Acetamide,2-amino-n-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]-,(r)- | 133163-25-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: Acetamide,2-amino-n-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]-,(r)-
• 英文别名: 2-amino-N-[(2R)-2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide
• CAS: 133163-25-4
• 化学式: C₁₂H₁₈N₂O₄
• 分子量: 254.28
• InChiKey: PTKSEFOSCHHMPD-JTQLQIEISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  93.8
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Benzodioxane and benzodioxolane derivatives and uses thereof
  申请人：Zhou Dahui

  公开号：US20060241172A1

  公开（公告）日：2006-10-26

  Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R 1 , R 2 , R 3 , R 4 , y, n, m, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.

  提供了化学式I或其药用可接受盐的化合物：其中R1、R2、R3、R4、y、n、m和Ar中的每一个如所定义，并在此处描述的类和亚类中，它们是大脑5-羟色胺受体2C亚型的激动剂或部分激动剂。这些化合物和含有这些化合物的组合物可用于治疗多种中枢神经系统疾病，如精神分裂症。
• Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
  申请人：——

  公开号：US20030130246A1

  公开（公告）日：2003-07-10

  Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.

  本文披露了一种在动物肠壁上具有高透过性的化合物。这些化合物可以选择性地与那些口服后吸收或透过肠壁运输效果不佳的药物结合，以提高药物-化合物共轭物口服后的治疗效果，并在口服药物-化合物共轭物时实现药物在全身血液中的浓度增加，可选择性地延长药物的治疗效果。还披露了含有这些化合物的药物组合物及使用这些化合物的方法。
• Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
  申请人：——

  公开号：US20030171303A1

  公开（公告）日：2003-09-11

  The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amenable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug compounds and methods for synthesizing these 1-acyl-alkyl derivatives.

  本发明提供了一种从1-酰基-烷基衍生物合成1-(酰氧基)-烷基衍生物的方法，该方法通常具有立体特异性，产率高，不需要使用活化中间体和/或有毒化合物，并且易于扩大生产规模。本发明还提供了已知药物化合物的1-酰基-烷基衍生物以及合成这些1-酰基-烷基衍生物的方法。
• Compounds for sustained release of orally delivered drugs
  申请人：——

  公开号：US20020098999A1

  公开（公告）日：2002-07-25

  Disclosed are methods for providing sustained systemic blood concentrations of orally delivered drugs. Still further, disclosed are compounds and pharmaceutical compositions that are used in such methods.

  揭示了提供口服药物持续系统血浆浓度的方法。此外，还揭示了在这些方法中使用的化合物和药物组合物。
• Benzofuranyl alkanamine derivatives and uses thereof
  申请人：Gross Laird Jonathan

  公开号：US20060247276A1

  公开（公告）日：2006-11-02

  Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R 1 , R 1′ , R 2 , R 3 , R 4 , n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.

  提供式I的化合物或其药学上可接受的盐： 其中R1、R1'、R2、R3、R4、n和Ar的定义如下，且在这里的类别和子类别中描述，这些化合物是2C亚型脑血清素受体的激动剂或部分激动剂。这些化合物和含有这些化合物的组合物可用于治疗多种中枢神经系统疾病，如精神分裂症。