(-)-Rosiglitazone | 163860-15-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: (-)-Rosiglitazone
• 英文别名: (5S)-5-{4-[(methyl-pyridin-2-yl-amino)-ethoxy]-benzyl}-thiazolidine-2,4-dione；Rosiglitazone, (S)-；(5S)-5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
• CAS: 163860-15-9
• 化学式: C₁₈H₁₉N₃O₃S
• mdl: MFCD00871760
• 分子量: 357.433
• InChiKey: YASAKCUCGLMORW-HNNXBMFYSA-N

物化性质

• 沸点：
  585.0±35.0 °C(Predicted)
• 密度：
  1.315±0.06 g/cm3(Predicted)

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 (-)-Rosiglitazone
  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

• MODIFICATIONS OF THERAPEUTIC AGENTS FOR ENHANCED DELIVERY TO TARGET SITES
  申请人：Partikula LLC

  公开号：US20180028647A1

  公开（公告）日：2018-02-01

  Compositions of a modulator of cell metabolism, typically targeting cellular glycolysis, preferably with a targeting moiety, attached directly or indirectly to the inhibitor, or to a nanoparticle or other delivery vehicle thereof, and methods of use for treating cancer, proliferative disorders, neurodegenerative diseases, autoimmune disorders, or inflammatory diseases are provided. Pharmaceutical compositions including the targeted modulator and a pharmaceutically acceptable carrier are also provided. The pharmaceutical compositions can be administered to a subject in need thereof in an effective amount to reduce one or symptoms of the cancer, proliferative disorders, neurodegenerative diseases, autoimmune disorders, or inflammatory diseases alone or prior to or in conjunction with a further therapy such as radiotherapy.

  提供了细胞代谢调节剂的组成，通常以靶向细胞糖酵解为目标，最好带有一个靶向基团，直接或间接连接到抑制剂，或连接到纳米颗粒或其他递送载体上，并提供了用于治疗癌症、增生性疾病、神经退行性疾病、自身免疫性疾病或炎症性疾病的方法。还提供了包括靶向调节剂和药学上可接受的载体的药物组合物。这些药物组合物可以以有效剂量给需要的受试者使用，以减少癌症、增生性疾病、神经退行性疾病、自身免疫性疾病或炎症性疾病的症状之一或多个，独立使用或在放疗等进一步治疗之前或同时使用。
• COMPOSITION FOR TREATING ATHEROSCLEROSIS AND A PREPARATION METHOD THEREOF
  申请人：WU YANG-CHANG

  公开号：US20130040996A1

  公开（公告）日：2013-02-14

  Disclosed are a composition for preventing and treating atherosclerosis which includes chalcone compound. In particular, the chalcone compound bound with 2-hydroxyl in ring A and 4′-methyoxy in ring B has versatile therapeutic potentials on anti-atherosclerosis by acting as PPARγ inducer, p44/42 MAPK inhibitor and cell cycle blocker and does not show toxicity to human aortic smooth muscle cells (HASMCs). In addition, the chalcone compound exhibits synergistic effect with the PPARγ ligand (rosiglitazone) to inhibit cell proliferation and the upregulation of cyclin D1, cyclin D3, interleukin-1β (IL-1β) and interleukin-6 (IL-6) induced by oxidized low density lipoprotein (Ox-LDL).

  本发明涉及一种用于预防和治疗动脉粥样硬化的组合物，其中包括查尔酮化合物。特别地，环A中与2-羟基结合，环B中与4'-甲氧基结合的查尔酮化合物具有多种治疗潜力，可作为PPARγ诱导剂、p44/42 MAPK抑制剂和细胞周期阻滞剂，且不对人体主动脉平滑肌细胞（HASMCs）显示毒性。此外，查尔酮化合物与PPARγ配体（罗格列酮）表现出协同作用，可抑制由氧化低密度脂蛋白（Ox-LDL）诱导的细胞增殖和cyclin D1、cyclin D3、白细胞介素-1β（IL-1β）和白细胞介素-6（IL-6）上调。
• 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。
• SYNERGISTIC COMPOSITIONS
  申请人：CADILA HEALTHCARE LIMITED

  公开号：US20160068484A1

  公开（公告）日：2016-03-10

  The present invention describes a synergistic composition comprising of one or more statins, or one or more dipeptidyl peptidase IV (DPP IV) inhibitor or one or more biguanide antihyperglycaemic agent and a PPAR agonist of formula (Ia) for the treatment of diabetes, especially non-insulin dependent diabetes (NIDDM) or Type 2 diabetes and conditions associated with diabetes mellitus and to compositions suitable for use in such method. The invention also describes the preparation of such compositions. The present invention also relates to certain novel salts of the PPAR agonist of formula (I): processes for the preparation of these novel salts and use thereof.

  本发明涉及一种协同作用组合物，包括一种或多种他汀类药物、一种或多种二肽基肽酶IV（DPP IV）抑制剂或一种或多种双胍类降糖药物以及一种公式（Ia）的PPAR激动剂，用于治疗糖尿病，特别是非胰岛素依赖性糖尿病（NIDDM）或2型糖尿病以及与糖尿病相关的疾病，以及适用于此类方法的组合物。本发明还描述了这种组合物的制备方法。本发明还涉及公式（I）的PPAR激动剂的某些新型盐：制备这些新型盐的方法及其用途。