2-O-(2-diethylaminoethyl)-carbamoyl-1,3-O-dioleoylglycerol | 160005-13-0

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: 2-O-(2-diethylaminoethyl)-carbamoyl-1,3-O-dioleoylglycerol
• 英文别名: 2-o-(2-diethylaminoethyl)carbamoyl-1,3-o-dioleoyl glycerol；2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoylglycerol；2-O-(2-Diethylaminoethyl)carbamoyl-1,3-o-dioleylglycerol；[2-[2-(diethylamino)ethylcarbamoyloxy]-3-[(Z)-octadec-9-enoyl]oxypropyl] (Z)-octadec-9-enoate
• CAS: 160005-13-0
• 化学式: C₄₆H₈₆N₂O₆
• 分子量: 763.199
• InChiKey: SDFOCMGSQNWWPN-SXAUZNKPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  15.5
• 重原子数：
  54
• 可旋转键数：
  43
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.85
• 拓扑面积：
  94.2
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• Galactose Derivative, Drug Carrier and Medicinal Composition
  申请人：Ohgi Tadaaki

  公开号：US20070244058A1

  公开（公告）日：2007-10-18

  The present invention relates to a novel and useful galactose derivative constituting a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the carrier and a medicine. The present invention also relates to a galactose derivative made up of galactose, a suitable spacer and a certain lipid, a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, or an oligo nucleic acid).

  本发明涉及一种新颖且有用的半乳糖衍生物，该衍生物构成了一种药物载体，可以有效地将药物转运到肝脏，包括该衍生物的药物载体以及包含该载体和药物的制药组合物。本发明还涉及由半乳糖、适当的间隔物和某种脂质组成的半乳糖衍生物，该衍生物构成了一种药物载体，包括该衍生物和阳离子脂质的药物载体，以及包含该载体和药物（优选为双链RNA、双链DNA或寡核苷酸）的制药组合物。
• POLYETHYLENE GLYCOL DERIVATIVE
  申请人：Sonoke Satoru

  公开号：US20100074880A1

  公开（公告）日：2010-03-25

  The present invention includes a novel polyethylene glycol derivative; a drug carrier comprising the derivative; and a pharmaceutical composition comprising the drug carrier having a pharmacologically active substance included therein. Specifically disclosed are: a polyethylene glycol derivative represented by the general formula (I); a drug carrier comprising the derivative and 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoyl-glycerol; and a pharmaceutical composition comprising the drug carrier and a pharmacologically active substance (preferably double-stranded RNA, double-stranded DNA or an oligonucleic acid), wherein R represents a saturated or unsaturated aliphatic hydrocarbon group having 10 to 30 carbon atoms or a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms; and n represents an integer of 30 to 150.

  本发明包括一种新型聚乙二醇衍生物；一种包含该衍生物的药物载体；以及一种包含有药理活性物质的药物组合物，其包括该药物载体。具体揭示了：由通式（I）表示的聚乙二醇衍生物；包括该衍生物和2-O-(2-二乙氨基乙基)氨基甲酰基-1,3-O-二油酰甘油的药物载体；以及包含有药理活性物质（优选为双链RNA、双链DNA或寡核苷酸）的药物组合物，其中R表示具有10到30个碳原子的饱和或不饱和脂肪族碳氢基团或脂肪酸残基；n表示30到150的整数。
• DRUG CARRIER
  申请人：Sonoke Satoru

  公开号：US20110098344A1

  公开（公告）日：2011-04-28

  A drug carrier characterized by mainly containing a polyethylene-glycol-modified phospholipid and a cationic lipid and containing the polyethylene-glycol-modified phospholipid in a concentration within a specific range. The drug carrier, which is of the in-blood residence type, is characterized by comprising a polyethylene-glycol-modified phospholipid represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: [wherein X represents the following (II) or (III) and n is an integer of 30-150] [wherein R 1 represents a saturated linear C 17-22 fatty acid residue] and 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoylglylcerol. It is further characterized in that the polyethylene-glycol-modified phospholipid represented by the general formula (I) is contained in an amount of 30-50 wt. % based on the total amount of the lipids in the drug carrier.

  一种药物载体，其主要包含聚乙二醇修饰的磷脂和阳离子脂质，并且聚乙二醇修饰的磷脂的浓度在特定范围内。该药物载体属于血内驻留型，其特征在于包含以下通式（I）表示的聚乙二醇修饰的磷脂或其药学上可接受的盐：[其中X表示以下（II）或（III），n是30-150的整数][其中R1表示饱和线性C17-22脂肪酸残基]和2-O-(2-二乙氨乙基)氨基甲酰基-1,3-O-二油酰基甘油。它进一步特征在于，根据药物载体中脂质的总量，聚乙二醇修饰的磷脂的含量为30-50重量％。
• ANTISENSE NUCLEIC ACIDS
  申请人：Watanabe Naoki

  公开号：US20130211062A1

  公开（公告）日：2013-08-15

  The present invention provides a pharmaceutical composition which causes skipping of the 53rd exon in the human dystrophin gene with a high efficiency. The present invention provides an oligomer which efficiently enables to cause skipping of the 53rd exon in the human dystrophin gene.

  本发明提供了一种药物组合物，其能高效地引起人类肌萎缩蛋白基因中的第53个外显子跳过。本发明提供了一种寡核苷酸，其能有效地引起人类肌萎缩蛋白基因中的第53个外显子跳过。
• DRUG COMPOSITION CONTAINING NUCLEIC ACID COPOLYMER
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0685234A1

  公开（公告）日：1995-12-06

  The invention aims at effectively utilizing a single-stranded nucleic acid copolymer, in particular, poly(adenylic acid-uridylic acid) and providing a drug composition having an antitumor effect. An example of the drug composition of the invention is one containing a lipid device, such as Lipofecting®, 3-O-(4-dimethylaminobutanoyl)-1,2-O-dioleylglycerol, 3-O-(2-dimethylaminoethyl)carbamoyl-1,2-O-dioleylglycerol, 3-O-(2-diethylaminoethyl)-carbamoyl-1,2-O-dioleylglycerol or 2-O-(2-diethyl-aminoethyl)carbamoyl-1,3-O-dioleylglycerol, and poly(adenylic acid-uridylic acid).

  本发明旨在有效利用单链核酸共聚物，特别是聚（腺嘌呤核酸-尿苷酸），并提供一种具有抗肿瘤效果的药物组合物。本发明药物组合物的一个例子是含有脂质装置，如 Lipofecting®、3-O-(4-二甲基氨基丁酰基)-1,2-O-二油酸甘油、3-O-(2-二甲基氨基乙基)氨基甲酰基-1、2-O-二烯丙基甘油、3-O-(2-二乙基氨基乙基)氨基甲酰基-1,2-O-二烯丙基甘油或 2-O-(2-二乙基氨基乙基)氨基甲酰基-1,3-O-二烯丙基甘油，以及聚(腺嘌呤核苷酸)。