左炔诺孕酮丁酸酯 | 86679-33-6

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 中文名称: 左炔诺孕酮丁酸酯
• 英文名称: levonorgestrel 17β-butyrate
• 英文别名: Levonorgestrel n-butanoate；levonorgestrel butanoate；Levonorgestrel butyrate；[(8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-3-oxo-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-yl] butanoate
• CAS: 86679-33-6
• 化学式: C₂₅H₃₄O₃
• 分子量: 382.543
• InChiKey: GPKLGCALNRZIDS-AYEDEZQKSA-N

物化性质

• 沸点：
  491.7±45.0 °C(Predicted)
• 密度：
  1.11

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.76
• 拓扑面积：
  43.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  丁酰氯 、 左炔诺孕酮 在 thallium (I) ethoxide 作用下， 生成 左炔诺孕酮丁酸酯
  参考文献：
  名称：

  Long-acting contraceptive agents: Design of the who chemical synthesis programme

  摘要：

  The great demand for improved long-acting injectable steroid contraceptives, particularly in developing countries, and the relative lack of interest from the pharmaceutical industry to develop such products stimulated WHO to launch a synthetic and screening programme to find improved, safe and acceptable injectable preparations. More than 210 esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) and levonorgestrel (D-(-)-13 beta-ethyl-17 alpha-ethynyl-17 beta-hydroxygon-4-en-3-one) have been prepared in university-based research laboratories situated mainly in developing countries, and then screened by NICHHD in animal models. The following three compounds, levonorgestrel butanoate, cyclopropylcarboxylate and cyclobutylcarboxylate, proved to be particularly long-acting when administered as microcrystalline suspensions. The overall strategy of this research and development programme is described.

  DOI：

  10.1016/0039-128x(83)90095-8

文献信息

• LONGER-ACTING PROGESTIN PRODRUG CONTRACEPTIVES
  申请人：Evestra, Inc.

  公开号：US20190117670A1

  公开（公告）日：2019-04-25

  Described herein are progestin compounds that have extended release rates and that can be used without an estrogen to produce a contraceptive state.

  本文描述了具有延长释放速率的孕激素化合物，可以在不使用雌激素的情况下用于产生避孕状态。
• Controlled release dosage form
  申请人：TRIASTEK, INC.

  公开号：US10143626B2

  公开（公告）日：2018-12-04

  The present invention generally relates to a pharmaceutical dosage form and controlled release of biologically active agents, diagnostic agents, reagents, cosmetic agents, and agricultural/insecticide agents. In one embodiment, the dosage form has a substrate that forms a compartment, wherein the substrate includes at least a first piece and a second piece, wherein the first piece operably links to the second piece. The dosage form contains a drug content that is loaded into the compartment. The dosage form also has a releaser operably linked to the substrate which upon contact with water or body fluid is capable of separating the first and second piece to open the compartment and release the drug content.

  本发明一般涉及一种药物剂型和生物活性制剂、诊断制剂、试剂、化妆品制剂和农用/杀虫剂制剂的控制释放。在一个实施方案中，该剂型具有形成隔室的基质，其中基质至少包括第一片和第二片，其中第一片与第二片可操作地连接。剂型含有装入隔室的药物成分。该剂型还具有与基质可操作连接的释放器，该释放器在与水或体液接触时能够分离第一和第二片，从而打开隔室并释放药物成分。
• Oral drug dosage forms having desired drug release profiles and uses thereof
  申请人：Triastek, Inc.

  公开号：US10258575B2

  公开（公告）日：2019-04-16

  The present disclosure provides a stable solid pharmaceutical dosage form for oral administration. The dosage form includes a substrate that forms at least one compartment and a drug content loaded into the compartment. The dosage form is so designed that the active pharmaceutical ingredient of the drug content is released in a controlled manner.

  本公开提供了一种用于口服的稳定固体药物剂型。该剂型包括至少形成一个小室的基质和装入小室的药物成分。该剂型的设计使药物内容物中的活性药物成分以可控方式释放。
• Compartmented pharmaceutical dosage forms
  申请人：Triastek, Inc.

  公开号：US10363220B2

  公开（公告）日：2019-07-30

  The present disclosure provides a stable solid pharmaceutical dosage form for oral administration. The dosage form includes a substrate that forms at least one compartment and a drug content loaded into the compartment. The dosage form is so designed that the active pharmaceutical ingredient of the drug content is released in a controlled manner.

  本公开提供了一种用于口服的稳定固体药物剂型。该剂型包括至少形成一个小室的基质和装入小室的药物成分。该剂型的设计使药物内容物中的活性药物成分以可控方式释放。
• Longer-acting progestin prodrug contraceptives
  申请人：Evestra, Inc.

  公开号：US10624903B2

  公开（公告）日：2020-04-21

  Described herein are progestin compounds that have extended release rates and that can be used without an estrogen to produce a contraceptive state.

  本文所述的孕激素化合物具有延长释放率的特点，可以在不使用雌激素的情况下产生避孕效果。