(+/-)-1,3t-dimethyl-4-m-tolyl-piperidin-4r-ol | 109245-65-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (+/-)-1,3t-dimethyl-4-m-tolyl-piperidin-4r-ol
• 英文别名: (3S,4S)-1,3-dimethyl-4-(3-methylphenyl)piperidin-4-ol
• CAS: 109245-65-0
• 化学式: C₁₄H₂₁NO
• 分子量: 219.327
• InChiKey: QNEWTHRJANXODU-JSGCOSHPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  23.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  1,3-二甲基-4-哌啶酮 、 甲基苯锂 在 乙醚 作用下， 生成 (+/-)-1,3t-dimethyl-4-m-tolyl-piperidin-4r-ol 、 alkaline earth salt of/the/ methylsulfuric acid
  参考文献：
  名称：

  Beckett et al., Journal of Pharmacy and Pharmacology, 1957, vol. 9, p. 939,944

  摘要：

  DOI：

文献信息

• Solid dispersions of opioid antagonists
  申请人：Kumar Virendra

  公开号：US20070082053A1

  公开（公告）日：2007-04-12

  Solid dispersions of stable, amorphous opioid antagonists, particularly [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid, with improved water solubility and bioavailability are disclosed. Also disclosed are methods of preventing or treating a side effect associated with an opioid. In addition, methods of treating or preventing pain, ileus, and opioid bowel dysfunction are disclosed.

  本发明揭示了稳定的非晶态阿片受体拮抗剂的固体分散体，特别是[[2(S)-[[4(R)-(3-羟基苯基)-3(R),4-二甲基哌啶基]甲基]-1-氧代-3-苯基丙基]氨基]乙酸，具有改善的水溶性和生物利用度。还揭示了预防或治疗与阿片受体相关的副作用的方法。此外，还揭示了治疗或预防疼痛、肠梗阻和阿片类药物肠功能紊乱的方法。
• Compositions containing opioid antagonists
  申请人：Buehler D. John

  公开号：US20070092576A1

  公开（公告）日：2007-04-26

  Compositions containing opioid antagonists are disclosed, particularly alvimopan and its active metabolite in solid dosage forms, where the drug is uniformly distributed, achieves the desired bioavailability, and is stable. Methods of preparing and using the compositions containing opioid antagonists are also disclosed. The results are achieved by a combination of processing techniques and component selection.

  披露了含有阿片受体拮抗剂的组合物，特别是阿尔维莫潘及其在固体剂型中的活性代谢物，其中药物均匀分布，达到所需的生物利用度，并且稳定。还披露了制备和使用含有阿片受体拮抗剂的组合物的方法。通过一系列加工技术和成分选择实现了这些结果。
• COMPOSITIONS CONTAINING OPIOID ANTAGONISTS
  申请人：Buehler John D.

  公开号：US20100240690A1

  公开（公告）日：2010-09-23

  Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and provide maximum levels of opioid antagonists when administered parenterally, particularly via injection. The results are achieved by a combination of processing techniques and component selection.
• US7700626B2
  申请人：——

  公开号：US7700626B2

  公开（公告）日：2010-04-20
• US7914776B2
  申请人：——

  公开号：US7914776B2

  公开（公告）日：2011-03-29