Aminocaproylhistamine | 78102-23-5

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: Aminocaproylhistamine
• 英文别名: 6-amino-N-[2-(1H-imidazol-5-yl)ethyl]hexanamide
• CAS: 78102-23-5
• 化学式: C₁₁H₂₀N₄O
• 分子量: 224.306
• InChiKey: RYEBECHCSCRVBJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  16
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  83.8
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  视黄醛 、 Aminocaproylhistamine 在 3 A molecular sieve 作用下， 以 乙醇 为溶剂， 反应 8.0h， 生成
  参考文献：
  名称：

  视觉颜料模型。咪唑基对视网膜希夫碱吸收最大值的影响

  摘要：

  使用外部添加或分子内组合的咪唑基研究了标题效应。N-视黄基丁胺在中性条件下被咪唑衍生物质子化，并且与羧酸相比在更长的波长下被吸收。分子内结合咪唑基的吸收峰受结构的影响很大，质子化的 Nα-视黄亚基-L-组氨酸十八烷基酰胺在 494 nm 处具有最大吸收，由诱导效应和极性咪唑基引起。

  DOI：

  10.1246/bcsj.54.1101
• 作为产物：
  描述：

  N-苄氧羰基--6-氨基己酸 在 sodium hydroxide 、 氢溴酸 、 sodium carbonate 、 N,N'-二环己基碳二亚胺 作用下， 以 溶剂黄146 为溶剂， 反应 6.75h， 生成 Aminocaproylhistamine
  参考文献：
  名称：

  视觉颜料模型。咪唑基对视网膜希夫碱吸收最大值的影响

  摘要：

  使用外部添加或分子内组合的咪唑基研究了标题效应。N-视黄基丁胺在中性条件下被咪唑衍生物质子化，并且与羧酸相比在更长的波长下被吸收。分子内结合咪唑基的吸收峰受结构的影响很大，质子化的 Nα-视黄亚基-L-组氨酸十八烷基酰胺在 494 nm 处具有最大吸收，由诱导效应和极性咪唑基引起。

  DOI：

  10.1246/bcsj.54.1101

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。
• AMIDE COMPOUNDS AND METHODS FOR THE PRODUCTION AND USE THEREOF
  申请人：Obschestvo S Ogranichennoi Otvetstennostiyu "Pharmenterprises"

  公开号：EP3118211A1

  公开（公告）日：2017-01-18

  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.

  本发明涉及医药，包括一种预防和治疗由含RNA和DNA病毒引起的疾病以及伴随疾病的方法，其中该方法包括使用有效量的通式I化合物或其药学上可接受的盐。本发明还涉及制备所述化合物的方法、用于预防或治疗由含 RNA 和 DNA 病毒引起的疾病的药物组合物，所述组合物包含有效量的通式 I 化合物或其药学上可接受的盐。本发明的目的是提供一种新型制剂，有效治疗由肠病毒属、偏肺病毒属、肺炎病毒属、呼吸道病毒属或阿法-冠状病毒属的含 RNA 病毒引起的疾病、和/或属于腺病毒科和/或疱疹病毒科的含 DNA 病毒，以及预防和治疗哮喘加重、慢性阻塞性肺病、粘液粘稠病、结膜炎、肠胃炎、肝炎、心肌炎；预防和治疗鼻炎、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、肺炎或气道阻塞综合征。
• ——
  作者：I. Yu. Garipova、V. N. Silnikov

  DOI：10.1023/a:1021329324527

  日期：——

  The reactions of histamine, the natural dipeptide carcinine (beta-Ala-HA), and its analogs with 5'-monodeoxyribonucleotides (dNMP) in the presence of triphenylphosphine, 2,2'-dipyridyl disulfide, and N-methylimidazole were studied. The yield of phosphamide derivatives decreases from 72% to 17% as the length of the linker group between the imidazole ring and the terminal aliphatic amino group is increased. Hydrolytic stability of the resulting conjugates was examined. The stability of the bonds in the -O-P(O)(2)-NH- group linking the nucleotide and peptide portions of the conjugate depends on the nature of the heterocyclic base of the nucleotide and decreases in the series dTMP > dCMP > dAMP.
• PRODUIT DE COUPLAGE DE L'HISTAMINE ET D'UN ACIDE AMINE
  申请人：EXSYMOL S.A.M.

  公开号：EP0684944B1

  公开（公告）日：2001-07-25
• US4381239A
  申请人：——

  公开号：US4381239A

  公开（公告）日：1983-04-26