2,2-dilinoleyl-4-N-morpholino-[1,3]-dioxane | 1217306-42-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2,2-dilinoleyl-4-N-morpholino-[1,3]-dioxane
• 英文别名: 4-[[2,2-bis[(9Z,12Z)-octadeca-9,12-dienyl]-1,3-dioxolan-4-yl]methyl]morpholine
• CAS: 1217306-42-7
• 化学式: C₄₄H₇₉NO₃
• 分子量: 670.116
• InChiKey: GYFBQQOJZSBBEL-MAZCIEHSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  14.9
• 重原子数：
  48
• 可旋转键数：
  32
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  30.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  吗啉 、 2,2-dilinoleyl-4-bromomethyl-[1,3]-dioxolane 在 potassium carbonate 作用下， 以 乙腈 为溶剂， 生成 2,2-dilinoleyl-4-N-morpholino-[1,3]-dioxane
  参考文献：
  名称：

  [EN] IMPROVED AMINO LIPIDS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS
  [FR] LIPIDES AMINÉS AMÉLIORÉS ET PROCÉDÉS D'ADMINISTRATION D'ACIDES NUCLÉIQUES

  摘要：

  本发明提供了用于将治疗剂传递给细胞的优越组合物和方法。具体来说，这些包括新型脂质和核酸-脂质颗粒，能够有效地封装核酸并有效地将封装的核酸传递给体内的细胞。本发明的组合物具有高度的效力，因此可以以相对较低的剂量有效地降低特定靶蛋白的表达。此外，本发明的组合物和方法与先前在艺术领域中已知的组合物和方法相比，毒性更低，并提供更大的治疗指数。

  公开号：

  WO2010042877A1

文献信息

• AMINO LIPIDS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS
  申请人：Hope Michael J.

  公开号：US20110256175A1

  公开（公告）日：2011-10-20

  The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

  本发明提供了优越的组合物和方法，用于将治疗剂传递到细胞。特别是，这些包括新型脂质和核酸-脂质颗粒，可有效地封装核酸，并将封装的核酸高效地传递到体内的细胞中。本发明的组合物具有高度的效力，因此可以在相对较低的剂量下有效地敲低特定靶蛋白。此外，本发明的组合物和方法与先前已知的组合物和方法相比，毒性更小，提供更大的治疗指数。
• Improved amino lipids and methods for the delivery of nucleic acids
  申请人：Tekmira Pharmaceuticals Corporation

  公开号：EP2743265A1

  公开（公告）日：2014-06-18

  The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipid having the structure below and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

  本发明提供了向细胞输送治疗剂的优良组合物和方法。其中特别包括具有以下结构的新型脂质和核酸-脂质颗粒，它们能有效地封装核酸并在体内将封装的核酸高效地输送到细胞中。本发明的组合物具有很高的效力，因此能以相对较低的剂量有效地敲除特定的靶蛋白。此外，与本领域以前已知的组合物和方法相比，本发明的组合物和方法毒性更低，治疗指数更高。
• IMPROVED AMINO LIPIDS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS
  申请人：Arbutus Biopharma Corporation

  公开号：EP3225621A1

  公开（公告）日：2017-10-04

  The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

  本发明提供了向细胞输送治疗剂的优良组合物和方法。其中特别包括新型脂质和核酸-脂质颗粒，它们能有效封装核酸，并在体内将封装的核酸高效递送至细胞。本发明的组合物具有很高的效力，因此能以相对较低的剂量有效地敲除特定的靶蛋白。此外，与本领域以前已知的组合物和方法相比，本发明的组合物和方法毒性更低，治疗指数更高。
• Amino lipids and methods for the delivery of nucleic acids
  申请人：ARBUTUS BIOPHARMA CORPORATION

  公开号：US10653780B2

  公开（公告）日：2020-05-19

  The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

  本发明提供了向细胞输送治疗剂的优良组合物和方法。其中特别包括新型脂质和核酸-脂质颗粒，它们能有效封装核酸，并在体内将封装的核酸高效递送至细胞。本发明的组合物具有很高的效力，因此能以相对较低的剂量有效地敲除特定的靶蛋白。此外，与本领域以前已知的组合物和方法相比，本发明的组合物和方法毒性更低，治疗指数更高。
• US9139554B2
  申请人：——

  公开号：US9139554B2

  公开（公告）日：2015-09-22