N-甲基-D-天冬氨酸、Zn2+和活性氧物种对皮层神经元的毒性侵害进行保护。因此，本发明提供了用于治疗中风、创伤性脑和脊髓损伤、癫痫以及伴有严重神经元丧失的神经退行性疾病的组合物和方法，这些疾病通过兴奋毒性、Zn2+神经毒性和自由基神经毒性引起。
• Pharmaceutical Composition for Treating or Preventing Degenerative and Inflammatory Diseases
  申请人：GWAG Byoung-Joo

  公开号：US20090240079A1

  公开（公告）日：2009-09-24

  The present invention relates to a pharmaceutical composition useful for treating or preventing inflammatory disease and cell damage, and a method for treating or preventing inflammatory disease and cell damage. The present invention uses the 2-hydroxybenzoic acid derivative represented by the specific chemical formula or its pharmaceutically acceptable salt. The compound of the present invention is useful for treating or preventing cell damage and inflammatory disease including gastritis, gastric ulcer, pancreatitis, colitis, arthritis, diabetes, arteriosclerosis, nephritis, hepatitis, Alzheimer's disease, Parkinson's disease and Lou Gehrig's disease.

  本发明涉及一种用于治疗或预防炎症性疾病和细胞损伤的药物组合物，以及一种用于治疗或预防炎症性疾病和细胞损伤的方法。本发明使用由特定化学式表示的2-羟基苯甲酸衍生物或其药用可接受的盐。本发明的化合物对治疗或预防包括胃炎、胃溃疡、胰腺炎、结肠炎、关节炎、糖尿病、动脉硬化、肾炎、肝炎、阿尔茨海默病、帕金森病和路易·盖里格病在内的细胞损伤和炎症性疾病有益。
• 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。