methyl ((9Z,12Z)-octadeca-9,12-dienyl)amine | 1098300-02-7

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: methyl ((9Z,12Z)-octadeca-9,12-dienyl)amine
• 英文别名: (9Z,12Z)-N-methyloctadeca-9,12-dien-1-amine；methyl((9Z,12Z)-octadeca-9,12-dienyl)amine
• CAS: 1098300-02-7
• 化学式: C₁₉H₃₇N
• 分子量: 279.509
• InChiKey: LAXQWOMQTPMYON-NQLNTKRDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7
• 重原子数：
  20
• 可旋转键数：
  15
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  methyl ((9Z,12Z)-octadeca-9,12-dienyl)amine 以 氯仿 、 甲苯 为溶剂， 反应 40.0h， 生成 (9Z,12Z)-N-methyl-(2-(pyridin-2-yldisulfaneyl)ethyl)octadeca-9,12-dien-1-amine
  参考文献：
  名称：

  [EN] IONIZABLE LIPIDS AND NANOPARTICLE COMPOSITIONS THEREOF
  [FR] LIPIDES IONISABLES ET COMPOSITIONS DE NANOPARTICULES ASSOCIÉES

  摘要：

  公开号：

  WO2021102411A8
• 作为产物：
  描述：

  亚油醇甲基磺酸酯 、 甲胺 以 四氢呋喃 为溶剂， 反应 1.5h， 生成 methyl ((9Z,12Z)-octadeca-9,12-dienyl)amine
  参考文献：
  名称：

  简化用于siRNA-脂质纳米颗粒的阳离子脂质的化学结构。

  摘要：

  我们报告了有效的阳离子脂质，SST-02（（3-羟丙基）二亚油胺），具有简单的化学结构，并且仅一步就合成了。阳离子脂质是siRNA-脂质纳米颗粒（LNP）的关键成分，可作为各种疾病的潜在治疗剂。十年来，化学家赋予阳离子脂质增强的功效和新功能以及结构复杂性。在这项研究中，我们进行了化学简单的药用化学研究，发现甚至二亚油基甲胺（SST-01）和甲基棕榈油胺也可以用于体内和体外siRNA递送。进一步的优化表明，羟基增强了效能，SST-02在VII因子（FVII）模型中显示的ID50为0.02 mg / kg。给予3 mg / kg SST-02 LNP的大鼠体重，血液化学或血液学参数无变化，而AST水平在5 mg / kg剂量下降低。SST-02的使用避免了冗长的合成路线，因此可以降低核酸治疗剂的未来成本。

  DOI：

  10.1021/acsmedchemlett.8b00652

文献信息

• LIPID NANO PARTICLES COMPRISING COMBINATION OF CATIONIC LIPID
  申请人：KYOWA HAKKO KIRIN CO., LTD.

  公开号：US20140045913A1

  公开（公告）日：2014-02-13

  The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) (wherein: R 1 and R 2 are, the same or different, alkenyl, etc, and X 3 is absent or is alkyl, etc, X 1 and X 2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and Y 1 is absent or anion, L 1 is a single bond, etc, R 3 is alkyl, etc), and a cationic lipid represented by formula (II) (wherein: R 4 and R 5 are, the same or different, alkenyl, etc, and X 4 and X 5 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X 6 is absent or is alkyl, etc, Y 2 is absent or anion, a and b are, the same or different, 0 to 3, and L 4 is a single bond, etc, R 6 is alkyl, etc, L 2 and L 3 are —O—, —CO—O— or —O—CO—), and the like.

  本发明提供了一种脂质纳米粒子，可以使核酸轻松地进入细胞，包括由式(I)表示的阳离子脂质（其中：R1和R2是相同或不同的烯基等，X3不存在或是烷基等，X1和X2是氢原子，或结合在一起形成单键或亚烷基，Y1不存在或是阴离子，L1是单键等，R3是烷基等），以及由式(II)表示的阳离子脂质（其中：R4和R5是相同或不同的烯基等，X4和X5是氢原子，或结合在一起形成单键或亚烷基，X6不存在或是烷基等，Y2不存在或是阴离子，a和b是相同或不同的0到3，L4是单键等，R6是烷基等，L2和L3是—O—，—CO—O—或—O—CO—）等。
• LIPID NANO PARTICLES COMPRISING CATIONIC LIPID FOR DRUG DELIVERY SYSTEM
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：US20140039032A1

  公开（公告）日：2014-02-06

  The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) (wherein: R 1 and R 2 are, the same or different, alkenyl, etc, and X 3 is absent or is alkyl, etc, X 1 and X 2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and Y 1 is absent or anion, L 1 is a single bond, etc, R 3 is alkyl, etc), and the like.

