promethazine dibenzoyl-L-tartrate | 121445-94-1

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: promethazine dibenzoyl-L-tartrate
• 英文别名: (2R,3R)-2,3-dibenzoyloxybutanedioic acid;N,N-dimethyl-1-phenothiazin-10-ylpropan-2-amine
• CAS: 121445-94-1
• 化学式: C₁₇H₂₀N₂S*C₁₈H₁₄O₈
• 分子量: 642.73
• InChiKey: SPIUNWBIJCSOCC-DTPOWOMPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.85
• 重原子数：
  46
• 可旋转键数：
  12
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  159
• 氢给体数：
  2
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  异丙嗪 、 O,O'-dibenzoyl-L-tartaric acid 在 盐酸 作用下， 以 丙酮 、 乙醚 为溶剂， 反应 72.0h， 生成 promethazine dibenzoyl-L-tartrate
  参考文献：
  名称：

  [EN] CONTROLLED RELEASE COMPOSITIONS AND METHODS FOR USING SAME
  [FR] COMPOSITIONS A LIBERATION PROGRESSIVE ET SON PROCEDE D'UTILISATION

  摘要：

  公开号：

  WO2003105811A3

文献信息

• Controlled release compositions and methods for using same
  申请人：Putcha Lakahmi

  公开号：US20050220888A1

  公开（公告）日：2005-10-06

  Pharmaceutical preparations adapted for mucosal delivery, preferably for nasal delivery, which can be easily and safely used over days to weeks with minimal side effects. The pharmaceutical preparations comprise microcapsules comprising at least one pharmaceutically active agent. The microcapsules provide controlled release of the pharmaceutically active agent. Cytotoxicity is avoided for cytotoxic pharmaceutically active agents and/or for cytotoxic dosages by one or more of the following: (a) manipulating the mucosal transport rate of the pharmaceutically active agent through the mucosal bodies to achieve a transport rate which is substantially the same as the controlled release rate, and/or (b) selecting only a most active and/or less cytotoxic enantiomer of the pharmaceutically active agent for use in the pharmaceutical preparation.

  适用于黏膜递送的制药制剂，优选为鼻递送，可在数天至数周内轻松安全地使用，副作用最小。该制药制剂包括至少一种药物活性成分的微胶囊。微胶囊提供药物活性成分的控制释放。通过以下一种或多种方式避免细胞毒性药物活性成分和/或细胞毒性剂量的细胞毒性：(a) 通过调节药物活性成分通过黏膜体的黏膜运输速率，实现与控制释放速率基本相同的运输速率，和/或(b) 仅选择药物活性成分的最活跃和/或细胞毒性较小的对映体用于制药制剂。
• Phenothiazine enantiomers as agents for the prevention of bone loss
  申请人：Boland J. Edward

  公开号：US20060258650A1

  公开（公告）日：2006-11-16

  Disclosed is the unexpected finding that enantiomers of phenothiazines, preferably the (+) enantiomer of promethazine, are particularly effective in inhibiting the bone resorbing cells, osteoclasts, thus providing new uses and methods for reducing bone loss and, e.g., treating periodontitis and osteoporosis. The invention provides a range of such uses, methods, medicaments and associated compositions and kits.

  本发明揭示了一个意外的发现，即苯并噻嗪的对映体，特别是异丙嗪的(+)对映体，对于抑制骨吸收细胞——破骨细胞特别有效，从而提供了减少骨量损失和治疗牙周病和骨质疏松症的新用途和方法。该发明提供了一系列这样的用途、方法、药物和相关组合物和试剂盒。
• SINGLE PHENOTHIAZINE ENANTIOMERS AS AGENTS FOR THE PREVENTION OF BONE LOSS
  申请人：McDonough Joseph

  公开号：US20100285087A1

  公开（公告）日：2010-11-11

  Enantomerically purified phenothiazines are provided as active ingredients of medicaments to limit activity of bone resorbing cells so as to reduce bone loss. Novel phenothiazine derivatives are provided. A method of synthesizing enantiomerically pure phenothiazine derivatives is provided that avoids post-synthetic enantiomeric resolution.

  提供了对映纯的苯并噻嗪作为药物的活性成分，以限制骨吸收细胞的活动，从而减少骨质流失。提供了新颖的苯并噻嗪衍生物。提供了一种合成对映纯苯并噻嗪衍生物的方法，避免了后合成对映异构体的分离。
• US8637503B2
  申请人：——

  公开号：US8637503B2

  公开（公告）日：2014-01-28
• [EN] PHENOTHIAZINE ENANTIOMERS AS AGENTS FOR THE PREVENTION OF BONE LOSS<br/>[FR] ENANTIOMERES DE PHENOTHIAZINE UTILES COMME AGENTS DE PREVENTION DE LA PERTE OSSEUSE
  申请人：UNIV TEXAS

  公开号：WO2004110458A1

  公开（公告）日：2004-12-23

  Disclosed is the unexpected finding that enantiomers of phenothiazines, preferably the (+) enantiomer of promethazine, are particularly effective in inhibiting the bone resorbing cells, osteoclasts, thus providing new uses and methods for reducing bone loss and, e.g., treating periodontitis and osteoporosis. The invention provides a range of such uses, methods, medicaments and associated compositions and kits.