2-azaniumyl-5-[[1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-5-oxopentanoate

• 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
• 英文名称: 2-azaniumyl-5-[[1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-5-oxopentanoate
• 化学式: C16H19N3O5
• 分子量: 333.34
• InChiKey: CATMPQFFVNKDEY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.7
• 重原子数：
  24
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  146
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• AMIDE COMPOUNDS, METHODS FOR PREPARATION, AND USE THEREOF AS AGENTS FOR THE TREATMENT AND PREVENTION OF DISEASES CAUSED BY RNA- AND/OR DNA-CONTAINING VIRUSES, AND CONCOMITANT DISEASES
  申请人：OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU "PHARMENTERPRISES"

  公开号：US20170183318A1

  公开（公告）日：2017-06-29

  The present invention relates to medicine and includes a method for preventing and treating diseases caused by RNA- and DNA-containing viruses, and concomitant diseases, wherein the method comprises the use of an effective amount of compounds of general formula I or pharmaceutically acceptable salts thereof. The invention also relates to methods for preparing said compounds, pharmaceutical compositions for the prevention or treatment of diseases caused by RNA- and DNA-containing viruses, said compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof. The invention addresses the object of providing a novel agent effective in the treatment of diseases caused by an RNA-containing virus belonging to the Enterovirus, Metapneumovirus, Pneumovirus, Respirovirus, or Alfa-coronavirus genus, and/or by a DNA-containing virus belonging to the Adenoviridae and/or Herpesviridae family, and in the prevention and treatment of asthma exacerbation, chronic obstructive pulmonary disease, mucoviscidosis, conjunctivitis, gastroenteritis, hepatitis, myocarditis; in the prevention and treatment of rhinorrhea, acute and infectious rhinitis, pharyngitis, nasopharyngitis, tonsillitis, laryngitis, laryngotracheitis, laryngotracheobronchitis, bronchitis, bronchiolitis, pneumonia, or airway obstructive syndrome.

  本发明涉及医学，包括一种用于预防和治疗由RNA-和DNA-含病毒引起的疾病以及相关疾病的方法，其中该方法包括使用通式I的化合物或其药用可接受盐的有效量。该发明还涉及制备上述化合物的方法，用于预防或治疗由RNA-和DNA-含病毒引起的疾病的药物组合物，该组合物包括通式I的化合物或其药用可接受盐的有效量。该发明解决了提供一种新型药剂的目标，用于治疗属于肠病毒、副呼吸道病毒、呼吸道病毒、呼吸道病毒或阿尔法冠状病毒属的RNA-含病毒引起的疾病，和/或属于腺病毒科和/或疱疹病毒科的DNA-含病毒引起的疾病，并在预防和治疗哮喘急性发作、慢性阻塞性肺疾病、黏液囊病、结膜炎、胃肠炎、肝炎、心肌炎；在预防和治疗流涕、急性和感染性鼻炎、咽炎、鼻咽炎、扁桃体炎、喉炎、喉气管炎、喉气管支气管炎、支气管炎、支气管炎、肺炎或气道梗阻综合征方面具有有效性。
• CRYSTALLINE D-ISOGLUTAMYL-D-TRYPTOPHAN AND THE MONO AMMONIUM SLAT OF D-ISOGLUTAMYL-D-TRYPTOPHAN
  申请人：TAM Tim Fat

  公开号：US20130059791A1

  公开（公告）日：2013-03-07

  A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D-tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1:1) is a stable pharmaceutical solid.

  提供了一种制备纯结晶D-异谷氨酰-D-色氨酸的过程，包括去保护基的步骤，将基本上纯的N-叔丁氧羰基-D-异谷氨酰-D-色氨酸或其二酯去保护，得到基本上纯的D-异谷氨酰-D-色氨酸。还提供了一种从基本上纯的N-叔丁氧羰基-D-异谷氨酰-D-色氨酸制备纯D-异谷氨酰-D-色氨酸单酰胺盐的过程。D-异谷氨酰-D-色氨酸铵盐（1:1）是一种稳定的药物固体。
• PHARMACEUTICALLY ACCEPTABLE SALTS OF THYMODEPRESSIN AND PREOCESSES FOR THEIR MANUFACTURE.
  申请人：Tam Tim Fat

  公开号：US20130072692A1

  公开（公告）日：2013-03-21

  The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1).

