弗拉沃迪酸 | 37470-13-6

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 中文名称: 弗拉沃迪酸
• 英文名称: 5,7-di-O-carboxymethyl chrysin
• 英文别名: Flavodic Acid；2-[5-(carboxymethoxy)-4-oxo-2-phenylchromen-7-yl]oxyacetic acid
• CAS: 37470-13-6
• 化学式: C₁₉H₁₄O₈
• mdl: MFCD00707892
• 分子量: 370.315
• InChiKey: IGCSSLDDCHLXGL-UHFFFAOYSA-N

物化性质

• 沸点：
  670.6±55.0 °C(Predicted)
• 密度：
  1.483±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  119
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  白杨素 在 甲醇 、 potassium carbonate 、 potassium hydroxide 作用下， 以 丙酮 为溶剂， 反应 10.0h， 生成 弗拉沃迪酸
  参考文献：
  名称：

  Synthesis and antitumor activity evaluation of chrysin derivatives

  摘要：

  A series of 5,7-disubstituted chrysin, 7-monosubstituted chrysin, 5-monosubstituted chrysin derivatives were synthesized by alkylation, acetylation, benzoylation, carboxymethylation, and evaluated on their antitumor activity of H22 cells in the search for potential antitumor agents. Among them, compound 3 (5,7-diacetyl chrysin) displayed the most potent antitumor activity with IC50 value of 141 mu M. Moreover, there is significant up-regulation of G2 in cell cycle of H22. (C) 2014 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2013.12.044

文献信息

• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• PHARMACEUTICAL COMPOSITION COMBINING VARIOUS VENOTONIC AND VASOPROTECTIVE AGENTS FOR THE TREATMENT OF CHRONIC VENOUS INSUFFICIENCY
  申请人：World Trade Import-Export, WTIE A.G.

  公开号：EP2208498A1

  公开（公告）日：2010-07-21

  The invention relates to a pharmaceutical composition comprising the synergic combination of three agents with venotonic and vasoprotective activity, known as a purified, micronized flavonoid fraction of diosmin and hesperidin and calcium dobesilate, as well as pharmaceutically acceptable excipients, which are formulated in a single dosage unit to be orally administered. The composition, which is used to control and treat chronic venous insufficiency, provides improved therapeutic effect and faster pharmacological action in less time, with smaller concentrations of the active principles and a reduction in the risk of severe complications and/or side effects.

  本发明涉及一种药物组合物，该组合物由三种具有静脉舒张和血管保护活性的制剂协同组合而成，这三种制剂被称为地奥司明和橙皮甙的纯化、微粉化黄酮组分和多贝西酸钙，以及药学上可接受的赋形剂，它们被配制在一个剂量单位中口服给药。该组合物用于控制和治疗慢性静脉功能不全，能在更短的时间内提高疗效和加快药理作用，活性成分的浓度更低，并能降低严重并发症和/或副作用的风险。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• LYOPHILIZATION PROCESS AND PRODUCTS OBTAINED THEREBY
  申请人：Scidose, Llc

  公开号：EP1954244A1

  公开（公告）日：2008-08-13
• CONTROLLED ABSORPTION WATER-SOLUBLE PHARMACEUTICALLY ACTIVE ORGANIC COMPOUND FORMULATION FOR ONCE-DAILY ADMINISTRATION
  申请人：STI Pharma, LLC

  公开号：EP2717860A1

  公开（公告）日：2014-04-16