(4S)-5-氨基-5-氧代-4-[(2-苯基乙酰基)氨基]戊酸 | 104771-88-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: (4S)-5-氨基-5-氧代-4-[(2-苯基乙酰基)氨基]戊酸
• 英文名称: phenylacetylisoglutamine
• 英文别名: (4S)-5-amino-5-oxo-4-[(2-phenylacetyl)amino]pentanoic acid
• CAS: 104771-88-2
• 化学式: C₁₃H₁₆N₂O₄
• 分子量: 264.281
• InChiKey: XBJLFHMAIQTBJX-JTQLQIEISA-N

物化性质

• 沸点：
  639.6±55.0 °C(Predicted)
• 密度：
  1.279±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  19
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  110
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (4S)-5-氨基-5-氧代-4-[(2-苯基乙酰基)氨基]戊酸 、 苯乙酰氯 、 L-谷氨酰胺 生成 N-苯乙酰基-L-谷氨酰胺
  参考文献：
  名称：

  Phenylacetic acid compositions for treating or preventing hypercholesterolemia

  摘要：

  本发明揭示了一种药物组合物，其中包括选自苯乙酰谷氨酰胺、苯乙酰异谷氨酰胺和苯乙酸的一种或多种化合物，以及其药学上可接受的盐、类似物和前体，可选地还包括异谷氨酰胺，与药学上可接受的载体、稀释剂或赋形剂混合使用，用于治疗或预防高胆固醇血症和高甘油三酯血症。本发明还揭示了使用该药物组合物治疗或预防高胆固醇血症和高甘油三酯血症的方法。

  公开号：

  US06987131B1

文献信息

• Treatment regimen for administration of phenylacetylglutamine, phenylacetylisoglutamine, and/or phenylacetate
  申请人：——

  公开号：US20010044466A1

  公开（公告）日：2001-11-22

  Herein is disclosed a method of treating neoplastic disease, including cancer, comprising administering a pharmaceutical composition, the pharmaceutical composition comprising a highly concentrated aqueous solution of phenylacetylglutamine and phenylacetylisoglutamine in a 4:1 ratio, at an infusion rate of from 100 mL/hr to 400 mL/hr. In a further embodiment, herein is also disclosed a method of treating neoplastic disease, including cancer, comprising administering a pharmaceutical composition, the pharmaceutical composition comprising a highly concentrated aqueous solution of phenylacetate and (phenylacetylglutamine or phenylacetylisoglutamine) in a 4:1 ratio, at an infusion rate of from 100 mL/hr to 400 mL/hr. Herein are also disclosed the pharmaceutical compositions used in the above methods.

  本文披露了一种治疗恶性肿瘤疾病，包括癌症的方法，该方法包括给予一种药物组合物，该药物组合物包括苯乙酰谷氨酰胺和苯乙酰异谷氨酰胺的高浓度水溶液，比例为4：1，输注速率为100毫升/小时至400毫升/小时。在另一种实施方式中，本文还披露了一种治疗恶性肿瘤疾病，包括癌症的方法，该方法包括给予一种药物组合物，该药物组合物包括苯乙酸和（苯乙酰谷氨酰胺或苯乙酰异谷氨酰胺）的高浓度水溶液，比例为4：1，输注速率为100毫升/小时至400毫升/小时。本文还披露了上述方法中使用的药物组合物。
• Composition for Prevention or Treatment of Obesity, Dyslipidemia, Fatty Liver or Insulin Resistance Syndrome Comprising Camphene as Active Ingredients
  申请人：Park Tae Sun

  公开号：US20120035274A1

  公开（公告）日：2012-02-09

  Disclosed is a composition including camphene as an active ingredient for preventing or treating obesity, dyslipidemia, fatty liver or insulin resistance syndrome. The composition of the present disclosure including camphene as an active ingredient suppresses differentiation of adipocytes, reduces body fat, reduces visceral fat, reduces total cholesterol level, reduces serum triglyceride level and reduces liver tissue triglyceride level, and thus exhibits preventive or therapeutic activity for obesity, hyperlipidemia or fatty liver. Furthermore, the composition of the present disclosure exhibits the effect of improving type 2 diabetes or insulin resistance and related metabolic disease by significantly reducing fasting blood sugar level and blood insulin level. Also, the composition of the present disclosure exhibits the effect of reducing visceral fat by significantly reducing the expression of nuclear transcription factors (C/EBPα and PPARγ2) playing key roles in adipogenesis or their target gene (aP2), the effect of improving chronically activated inflammation in the visceral fat tissue induced by obesity by significantly reducing the expression of cytokines (TNF-α or IL-6) activating inflammation, and the effect of improving suppressed heat generation in the visceral fat tissue induced by obesity by significantly increasing the expression of UCP (UCP1 or UCP3) genes regulating body heat production.

