N-(苄氧基)-n-((3s,4r)-6-氰基-3-羟基-2,2-二甲基苯并二氢吡喃-4-基)乙酰胺 | 127408-30-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 中文名称: N-(苄氧基)-n-((3s,4r)-6-氰基-3-羟基-2,2-二甲基苯并二氢吡喃-4-基)乙酰胺
• 英文名称: N-(Benzyloxy)-N-((3S,4R)-6-cyano-3-hydroxy-2,2-dimethylchroman-4-yl)acetamide
• 英文别名: N-[(3S,4R)-6-cyano-3-hydroxy-2,2-dimethyl-3,4-dihydrochromen-4-yl]-N-phenylmethoxyacetamide
• CAS: 127408-30-4
• 化学式: C₂₁H₂₂N₂O₄
• mdl: MFCD00899866
• 分子量: 366.4
• InChiKey: RHFUXPCCELGMFC-UXHICEINSA-N

物化性质

• 沸点：
  513.4±60.0 °C(Predicted)
• 密度：
  1.28±0.1 g/cm3(Predicted)
• 溶解度：
  温和加热下在乙醇中的溶解度为 5 mM，在 DMSO 中的溶解度为 25 mM

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  82.8
• 氢给体数：
  1
• 氢受体数：
  5

制备方法与用途

生物活性

Y-27152 是KATP (Kir6)通道开放剂 Y-26763 的前体药物，是一种长效的钾离子通道开放剂。在高血压大鼠和狗处于清醒状态时，Y-27152 可发挥降压作用，并且具有较低的心动过速副作用。

靶点

K+ 通道

文献信息

• METHOD OF MANUFACTURING COMPOSITION FOR SOLID MEDICINE
  申请人：JAPAN TOBACCO INC.

  公开号：EP0667153A1

  公开（公告）日：1995-08-16

  A method of manufacturing a composition for solid medicine having a controlled elution rate and containing as active ingredients a potassium channel activator and a pharmaceutically permissible water-insoluble macromolecular substance of cellulose, comprising the steps of dissolving a potassium channel activator in a solvent to obtain a medical solution, adding the medical solution to a water-insoluble macromolecular substance of cellulose which is inactive with respect to the solvent, and which has a quantity necessary and sufficient to obtain a predetermined elution rate, and mixing them together uniformly, and then drying the resultant mixture so as to remove the solvent therefrom; and a solid medical composition obtained by this manufacturing method. According to the method of the present invention, the elution rate of the active component of the potassium channel activator-containing medicine, a sustained release medicine, can be controlled easily and highly reproducible.

  一种制造具有可控洗脱率的固体药物组合物的方法，该组合物含有一种钾离子通道活化剂和一种药学上允许的纤维素水不溶性大分子物质作为活性成分，该方法包括以下步骤： 将钾离子通道活化剂溶解在溶剂中，得到一种医用溶液、将该医用溶液添加到对溶剂无活性的水不溶性纤维素大分子物质中，该纤维素大分子物质的数量必须且足以获得预定的洗脱率，并将它们均匀地混合在一起，然后干燥所得混合物，以除去其中的溶剂；以及通过这种制造方法获得的固体药物组合物。根据本发明的方法，含有钾通道激活剂的药物（一种缓释药物）的活性成分的洗脱率可以很容易地控制，并且具有很高的可重复性。
• Benzopyran compound and its pharmaceutical use
  申请人：YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

  公开号：EP0339562B1

  公开（公告）日：1993-09-15
• METHODS OF TREATING NEUROPSYCHIATRIC DISORDERS
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20200197445A1

  公开（公告）日：2020-06-25

  The present disclosure is directed to a method of treating a neuropsychiatric disorder. This method involves selecting a subject having the neuropsychiatric disorder and administering to the selected subject a preparation of glial progenitor cells at a dosage effective to treat the neuropsychiatric disorder in the subject. Another aspect of the disclosure is directed to a method of treating a neuropsychiatric disorder that includes selecting a subject having the neuropsychiatric disorder and administering, to the selected subject, a potassium (K + ) channel activator at a dosage effective to restore normal brain interstitial glial K + levels in the selected subject and treat the neuropsychiatric disorder is also disclosed.
• US5021432A
  申请人：——

  公开号：US5021432A

  公开（公告）日：1991-06-04
• US5143936A
  申请人：——

  公开号：US5143936A

  公开（公告）日：1992-09-01