D,L-arginine salt of 2-(4-isobutylphenyl)-propionic acid | 57469-81-5

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 英文名称: D,L-arginine salt of 2-(4-isobutylphenyl)-propionic acid
• 英文别名: 2-Amino-5-(diaminomethylideneamino)pentanoic acid;2-[4-(2-methylpropyl)phenyl]propanoic acid
• CAS: 57469-81-5
• 化学式: C₆H₁₄N₄O₂*C₁₃H₁₈O₂
• 分子量: 380.487
• InChiKey: GCCOJNYCFNSJII-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.73
• 重原子数：
  27
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  165
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• Aryl (Ethanoic) Propanoic Acid Ascorbyl Ester, Preparation Method Thereof And Medicament Containing The Same
  申请人：Tang Luhong

  公开号：US20120115897A1

  公开（公告）日：2012-05-10

  The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkaline, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, analgesia, treatment of arthritis, dysmenorrheal, multiple sclerosis, pneumonia cystic fibrosis and patent ductus arteriosus of premature infants, and prevention and treatment of cerebral apoplexy, hypoxic-ischemic brain damage, senile dementia and certain cancers.

  本发明设计并合成了芳基（乙酸）丙酸非甾体抗炎药物，例如布洛芬、酮洛芬和萘普生的抗坏血酸酯衍生物，以及这些衍生物与药用酸或药用碱的加成盐。以布洛芬为代表的非甾体抗炎药是一种常见的解热镇痛药。本发明除了具有抗炎效果外，还具有显著的解热和镇痛效果，安全性良好，因此不仅适用于成人，也适用于老年人、婴幼儿。芳基（乙酸）丙酸抗坏血酸酯可转化为抗坏血酸酯衍生物以及这些衍生物与药用酸或药用碱的加成盐，这可以提高其水溶性，便于静脉给药，减少起效时间，提高生物利用度，减少对胃肠道的刺激作用，增强穿透血脑屏障的能力，并可作为新型药物应用于消炎、解热、镇痛、治疗关节炎、痛经、多发性硬化症、肺炎、囊性纤维化和早产儿动脉导管未闭，以及预防和治疗脑卒中、缺氧缺血性脑损伤、老年痴呆症和某些癌症。
• Non-effervescent ibuprofen compositions
  申请人：Roche Consumer Health (Worldwide) Ltd

  公开号：EP0418043A1

  公开（公告）日：1991-03-20

  The unpleasant taste of water-soluble ibuprofen salts in aqueous solution is masked by incorporating in the solution a taste-masking amount of an alkali metal bicarbonate, alkali metal monohydrogen phosphate or alkali metal tribasic citrate. Preferably, the taste-masking compound is an alkali metal bicarbonate, especially sodium bicarbonate.

  在水溶液中加入一定量的碱金属碳酸氢盐、碱金属磷酸一氢盐或碱金属柠檬酸三盐，可掩盖水溶性布洛芬盐的难闻味道。掩味化合物最好是碱金属碳酸氢盐，特别是碳酸氢钠。
• Antiprotozoal methods, compositions and feedstuffs
  申请人：UNIVERSITEIT GENT

  公开号：EP1234508A1

  公开（公告）日：2002-08-28

  Methods and compositions for the prophylactic treatment of coccidiosis and other protozoal infections are described. Preferably, these are administered in the drinking water of the animals, e.g. in the drinking water of poultry to provide a mass prophylactic treatment. These formulations include L-arginine and may also include a modulator of the NO biosynthesis pathway, e.g. and NSAID such as Ibuprofen. These formulations have also been found to improve egg production in hens.

  本文介绍了预防性治疗球虫病和其他原生动物感染的方法和组合物。最好是在动物的饮用水中，例如在家禽的饮用水中施用，以提供大规模的预防性治疗。 这些制剂包括 L-精氨酸，还可能包括 NO 生物合成途径的调节剂，例如非甾体抗炎药，如布洛芬。 研究还发现，这些制剂可提高母鸡的产蛋量。
• ASCORBIC ACID ARYL ACETATE/PROPIONATE ESTER, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITION THEREOF
  申请人：Wuxi Hongrui Biomedical Technology Co., Ltd.

  公开号：EP2431361A1

  公开（公告）日：2012-03-21

  The present invention designs and synthesizes ascorbyl ester derivatives of aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkali. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkali, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, analgesia, treatment of arthritis, dysmenorrheal, multiple sclerosis, pneumonia cystic fibrosis and patent ductus arteriosus of premature infants, and prevention and treatment of cerebral apoplexy, hypoxic-ischemic brain damage, senile dementia and certain cancers.

  本发明设计合成了布洛芬、酮洛芬、萘普生等芳基（乙）丙酸类非甾体抗炎药物的抗坏血酸酯衍生物，以及衍生物与药用酸或药用碱的加成盐。以布洛芬为代表的非甾体抗炎药物是一种常用的解热镇痛药物。本发明除消炎作用外，解热镇痛效果显著，安全性好，不仅适用于成人，也适用于老人、婴幼儿。芳基（乙）丙酸抗坏血酸酯可转化为抗坏血酸酯衍生物及衍生物与药用酸或药用碱的加成盐，可提高其水溶性，便于静脉给药，缩短起效时间，提高生物利用度，减少对胃肠道的刺激作用、可作为新型药物应用于抗抑郁、镇痛、治疗关节炎、痛经、多发性硬化、肺炎囊性纤维化和早产儿动脉导管未闭，以及预防和治疗脑中风、缺氧缺血性脑损伤、老年性痴呆和某些癌症。
• MULTI-LAYER TRANSDERMAL DRUG DELIVERY SYSTEM CONTAINING IBUPROFEN OR STRUCTURAL ANALOGUE THEREOF
  申请人：Demotech. Inc.

  公开号：EP3900710A1

  公开（公告）日：2021-10-27

  A multi-layer transdermal drug delivery system containing ibuprofen or a structural analogue thereof, comprising a transdermal patch containing ibuprofen or a structural analogue thereof and a second combined layer. The transdermal patch comprises a polymer matrix layer, the polymer matrix layer comprising an active ingredient, a compound containing at least one amino group, and a pressure-sensitive adhesive. All or some of active ingredient-amino compound salts or all or some of free active ingredients formed in the polymer matrix layer are kept in a uniform dissolution state in the polymer matrix, and can be stably stored before use, without recrystalization. The transdermal drug delivery system can continuously and controllably deliver a therapeutically effective amount of ibuprofen or a structural analogue thereof for 12 to 24 hours in the absence of a transdermal enhancer, has excellent wearing ability, and avoids a cold flow phenomenon.

  一种含有布洛芬或其结构类似物的多层透皮给药系统，包括一个含有布洛芬或其结构类似物的透皮贴片和一个第二组合层。透皮贴片包括聚合物基质层，聚合物基质层包括活性成分、含有至少一个氨基的化合物和压敏粘合剂。聚合物基质层中形成的全部或部分活性成分-氨基化合物盐或全部或部分游离活性成分在聚合物基质中保持均匀溶解状态，使用前可稳定保存，不会再结晶。该透皮给药系统在不使用透皮增强剂的情况下，可在 12 至 24 小时内连续、可控地给药治疗有效量的布洛芬或其结构类似物，具有良好的耐磨性，并可避免冷流现象。