Ethyl 4-acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Ethyl 4-acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylate
• 化学式: C₁₆H₂₈N₂O₄
• 分子量: 312.4
• InChiKey: VSZGPKBBMSAYNT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  22
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  90.6
• 氢给体数：
  2
• 氢受体数：
  5

ADMET

毒理性

• 在妊娠和哺乳期间的影响

乳哺期间使用总结：有限的数据表明，奥司他韦及其活性代谢物很少排入母乳。母亲每日剂量为150毫克，在乳汁中产生的水平较低，预计不会对哺乳婴儿造成任何不良反应。超过2周大的婴儿可以直接接受奥司他韦，剂量远大于母乳中的剂量。 对哺乳婴儿的影响：截至修订日期，没有找到相关的已发布信息。 对泌乳和母乳的影响：截至修订日期，没有找到相关的已发布信息。

◉ Summary of Use during Lactation:Limited data indicate that oseltamivir and its active metabolite are poorly excreted into breastmilk. Maternal dosages of 150 mg daily produce low levels in milk and would not be expected to cause any adverse effects in breastfed infants. Infants over 2 weeks of age can receive oseltamivir directly in doses much larger than those in breastmilk. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

文献信息

• Labeled substrate conjugates for identifying enzyme inhibitors
  申请人：Ying Laiqiang

  公开号：US20060057658A1

  公开（公告）日：2006-03-16

  This invention provides labeled-substrate conjugates for assaying enzymes, particularly neuraminidases. Also provided are assays that are useful for identifying compounds that inhibit sialyltransferases or neuraminidases and may be useful in treating subjects with influenza. In particular, the present invention relates to methods of using such labeled substrate conjugates to screen for enzyme inhibitors, particularly in a high-throughput format.

  本发明提供了用于测定酶的标记底物结合物，特别是神经氨酸酶。还提供了用于鉴定抑制唾液酸转移酶或神经氨酸酶的化合物的测定方法，并可用于治疗患有流感的受试者。特别是，本发明涉及使用这种标记底物结合物在高通量格式中筛选酶抑制剂的方法。
• POST-EXPOSURE THERAPY OF INFLUENZA A INFECTIONS
  申请人：Wong Jonathan P.

  公开号：US20120195960A1

  公开（公告）日：2012-08-02

  Poly ICLC or liposome-encapsulated Poly ICLC (LE Poly ICLC) in combination with antisense oligonucleotides (AS) act synergistically in post-exposure prophylaxis or therapy of influenza infections, especially H5N1 virus infections.
• ORALLY-DISINTEGRATING OSELTAMIVIR TABLET AND METHOD FOR PREPARING THE SAME
  申请人：Zhongshuai Pharmaceutical Sci & Tech Incorporated Co., Ltd.

  公开号：US20160120802A1

  公开（公告）日：2016-05-05

  An orally-disintegrating oseltamivir tablet, including: between 10 and 50 wt. % of a taste-masking pellet, between 30 and 80 wt. % of a first filler, between 1 and 6 wt. % of a first adhesive, between 2 and 10 wt. % of a disintegrant, between 0 and 5 wt. % of a flavoring agent, between 0.5 and 2.5 wt. % of a lubricant. The taste-masking pellet includes: an active ingredient-loaded pellet core and a coating layer. The active ingredient of the pellet core is oseltamivir or a pharmaceutically acceptable salt of oseltamivir and accounts for between 10 and 40 wt. % of a total weight of the taste-masking pellet. The coating layer include a polyacrylic acid resin IV and accounts for between 1 and 50 wt. % of the total weight of the taste-masking pellet. The diameter of the taste-masking pellet is between 0.10 and 0.50 mm.
• ORAL PHARMACEUTICAL COMPOSITION COMPRISING OSELTAMIVIR AND METHOD OF PREPARING THE SAME
  申请人：Zhongshuai Pharmaceutical Sci & Tech Incorporated Co., Ltd.

  公开号：US20160120820A1

  公开（公告）日：2016-05-05

  A pharmaceutical composition, including: an active ingredient-loaded pellet core and a coating layer. The active ingredient of the pellet core is oseltamivir or a pharmaceutically acceptable salt thereof. The active ingredient accounts for between 10 and 40 wt. % of the total weight of the pharmaceutical composition. The coating layer includes a polyacrylic acid resin IV and accounts for between 1 and 50 wt. % of the total weight of the pharmaceutical composition. The pharmaceutical composition has a diameter of between 0.10 and 0.50 mm.
• PHARMACEUTICAL COMPOSITIONS COMPRISING DANIRIXIN FOR TREATING INFECTIOUS DISEASES
  申请人：GlaxoSmithKline Intellectual Property (No. 2) Limited

  公开号：US20170100385A1

  公开（公告）日：2017-04-13

  Provided are compounds and pharmaceutically acceptable salts thereof, and combinations of compounds, their pharmaceutical compositions, their methods of preparation, and methods for their use in treating or preventing infectious disease.