  本公开涉及一种包括蒎烯作为活性成分的组合物，用于预防或治疗肥胖症、血脂异常、脂肪肝或胰岛素抵抗综合征。本公开的组合物包括蒎烯作为活性成分，可以抑制脂肪细胞的分化，降低体脂肪、内脏脂肪、总胆固醇水平、血清甘油三酯水平和肝脏组织甘油三酯水平，因此具有预防或治疗肥胖症、高脂血症或脂肪肝的活性。此外，本公开的组合物通过显著降低空腹血糖水平和血中胰岛素水平，展现了改善2型糖尿病或胰岛素抵抗及相关代谢性疾病的效果。同时，本公开的组合物通过显著降低核转录因子（C/EBPα和PPARγ2）及其靶基因（aP2）的表达，展现了减少内脏脂肪的效果；通过显著降低激活炎症的细胞因子（TNF-α或IL-6）的表达，展现了改善肥胖引起的内脏脂肪组织中慢性活化炎症的效果；通过显著增加调节体热产生的UCP（UCP1或UCP3）基因的表达，展现了改善肥胖引起的内脏脂肪组织中抑制性热产生的效果。
• Use of a combination of antineoplastons for the manufacture of a medicament for the treatment of neurofibromatosis
  申请人：BURZYNSKI, Stanislaw R.

  公开号：EP0680756A1

  公开（公告）日：1995-11-08

  The present invention provides methods for treating neurofibromatosis in humans by administering to an afflicted host pharmaceutical compositions containing a therapeutically effective amount of a combination of in a weight ratio ranging from about 1:1 to about 1:10 (A:B); wherein R is OH, NH₂, OW, or H; X is H, F, Cl, Br, I, OH, OW, NO₂ or NH₂; Y is H, F, Cl, Br, or I; W is or a C₁ to C₂ aliphatic group; Z is an aliphatic or aromatic group of C₁ to C₁₂; X and Y can both vary within the compound; or pharmaceutically acceptable salts thereof. Particularly disclosed herein is a composition comprising a 1:4 ratio of the sodium salts of phenylacetylglutamine and phenylacetic acid, formulated in both oral and parenteral forms. Typically, the patient is given the combination composition from 1 to 20g/day in divided doses. After several months of treatment patients exhibit significant decrease in number and size of nodules.

  本发明提供了治疗人类神经纤维瘤病的方法，其方法是向患病宿主施用药物组合物，该药物组合物含有治疗有效量的以下物质的组合 重量比范围为约 1:1 至约 1:10 (A:B)； 其中 R 是 OH、NH₂、OW 或 H； X 是 H、F、Cl、Br、I、OH、OW、NO₂ 或 NH₂； Y 是 H、F、Cl、Br 或 I； W 是 或 C₁ 至 C₂ 脂肪族基团； Z 是 C₁ 至 C₁₂ 脂肪族或芳香族基团； X 和 Y 可在化合物中同时变化；或 其药学上可接受的盐类。 本文特别公开了一种组合物，它由苯乙酰谷氨酰胺钠盐和苯乙酸钠盐按 1:4 的比例配制而成，既有口服形式，也有肠外形式。通常情况下，患者每天分次服用 1 至 20 克的组合物。经过几个月的治疗后，患者的结节数量和大小都会明显减少。
• Formulation of amino acids and riboflavin useful to reduce toxic effects of cytotoxic chemotherapy
  申请人：Burzynski R. Stanislaw

  公开号：US20050182064A1

  公开（公告）日：2005-08-18

  Pharmaceutical compositions effective in alleviating or reducing the effects of fatigue and weakness associated with cancer and cancer chemotherapy are disclosed. The pharmaceutical compositions of the present invention comprise riboflavin, effectors of the urea cycle in free form or pharmacologically acceptable salts thereof, and amino acids selected from the groups of essential and non-essential amino acids, in free form or pharmaceutically acceptable salts thereof, suitably combined with appropriate carriers, diluents, or excipients. Also disclosed are methods of alleviating or reducing the effects of fatigue and weakness associated with cancer and cancer chemotherapy by administration of pharmaceutical compositions of the present invention.

  本发明公开了可有效缓解或减轻与癌症和癌症化疗相关的疲劳和虚弱症状的药物组合物。本发明的药物组合物包含核黄素、游离形式的尿素循环效应物或其药理学上可接受的盐，以及选自必需氨基酸和非必需氨基酸组的游离形式的氨基酸或其药理学上可接受的盐，与适当的载体、稀释剂或赋形剂适当结合。还公开了通过施用本发明的药物组合物来缓解或减轻与癌症和癌症化疗相关的疲劳和虚弱的影响的方法。
• Method for the treatment of von Hippel-Lindau (VHL) disease with phenylacetyl-derivatives
  申请人：Burzynski R. Stanislaw

  公开号：US20060205818A1

  公开（公告）日：2006-09-14

  Provided are methods of treating von Hippel-Lindau disease (VHL). Specifically embodiments of the invention provide methods for the treatment of a patient afflicted with VHL using phenylacetyl-derivatives. Preferred embodiments of the invention provide for the use of phenylacetic acid (or its sodium salt), phenylacetylglutamine (or its sodium salt) and/or phenylacetylisoglutamine (or its sodium salt) to treat VHL. Other embodiments of the invention provide for the use of phenylacetyl-derivatives for the manufacture of a medicament for the treatment of VHL.

  本发明提供了治疗von Hippel-Lindau病（VHL）的方法。具体而言，本发明的实施方案提供了使用苯乙酰基衍生物治疗VHL患者的方法。本发明的优选实施方案提供了使用苯乙酸（或其钠盐）、苯乙酰基谷氨酰胺（或其钠盐）和/或苯乙酰基异谷氨酰胺（或其钠盐）治疗VHL的方法。本发明的其他实施方案提供了苯乙酰基衍生物用于制造治疗 VHL 的药物。