α-hydroxy-isobutyric acid m-toluidide | 103855-93-2

• 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: α-hydroxy-isobutyric acid m-toluidide
• 英文别名: α-Hydroxy-isobuttersaeure-m-toluidid；2-hydroxy-2-methyl-N-(3-methylphenyl)propanamide
• CAS: 103855-93-2
• 化学式: C₁₁H₁₅NO₂
• 分子量: 193.246
• InChiKey: WVTXCTBBKLPVRY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  3-甲基苯胺 、 2-羟基异丁酸乙酯 生成 α-hydroxy-isobutyric acid m-toluidide
  参考文献：
  名称：

  α-Hydroxy Amides and Related Compounds

  摘要：

  DOI：

  10.1021/ja01532a052

文献信息

• PHARMACEUTICAL FORMULATION COMPRISING (R)-BICALUTAMIDE
  申请人：AstraZeneca UK Limited

  公开号：EP1439823A1

  公开（公告）日：2004-07-28
• [EN] PHARMACEUTICAL FORMULATION COMPRISING (R) -BICALUTAMIDE<br/>[FR] PREPARATION PHARMACEUTIQUE CONTENANT DU (R)-BICALUTAMIDE
  申请人：ASTRAZENECA AB

  公开号：WO2003032950A1

  公开（公告）日：2003-04-24

  The present invention relates to a pharmaceutical formulation comprising the drug 4'-cyano-α', α', α'-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2-methylpropiono-m-toluidide in a solid dispersion with an enteric polymer having a pKa from 3 to 6, wherein > 50 % of the drug is provided in the form of the R-enantiomer. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of an enteric polymer having a pKa from 3 to 6 in solid dispersion with the drug, wherein > 50 % of the drug is provided in the form of the R-enantiomer, for increasing the bioavailability of the drug; for reducing inter-patient variability in plasma concentrations of the drug; for enhancing the storage stability of the drug; or for treating and/or reducing the risk of prostate cancer in a patient.