1,2-dilinoleyloxy-3-(4'-hydroxypiperidino)propylamine | 1260142-12-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1,2-dilinoleyloxy-3-(4'-hydroxypiperidino)propylamine
• 英文别名: 1-[2,3-bis[(9Z,12Z)-octadeca-9,12-dienoxy]propyl]piperidin-4-ol
• CAS: 1260142-12-8
• 化学式: C₄₄H₈₁NO₃
• 分子量: 672.132
• InChiKey: ZVWXSBHUQQKHMJ-MAZCIEHSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  14.3
• 重原子数：
  48
• 可旋转键数：
  35
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  41.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  亚油醇甲基磺酸酯 在 四(三苯基膦)钯 四丁基硫酸氢铵 、 三乙胺 、 三氟乙酸 作用下， 以 乙醇 、 二氯甲烷 、 甲苯 为溶剂， 反应 49.08h， 生成 1,2-dilinoleyloxy-3-(4'-hydroxypiperidino)propylamine
  参考文献：
  名称：

  [EN] IMPROVED CATIONIC LIPIDS AND METHODS FOR THE DELIVERY OF THERAPEUTIC AGENTS
  [FR] LIPIDES CATIONIQUES ET PROCÉDÉS AMÉLIORÉS POUR L'ADMINISTRATION D'AGENTS THÉRAPEUTIQUES

  摘要：

  本发明提供了用于将治疗剂传递到细胞的组合物和方法。具体包括新型阳离子脂质和核酸-脂质颗粒，它们能够有效地封装核酸并将封装的核酸有效地传递到体内的细胞中。本发明的组合物具有很高的效力，因此可以在相对较低的剂量下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已知的组合物和方法相比，毒性较低，提供更高的治疗指数。

  公开号：

  WO2011000106A1

文献信息

• COMPOSITIONS AND METHODS FOR SILENCING APOLIPOPROTEIN B
  申请人：Lee Amy C.H.

  公开号：US20110195127A1

  公开（公告）日：2011-08-11

  The present invention provides compositions and methods for the delivery of interfering RNAs that silence APOB expression to liver cells. In particular, the nucleic acid-lipid particles 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 APOB 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.

  本发明提供了一种递送干扰RNA以沉默APOB表达至肝细胞的组合物和方法。具体来说，核酸-脂质颗粒有效地封装核酸并有效地将封装的核酸递送至体内的细胞。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降低APOB的表达。此外，本发明的组合物和方法与先前已知的技术相比，毒性更低，并提供了更大的治疗指数。
• COMPOSITIONS AND METHODS FOR SILENCING EBOLA VIRUS GENE EXPRESSION
  申请人：Geisbert Thomas W.

  公开号：US20110201667A1

  公开（公告）日：2011-08-18

  The present invention provides compositions comprising therapeutic nucleic acids (e.g., interfering RNA such as siRNA) that target Ebola virus (EBOV) gene expression and methods of using such compositions to silence EBOV gene expression. More particularly, the invention provides unmodified and chemically modified interfering RNA which silence EBOV gene expression and methods of use thereof, e.g., for preventing or treating EBOV infections caused by one or more EBOV species such as Zaire EBOV. The invention also provides serum-stable nucleic acid-lipid particles comprising one or more interfering RNA molecules, a cationic lipid, and a non-cationic lipid, which can further comprise a conjugated lipid that inhibits aggregation of particles. Methods of silencing EBOV gene expression by administering one or more interfering RNA molecules to a mammalian subject are also provided.

  本发明提供了包含治疗性核酸（例如干扰RNA，如siRNA）的组合物，这些核酸靶向埃博拉病毒（EBOV）基因表达，并提供使用这些组合物来沉默EBOV基因表达的方法。更具体地，本发明提供了未经修饰和化学修饰的干扰RNA，这些RNA可以沉默EBOV基因表达，并提供了这些方法的使用，例如，用于预防或治疗由一个或多个EBOV种类（如扎伊尔EBOV）引起的EBOV感染。本发明还提供了包含一个或多个干扰RNA分子、一个阳离子脂质和一个非阳离子脂质的血清稳定的核酸脂质颗粒，该颗粒可以进一步包含抑制颗粒聚集的共轭脂质。还提供了通过向哺乳动物主体注射一个或多个干扰RNA分子来沉默EBOV基因表达的方法。
• NOVEL LIPID FORMULATIONS FOR DELIVERY OF THERAPEUTIC AGENTS TO SOLID TUMORS
  申请人：Yaworski Ed

  公开号：US20110076335A1

  公开（公告）日：2011-03-31

  The present invention provides novel, serum-stable lipid particles comprising one or more active agents or therapeutic agents, methods of making the lipid particles, and methods of delivering and/or administering the lipid particles. More particularly, the present invention provides serum-stable nucleic acid-lipid particles (SNALP) comprising a nucleic acid (e.g., one or more interfering RNA molecules), methods of making the SNALP, and methods of delivering and/or administering the SNALP (e.g., for the treatment of cancer). In particular embodiments, the present invention provides tumor-directed lipid particles that preferentially target solid tumors. The tumor-directed formulations of the present invention are capable of preferentially delivering a payload such as a nucleic acid to cells of solid tumors compared to non-cancerous cells.

  本发明提供了新型的血清稳定脂质粒子，包括一种或多种活性剂或治疗剂，制备脂质粒子的方法以及传递和/或管理脂质粒子的方法。更具体地，本发明提供了血清稳定的核酸脂质粒子（SNALP），包括核酸（例如一种或多种干扰RNA分子），制备SNALP的方法，以及传递和/或管理SNALP的方法（例如用于癌症治疗）。在特定实施例中，本发明提供了针对实体肿瘤的肿瘤定向脂质粒子。本发明的肿瘤定向配方能够优先将有效载荷如核酸传递到实体肿瘤细胞，而不是非癌细胞。
• CATIONIC LIPIDS AND METHODS FOR THE DELIVERY OF THERAPEUTIC AGENTS
  申请人：Heyes James

  公开号：US20120202871A1

  公开（公告）日：2012-08-09

  The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic 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 a specific target protein 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.

  本发明提供了用于向细胞传递治疗剂的组合物和方法。特别地，这些包括新型阳离子脂质和核酸-脂质颗粒，它们提供了核酸的高效封装和封装核酸的高效递送到体内的细胞。本发明的组合物具有高度的效力，因此在相对较低的剂量下允许有效地抑制特定目标蛋白。此外，本发明的组合物和方法比先前已知的组合物和方法更少毒性并提供更大的治疗指数。
• SNALP FORMULATIONS CONTAINING ANTIOXIDANTS
  申请人：Yaworski Ed

  公开号：US20130022649A1

  公开（公告）日：2013-01-24

  The present invention provides methods of preventing, decreasing, or inhibiting the degradation of cationic lipids and/or active agents (e.g., therapeutic nucleic acids) present in lipid particles, compositions comprising lipid particles stabilized by these methods, methods of making these lipid particles, and methods of delivering and/or administering these lipid particles, e.g., for the treatment of a disease or disorder.