  本发明提供了一种脂质纳米粒子，允许核酸轻松地被引入细胞中，包括由式(I)表示的阳离子脂质（其中：R1和R2是相同或不同的烯基等，X3不存在或是烷基等，X1和X2是氢原子，或结合在一起形成单键或亚烷基，Y1不存在或是阴离子，L1是单键等，R3是烷基等），等等。
• RNAi PHARMACEUTICAL COMPOSITION FOR SUPPRESSING EXPRESSION OF KRAS GENE
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：US20140044755A1

  公开（公告）日：2014-02-13

  The present invention provides a composition for suppressing the expression of a KRAS gene, comprising a lipid particle containing, as a drug, a double-stranded nucleic acid having an antisense strand having a sequence of bases complementary to the sequence of at least 19 continuous bases of any one KRAS gene's mRNA of sequence Nos. 1 to 3; and a cationic lipid represented by the following formula (I): wherein R 1 and R 2 , which are the same or different, are each linear or branched alkyl, alkenyl or alkynyl having a carbon number of from 12 to 24; L 1 and L 2 , which are the same or different, are each —CO—O— or —O—CO—; a and b, which are the same or different, are each 1 to 3; and R 3 is a hydrogen atom, alkyl having a carbon number of from 1 to 6, or alkenyl having a carbon number of from 3 to 6, and the like.

  本发明提供了一种用于抑制KRAS基因表达的组合物，包括含有脂质颗粒的药物，该药物是具有与序列号为1至3的任一KRAS基因的mRNA的至少19个连续碱基序列互补的反义链的双链核酸；以及由以下式（I）表示的阳离子脂质： 其中 R1和R2，相同或不同，分别是线性或支链烷基，烯基或炔基，碳数为12至24； L1和L2，相同或不同，分别是—CO—O—或—O—CO—； a和b，相同或不同，分别为1至3； R3是氢原子，碳数为1至6的烷基，或碳数为3至6的烯基等。
• [EN] FLUORESCENT DYES<br/>[FR] COLORANTS FLUORESCENTS
  申请人：EXOPHARM LTD

  公开号：WO2022133552A1

  公开（公告）日：2022-06-30

  The present invention relates to fluorescent dyes of formula (I), including salts thereof, and extracellular vesicles and cells labelled with the fluorescent dyes. The present invention also relates to methods, uses and kits thereof. (Formula (I))

  本发明涉及式(I)的荧光染料，包括其盐，以及使用该荧光染料标记的细胞外囊泡和细胞。本发明还涉及其方法、用途和试剂盒。 (式(I))
• ALKYLENE OXIDE ADDUCT MANUFACTURING METHOD AND ALKYLENE OXIDE ADDUCT
  申请人：Takemoto Yushi Kabushiki Kaisha

  公开号：EP3118184A1

  公开（公告）日：2017-01-18

  This is to provide a process for producing an alkylene oxide adduct which can continuously produce the alkylene oxide adduct with an optional size from a small size to a large size, a temperature and a pressure at the time of the addition reaction can be controlled with high precision, and as a result, the alkylene oxide adduct with high quality having no coloring and narrow molecular weight distribution can be continuously produced, and the above can be accomplished simultaneously, and such an alkylene oxide adduct. An alkylene oxide adduct was produced by using a microflow reactor having a flow passage with an inner diameter of 0.05 to 3.5 mm, continuously supplying a predetermined amount of alkylene oxide and a predetermined amount of an organic compound having an active hydrogen atom(s) to the flow passage in a liquid state, and these materials were reacted while passing therethrough under the conditions of a temperature of the flow passage of 70 to 200°C and a pressure of the supply port of the flow passage of 1 to 10 MPa.

  本发明的目的是提供一种环氧烷加成物的生产工艺，该工艺可连续生产粒径从小到大可供选择的环氧烷加成物，加成反应时的温度和压力可得到高精度控制，因此可连续生产无着色、分子量分布窄的高质量环氧烷加成物，并可同时完成上述工艺和环氧烷加成物。 生产环氧亚烷基加合物的方法是使用一个微流反应器，该反应器具有一个内径为 0.05 至 3.5 毫米的流道，以液态向流道连续供应预定量的环氧亚烷基和预定量的具有活性氢原子的有机化合物，在流道温度为 70 至 200°C 和流道供应口压力为 1 至 10 兆帕的条件下，这些材料在通过流道时发生反应。