二十碳六烯酸-4,8,12,16-四乙酸 | 106868-37-5

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 中文名称: 二十碳六烯酸-4,8,12,16-四乙酸
• 英文名称: eicosa-4,8,12,16-tetraenoic acid
• 英文别名: Eicosa-4,8,12,16-tetraensaeure；4,8,12,16-Eicosatetraenoic acid；(4E,8E,12E,16E)-icosa-4,8,12,16-tetraenoic acid
• CAS: 106868-37-5
• 化学式: C₂₀H₃₂O₂
• 分子量: 304.473
• InChiKey: QSMHRTSIMKYDTO-FFIJXKSSSA-N

物化性质

• 沸点：
  439.6±24.0 °C(Predicted)
• 密度：
  0.928±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.7
• 重原子数：
  22
• 可旋转键数：
  14
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  二十碳六烯酸-4,8,12,16-四乙酸 在 乙醚 、 溴 作用下， 生成 4,5,8,9,12,13,16,17-octabromo-eicosanoic acid
  参考文献：
  名称：

  Toyama; Tsuchiya, Bulletin of the Chemical Society of Japan, 1935, vol. 10, p. 243,297

  摘要：

  DOI：

文献信息

• Cationic cardiolipin analoges and its use thereof
  申请人：Ahmad U. Moghis

  公开号：US20050277611A1

  公开（公告）日：2005-12-15

  The invention provides cationic cardiolipin compounds, and methods for synthesizing and using them in liposomal formulation, gene transfection, etc. In particular, the invention provides liposomes comprising cationic cardiolipin analog, pharmaceutical compositions comprising cationic cardiolipin analogs, and methods of using such liposomes and compositions, in delivering active pharmaceutical agents to treat human and animal diseases and/or in diagnostic assays.

  本发明提供了阳离子心磷脂化合物以及其合成和在脂质体制剂、基因转染等方面的使用方法。特别地，本发明提供了含阳离子心磷脂类似物的脂质体、含阳离子心磷脂类似物的药物组合物以及使用这些脂质体和组合物的方法，用于传递活性药物治疗人类和动物疾病和/或诊断测定。
• Cardiolipin molecules and methods of synthesis
  申请人：Ahmad U. Moghis

  公开号：US20050266068A1

  公开（公告）日：2005-12-01

  The invention provides new synthetic routes for cardiolipin with different fatty acids and/or alkyl chains with varying chain length and also with or without unsaturation, particularly a short-chain cardiolipin. The methods comprise reacting a 1,2-O-sn-diacyl/1,2-O-sn-dialkyl glycerol or a 2-O-protected glycerol, with a phosphoramidite reagent or a phosphate triester to produce a protected cardiolipin, which is deprotected to prepare the short chain cardiolipin. The reaction schemes can be used to generate new variants of cardiolipin. The cardiolipin prepared by the present methods can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays. Liposomes can also include ligands for targeting a particular cell type or specific tissue.

  本发明提供了一种合成不同脂肪酸和/或不同链长烷基的心磷脂的新合成路线，以及具有或不具有不饱和度，特别是一种短链心磷脂。该方法包括将1,2-O-sn-二酰基/1,2-O-sn-二烷基甘油或2-O-保护甘油与磷酸酰胺试剂或磷酸三酯反应以产生受保护的心磷脂，然后去保护以制备短链心磷脂。该反应方案可用于生成心磷脂的新变体。通过本方法制备的心磷脂可以被纳入到脂质体中，这些脂质体还可以包括疏水性或亲水性药物等活性剂。这样的脂质体可以用于治疗疾病或在诊断和/或分析检测中使用。脂质体还可以包括用于靶向特定细胞类型或特定组织的配体。
• Cardiolipin compositions their methods of preparation and use
  申请人：Ahmad U. Moghis

  公开号：US20050181037A1

  公开（公告）日：2005-08-18

  The invention provides new synthetic routes for cardiolipin with different fatty acids and/or alkyl chains with varying chain length and also with or without unsaturation. The reaction schemes can be used to generate new forms of cardiolipin, including cardiolipin variants. The cardiolipin prepared by the present methods can conveniently be incorporated into liposomes and other lipid formulations that can also include active agents such as hydrophobic or hydrophilic drugs. Such formulations can be used to treat diseases or in diagnostic and/or analytical assays. Liposomes also can include ligands, e.g., for targeting them to a cell type or specific tissue.

  本发明提供了一种用于合成不同脂肪酸和/或不同碳链长度以及有或没有不饱和度的磷脂酰肌醇的新合成路线。反应方案可用于生成新形式的磷脂酰肌醇，包括磷脂酰肌醇变异体。通过本方法制备的磷脂酰肌醇可以方便地被纳入脂质体和其他脂质制剂中，这些制剂也可以包括疏水性或亲水性药物等活性剂。这样的制剂可用于治疗疾病或在诊断和/或分析测定中使用。脂质体还可以包括配体，例如用于将其定向到特定细胞类型或组织的配体。
• Enzyme formation suppressing agent
  申请人：KABUSHIKI KAISHA HAYASHIBARA SEIBUTSU KAGAKU KENKYUJO

  公开号：EP0345082A2

  公开（公告）日：1989-12-06

  The present invention relates to a pharmaceutical agent to suppress the formation of an enzyme, more particularly, to an entirely novel pharmaceutical agent which does not inhibit the action or activity of tyrosinase which has been formed, but prevents its formation. The pharmaceutical agent comprises one or more members selected from the group consisting of acetic acid, lactic acid, pyruvic acid, and their salts and derivatives as the effective component.

  本发明涉及一种抑制酶的形成的药剂，更具体地说，涉及一种全新的药剂，它不抑制已形成的酪氨酸酶的作用或活性，而是防止其形成。该药剂包括从乙酸、乳酸、丙酮酸及其盐和衍生物组成的组中选出的一个或多个成员作为有效成分。
• Endoxifen compositions and methods
  申请人：Jina Pharmaceuticals, Inc.

  公开号：US10376479B2

  公开（公告）日：2019-08-13

  The present invention provides compositions containing endoxifen, formulations and liposomes of endoxifen, methods of preparation of such agents and formulations, and use of such agents and formulations for the treatment of breast cancer and other breast diseases and diseases susceptible to endoxifen. In particular, the compositions of the present invention include liposomes, complexes, vesicles, emulsions, micelles and mixed micelles of endoxifen in which the compositions further contain any of a variety of neutral or charged lipids and desirably, cholesterol and cholesterol derivatives, sterols, Z- and E-guggulsterones, phospholipids, fatty acids, vitamin D, and vitamin E. The present invention also provides methods of preparing endoxifen. The present invention provides methods for treating and preventing breast cancer and other breast related diseases by administrating novel formulations or compositions comprising a therapeutically effective amount of endoxifen.

  本发明提供了含有内酯昔芬的组合物、内酯昔芬的制剂和脂质体、制备此类制剂和制剂的方法，以及使用此类制剂和制剂治疗乳腺癌和其他乳腺疾病以及易受内酯昔芬影响的疾病。特别是，本发明的组合物包括内酯昔芬的脂质体、复合物、囊泡、乳液、胶束和混合胶束，其中组合物进一步含有各种中性或带电脂质中的任何一种，最好是胆固醇和胆固醇衍生物、甾醇、Z-和E-古杉甾酮、磷脂、脂肪酸、维生素D和维生素E。本发明提供了通过施用包含治疗有效量的内昔芬的新型制剂或组合物来治疗和预防乳腺癌及其他乳腺相关疾病的方法。