N-methyl-2,3-bis[(9Z,12Z)-octadeca-9,12-dienoxy]propan-1-amine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-methyl-2,3-bis[(9Z,12Z)-octadeca-9,12-dienoxy]propan-1-amine
• 化学式: C₄₀H₇₅NO₂
• 分子量: 602.0
• InChiKey: YCTDTEWPGCDATF-QYCRHRGJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  14
• 重原子数：
  43
• 可旋转键数：
  35
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  30.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• CATIONIC LIPID
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：US20150174261A1

  公开（公告）日：2015-06-25

  Provided are a cationic lipid which facilitates the introduction of a nucleic acid into, for example, a cell or the like; a composition containing the cationic lipid and a nucleic acid; a method for introducing a nucleic acid into a cell by using a composition containing the cationic lipid and the nucleic acid; and the like. The cationic lipid is, for example, a cationic lipid represented by formula (A): formula (A): (wherein R 1 is alkenyl or the like, R 2 is alkenyl or the like, R 3 and R 4 are each alkyl, or are combined together to form alkylene, or R 3 and R 5 are combined together to form alkylene, R 5 is a hydrogen atom or the like, or is combined together with R 3 to form alkylene, X 1 is alkylene, and X 2 is a single bond or alkylene).

  提供了一种阳离子脂质，可促进核酸（例如，细胞或类似物质）的引入；一种含有该阳离子脂质和核酸的组合物；通过使用含有该阳离子脂质和核酸的组合物将核酸引入细胞的方法；等等。该阳离子脂质是例如由式(A)表示的阳离子脂质：式(A)：（其中，R1是烯基或类似物，R2是烯基或类似物，R3和R4分别是烷基，或结合在一起形成亚烷基，或R3和R5结合在一起形成亚烷基，R5是氢原子或类似物，或与R3结合在一起形成亚烷基，X1是烷基，X2是单键或烷基）。
• 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。
• COMPOSITIONS AND METHODS FOR DELIVERING MESSENGER RNA
  申请人：Arbutus Biopharma Corporation

  公开号：EP3677567A1

  公开（公告）日：2020-07-08

  The present invention provides compositions comprising mRNA molecules encapsulated within lipid particles. The lipid particles comprise a cationic lipid, a non-cationic lipid, and an mRNA molecule that is encapsulated within the lipid particle. The compositions are useful, for example, to introduce the mRNA molecules into a human subject where they are translated to produce a polypeptide that functions to ameliorate one or more symptoms of a disease. The invention also provides cationic lipids that are useful for preparing the compositions of the invention.

  本发明提供了包含封装在脂质颗粒内的 mRNA 分子的组合物。脂质颗粒包括阳离子脂质、非阳离子脂质和封装在脂质颗粒内的 mRNA 分子。这些组合物可用于将 mRNA 分子导入人体，在人体中翻译产生多肽，从而改善疾病的一种或多种症状。本发明还提供了可用于制备本发明组合物的阳离子脂质。
• Cationic lipid
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：US10342758B2

  公开（公告）日：2019-07-09

  Provided are a cationic lipid which facilitates the introduction of a nucleic acid into, for example, a cell or the like; a composition containing the cationic lipid and a nucleic acid; a method for introducing a nucleic acid into a cell by using a composition containing the cationic lipid and the nucleic acid; and the like. The cationic lipid is, for example, a cationic lipid represented by formula (A): formula (A): (wherein R1 is alkenyl or the like, R2 is alkenyl or the like, R3 and R4 are each alkyl, or are combined together to form alkylene, or R3 and R5 are combined together to form alkylene, R5 is a hydrogen atom or the like, or is combined together with R3 to form alkylene, X1 is alkylene, and X2 is a single bond or alkylene).

  本文提供了一种有助于将核酸导入细胞等的阳离子脂质；一种含有该阳离子脂质和核酸的组合物；一种通过使用含有该阳离子脂质和核酸的组合物将核酸导入细胞的方法等。例如，阳离子脂质是由式（A）表示的阳离子脂质： 式（A）： (其中 R1 是烯基或类似物，R2 是烯基或类似物，R3 和 R4 各自是烷基，或结合在一起形成亚烷基，或 R3 和 R5 结合在一起形成亚烷基，R5 是氢原子或类似物，或与 R3 结合在一起形成亚烷基，X1 是亚烷基，X2 是单键或亚烷基）。