  本发明涉及D-异谷氨酰-D-色氨酸的药学可接受的结晶和非晶态盐，以及其制造工艺、包含它们的制药组合物，以及它们在制备用于治疗各种疾病和/或疾病的制药组合物中的用途。特别是，本发明涉及D-异谷氨酰-D-色氨酸钾盐（1:1）、D-异谷氨酰-D-色氨酸锂盐（1:1）、D-异谷氨酰-D-色氨酸钙盐（2:1）、D-异谷氨酰-D-色氨酸镁盐（2:1）和D-异谷氨酰-D-色氨酸有机铵盐（1:1）。
• Pharmazeutisches Mittel zur Behandlung von virusbedingten Krankheiten, wie Grippe
  申请人：OOO "CytoNIR"

  公开号：EP2918282A1

  公开（公告）日：2015-09-16

  Die Erfindung betrifft ein pharmazeutisches Mittel zur Behandlung von virusbedingten Krankheiten, wie Grippe. Die Erfindung ist in der Medizin einsetzbar, und zwar für Peptide-Arzneimittel und insbesondere für Präparate, die bei einer Behandlung von Viruskrankheiten, wie Grippe, angewendet werden können. Das pharmazeutische Mittel enthält einen Induktor eines endogenen Interferons Glutaminsäure-Dipeptid, welches aus einer Gruppe gewählt ist, die α-Glutamyltryptophan, γ-Glutamyltryptophan und α-Lysylglutamyl einschließt, und einen Koinduktor eines endogenen Interferons Glycyrrhizinsäure in Form eines Natriumsalzes oder eines Ammoniumsalzes nach der Erfindung in folgenden Mengen: Dipeptid 0,02 - 0,2 mg/kg des Körpergewichts des Patienten, Glycyrrhizinat 0,2 - 2,0 mg/kg des Körpergewichts des Patienten. Damit ist mit diesem Mittel die Aufgabe der Erfindung gelöst: Das Mittel kann bei einer Behandlung von beliebigen Arten der Grippe, darunter auch von pandemischer Grippe, unabhängig von ihrem Pathogenitätsgrad erfolgreich angewendet werden.

  本发明涉及一种用于治疗流感等病毒性疾病的药物组合物。 本发明适用于医药，即肽类药物，特别是可用于治疗流感等病毒性疾病的制剂。 药物组合物包括根据本发明选自包括 α-谷氨酰色氨酸、γ-谷氨酰色氨酸和 α-赖氨酰谷氨酰在内的一组的内源性干扰素谷氨酸二肽的诱导剂和以钠盐或铵盐形式存在的内源性干扰素甘草酸的辅助诱导剂，其用量如下：二肽 0.02 - 0.2 mg/kg 病人体重，甘草酸盐 0.2 - 2.0 mg/kg 病人体重。 这样，本发明的任务就通过这种制剂得到了解决：这种制剂可以成功地用于治疗任何类型的流感，包括大流行性流感，无论其致病程度如何。
• Methods and systems for determining autism spectrum disorder risk
  申请人：Laboratory Corporation of America Holdings

  公开号：US10041932B2

  公开（公告）日：2018-08-07

  In certain embodiments, the invention stems from the discovery that analysis of population distribution curves of metabolite levels in blood can be used to facilitate predicting risk of autism spectrum disorder (ASD) and/or to differentiate between ASD and non-ASD developmental delay (DD) in a subject. In certain aspects, information from assessment of the presence, absence, and/or direction (upper or lower) of a tail effect in a metabolite distribution curve is utilized to predict risk of ASD and/or to differentiate between ASD and DD.

  在某些实施方案中，本发明源于发现血液中代谢物水平的群体分布曲线分析可用于促进预测自闭症谱系障碍（ASD）的风险和/或区分受试者的自闭症谱系障碍和非自闭症谱系障碍发育迟缓（DD）。在某些方面，评估代谢物分布曲线中尾部效应的存在、不存在和/或方向（上部或下部）的信息可用于预测 ASD 的风险和/或区分 ASD 和 DD。