2,4-噻唑烷二酮,5-[[4-[2-(甲基-2-吡啶基氨基)乙氧基]苯基]甲基]-,(5R)- | 163860-16-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: 2,4-噻唑烷二酮,5-[[4-[2-(甲基-2-吡啶基氨基)乙氧基]苯基]甲基]-,(5R)-
• 英文名称: (+)-Rosiglitazone
• 英文别名: rosiglitazone；(5R)-5-{4-[(methyl-pyridin-2-yl-amino)-ethoxy]-benzyl}-thiazolidine-2,4-dione；(5R)-5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
• CAS: 163860-16-0
• 化学式: C₁₈H₁₉N₃O₃S
• 分子量: 357.433
• InChiKey: YASAKCUCGLMORW-OAHLLOKOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  25
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  96.8
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  罗格列酮 生成 2,4-噻唑烷二酮,5-[[4-[2-(甲基-2-吡啶基氨基)乙氧基]苯基]甲基]-,(5R)-
  参考文献：
  名称：

  Differential activity of rosiglitazone enantiomers at PPARγ

  摘要：

  Analysis of the enantiomers of rosiglitazone in a PPAR gamma binding assay suggests that the (S)-(-)isomer is responsible for the antidiabetic activity. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00664-7

文献信息

• METHODS AND SYSTEMS FOR DESIGNING AND/OR CHARACTERIZING SOLUBLE LIPIDATED LIGAND AGENTS
  申请人：TUFTS MEDICAL CENTER

  公开号：US20160052982A1

  公开（公告）日：2016-02-25

  The present application provides methods for preparing soluble lipidated ligand agents comprising a ligand entity and a lipid entity, and in some embodiments, provides relevant parameters of each of these components, thereby enabling appropriate selection of components to assemble active agents for any given target of interest.

  本申请提供了制备可溶性脂质化配体药剂的方法，包括配体实体和脂质实体，并在某些实施例中提供了这些组分的相关参数，从而使得能够适当选择组分来组装出针对任何感兴趣的靶点的活性药剂。
• RESPIRATORY DISEASE TREATMENT
  申请人：Finch Harry

  公开号：US20110053986A1

  公开（公告）日：2011-03-03

  There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and/or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and kit.

  提供了一种适用于肺部吸入的药物组合物，该组合物包括一种格列吡嗪，例如派格列酮或罗格列酮，以及一种或多种药用载体和/或赋形剂，其中该组合物的格列吡嗪含量由至少95%的5R对映体和少于5%的5S对映体组成。还提供了使用和工具包。
• Respiratory Disease Treatment
  申请人：FINCH Harry

  公开号：US20120264787A1

  公开（公告）日：2012-10-18

  There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and/or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and kit.

  提供了一种适用于通过吸入进行肺部给药的制剂，该制剂包括一种glitazone，例如pioglitazone或rosiglitazone，以及一种或多种药学上可接受的载体和/或赋形剂，其中该制剂中的glitazone含量由至少95%的5R对映体和少于5%的5S对映体组成。还提供了一种用途和工具包。
• Methods and systems for designing and/or characterizing soluble lipidated ligand agents
  申请人：Tufts Medical Center

  公开号：US10233219B2

  公开（公告）日：2019-03-19

  The present application provides methods for preparing soluble lipidated ligand agents comprising a ligand entity and a lipid entity, and in some embodiments, provides relevant parameters of each of these components, thereby enabling appropriate selection of components to assemble active agents for any given target of interest.

  本申请提供了制备由配体实体和脂质实体组成的可溶性脂质配体制剂的方法，在某些实施方案中，还提供了这些成分中每种成分的相关参数，从而能够适当选择成分，为任何给定的感兴趣的靶标组装活性制剂。
• Cantello, Barrie C. C.; Eggleston, Drake S.; Haigh, David, Journal of the Chemical Society. Perkin transactions I, 1994, # 22, p. 3319 - 3324
  作者：Cantello, Barrie C. C.、Eggleston, Drake S.、Haigh, David、Haltiwanger, R. Curtis、Heath, Catherine M.、et al.

  DOI：——

  日期：——