(11Z,14Z)-icosa-11,14-dienyl methanesulfonate | 72996-07-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磺酸及其衍生物
• 英文名称: (11Z,14Z)-icosa-11,14-dienyl methanesulfonate
• 英文别名: (11Z,14Z)-icos-11,14-dienyl methanesulfonate；[(11Z,14Z)-icosa-11,14-dienyl] methanesulfonate
• CAS: 72996-07-7
• 化学式: C₂₁H₄₀O₃S
• 分子量: 372.613
• InChiKey: IIHFOWOVWJAFNN-NQLNTKRDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.9
• 重原子数：
  25
• 可旋转键数：
  18
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.81
• 拓扑面积：
  51.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (11Z,14Z)-icosa-11,14-dienyl methanesulfonate 在 sodium iodide 作用下， 以 乙腈 为溶剂， 生成 1-iodo-(Z,Z)-11,14-eicosadien
  参考文献：
  名称：

  Martin; Beletskaya; Patrick, Journal of Pharmacology and Experimental Therapeutics, 2000, vol. 294, # 3, p. 1209 - 1218

  摘要：

  DOI：
• 作为产物：
  描述：

  9-羟基-10-氧代十八烷酸甲酯 、 甲基磺酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 (11Z,14Z)-icosa-11,14-dienyl methanesulfonate
  参考文献：
  名称：

  Martin; Beletskaya; Patrick, Journal of Pharmacology and Experimental Therapeutics, 2000, vol. 294, # 3, p. 1209 - 1218

  摘要：

  DOI：

文献信息

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

  公开号：US20140294978A1

  公开（公告）日：2014-10-02

  The present invention provides a cationic lipid and the like. The cationic lipid is for delivering a medicament containing a cationic lipid which facilitates the introduction of a nucleic acid into a cell or the like, and is represented by formula (I). In the formula, R 1 is linear or branched alkyl, alkenyl, or alkynyl, each having 8 to 24 carbon atoms, R 2 is linear or branched alkyl, alkenyl, or alkynyl, each having 8 to 24 carbon atoms, or alkoxyethylene, alkoxypropylene, alkenyloxyethylene, alkenyloxypropylene, alkynyloxyethylene, or alkynyloxypropylene, R 3 and R 4 may be the same or different, and are each alkyl having 1 to 3 carbon atoms or are combined together to form alkylene having 2 to 6 carbon atoms, or R 3 and R 5 are combined together to form alkylene having 2 to 6 carbon atoms, R 5 is a hydrogen atom, alkyl having 1 to 6 carbon atoms, alkenyl having 3 to 6 carbon atoms, amino, monoalkylamino, hydroxy, alkoxy, carbamoyl, monoalkylcarbamoyl, dialkylcarbamoyl, or the like, or is combined together with R 3 to form alkylene having 2 to 6 carbon atoms, X is alkylene having 1 to 6 carbon atoms, and Y is a single bond, alkylene having 1 to 6 carbon atoms, or the like.

  本发明提供了一种阳离子脂质等。该阳离子脂质用于传递含有阳离子脂质的药物，有助于将核酸引入细胞或类似物中，并由式(I)表示。在该式中，R1为具有8到24个碳原子的线性或支链烷基、烯基或炔基，R2为具有8到24个碳原子的线性或支链烷基、烯基或炔基，或者为烷氧乙烯、烷氧丙烯、烯氧乙烯、烯氧丙烯、炔氧乙烯或炔氧丙烯，R3和R4可以相同也可以不同，分别为具有1到3个碳原子的烷基，或者结合在一起形成具有2到6个碳原子的烷基，或者R3和R5结合在一起形成具有2到6个碳原子的烷基，R5为氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的烯基、氨基、单烷基氨基、羟基、烷氧基、氨基甲酰基、单烷基氨基甲酰基、二烷基氨基甲酰基等，或者与R3结合在一起形成具有2到6个碳原子的烷基，X为具有1到6个碳原子的烷基，Y为单键、具有1到6个碳原子的烷基等。
• 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。
• Cationic lipid
  申请人：Kuboyama Takeshi

  公开号：US09408914B2

  公开（公告）日：2016-08-09

  The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

  本发明提供了一种阳离子脂质，可以使核酸轻松地引入细胞中，其化学式表示为（I）（其中：R1和R2是相同或不同的烯基等，X1和X2是氢原子，或结合在一起形成单键或烷基，X3不存在或是烷基等，Y不存在或是阴离子，a和b是相同或不同的0到3，L3是单键等，R3是烷基等，L1和L2是-O-，-CO-O-或-O-CO-），以及包括该阳离子脂质和核酸的组合物，使用该组合物将核酸引入细胞中的方法等。