N,N-dioleyl-p-toluenesulfonamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N,N-dioleyl-p-toluenesulfonamide
• 英文别名: 4-methyl-N,N-bis[(Z)-octadec-9-enyl]benzenesulfonamide
• 化学式: C₄₃H₇₇NO₂S
• 分子量: 672.156
• InChiKey: AQSCRPVEHVNUFY-AUYXYSRISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  17.2
• 重原子数：
  47
• 可旋转键数：
  34
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.77
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-溴-顺-9-十八碳烯 、 对甲苯磺酰胺 在 potassium carbonate 作用下， 以87%的产率得到N,N-dioleyl-p-toluenesulfonamide
  参考文献：
  名称：

  Lipid complexes for transferring at least a therapeutically active substance, in particular a polynucleotide into a target cell and use in gene therapy

  摘要：

  该发明涉及至少包含一种脂质和至少一种有治疗活性的物质的复合物，用于将该物质转运到靶细胞中，其特征在于所述脂质的化学式为（I）：其中：n1、n2为0到1之间的整数；R1、R2相同或不同，选自由氢原子和烷基基团（含1到6个碳原子，可选地独立地被羟基基团取代）的群中；或在一个特定情况下，当n1=n2=1时，R1和R2可以共同形成2到3个碳原子（C2-C3）的二价烷基链；R3、R4相同或不同，为1到6个碳原子的烷基基团，或者共同形成2到3个碳原子（C2-C3）的二价烷基链；m、p相同或不同为1到10之间的整数；R5、R6相同或不同，选自下列基团的群中：1）R7C(═O)—X—其中：X=NH、O、S；R7为6到23个碳原子（C6-C23）的直链或支链烷基或烯基基团；2）R8R9NC(═O)—其中：R8、R9相同或不同，选自氢原子或6到23个碳原子的直链或支链烷基或烯基基团，前提是R8、R9不能同时对应于氢原子；3）并且其中一个基团R5、R6还可以对应于氢原子。该发明还涉及在基因治疗中使用所述复合物。

  公开号：

  US06291423B1

文献信息

• Novel lipid complexes for transferring at least one therapeutically active substance, in particular a polynucleotide, into a target cell, and use in gene therapy
  申请人：——

  公开号：US20020025920A1

  公开（公告）日：2002-02-28

  The present invention relates to a complex comprising at least a lipid and at least a therapeutically active substance for transferring the therapeutically active substance into a target cell. The present invention also relates to a method of transferring a therapeutically active substance into cells.

  本发明涉及至少包括脂质和至少一种治疗活性物质的复合物，用于将治疗活性物质转移至靶细胞。本发明还涉及将治疗活性物质转移至细胞的方法。
• NOUVEAUX COMPLEXES LIPIDIQUES POUR LE TRANSFERT D'AU MOINS UNE SUBSTANCE THERAPEUTIQUEMENT ACTIVE, NOTAMMENT UN POLYNUCLEOTIDE, DANS UNE CELLULE CIBLE ET UTILISATION EN THERAPIE GENIQUE
  申请人：TRANSGENE S.A.

  公开号：EP0956050A1

  公开（公告）日：1999-11-17
• US6291423B1
  申请人：——

  公开号：US6291423B1

  公开（公告）日：2001-09-18
• [EN] NOVEL LIPID COMPLEXES FOR TRANSFERRING AT LEAST A THERAPEUTICALLY ACTIVE SUBSTANCE, IN PARTICULAR A POLYNUCLEOTIDE INTO A TARGET CELL AND USE IN GENE THERAPY<br/>[FR] NOUVEAUX COMPLEXES LIPIDIQUES POUR LE TRANSFERT D'AU MOINS UNE SUBSTANCE THERAPEUTIQUEMENT ACTIVE, NOTAMMENT UN POLYNUCLEOTIDE, DANS UNE CELLULE CIBLE ET UTILISATION EN THERAPIE GENIQUE
  申请人：TRANSGENE S.A.

  公开号：WO1998056423A1

  公开（公告）日：1998-12-17

  (EN) The invention concerns a complex comprising at least a lipid and at least a therapeutically active substance useful for transferring said substance into a target cell, characterised in that said lipid is of formula (I): in which: n1, n2, identical or different are whole numbers between 0 and 1; R1, R2, identical or different are: a) selected among the group consisting of a hydrogen atom and alkyl radicals with 1 to 6 carbon atoms optionally substituted, independently of one another, by a hydroxyl radical; or b) in one particular case for which n1 = n2 = 1, R1 and R2 can form together a divalent alkylene chain of 2 to 3 carbon atoms (C2-C3); R3, R4, identical or different are alkyl radicals of 1 to 6 carbon atoms or can together form a divalent alkylene chain of 2 to 3 carbon atoms (C2-C3); m, p, identical or different are whole numbers between 1 and 10; R5, R6, identical or different are selected in the group consisting of radicals of formula: 1) R7 C(=0)-X- in which: X = NH, 0, S; R7 is an alkyl or alkenyl radical of 6 to 23 carbon atoms (C6-C23), linear or branched; 2) R8R9NC(=0)- in which: R8, R9, identical or different are selected among the group consisting of the hydrogen atom or alkyl or alkenyl radicals of 6 to 23 carbon atoms, linear or branched, provided that R8, R9, cannot simultaneously correspond to the hydrogen atom; 3) and one of the radicals R5, R6 can moreover correspond to the hydrogen atom. The invention also concerns the use of said complex in gene therapy.(FR) L'invention concerne un complexe comprenant au moins un lipide et au moins une substance thérapeutiquement active utilisable pour le transfert de ladite substance à l'intérieur d'une cellule cible, caractérisé en ce que ledit lipide est de formule (I), dans laquelle: n1, n2 identiques ou différents sont des nombres entiers choisis parmi 0 ou 1; R1, R2 identiques ou différents, sont: a) choisis parmi le groupe constitué par un atome d'hydrogène et des radicaux alkyle de 1 à 6 atomes de carbone éventuellement substitués, indépendamment les uns des autres, par un radical hydroxyle; ou b) selon un cas particulier pour lequel n1 = n2 = 1, R1 et R2 peuvent former ensemble une chaîne divalente alkylène de 2 à 3 atomes de carbone (C2-C3); R3, R4, identiques ou différents sont des radicaux alkyle de 1 à 6 atomes de carbone ou peuvent former ensemble une chaîne divalente alkylène de 2 à 3 atomes de carbone (C2-C3); m, p identiques ou différents sont des nombres entiers compris entre 1 et 10; R5, R6, identiques ou différents sont choisis dans le groupe constitué par les radicaux de formule: 1) R7 C(=0)-X- dans laquelle: X = NH, 0, S; R7 est un radical de 6 à 23 atomes de carbone (C6-C23) alkyle ou alcényle, linéaire ou ramifié; 2) R8R9NC(=0)- dans laquelle: R8, R9, identiques ou différents sont choisis parmi le groupe constitué par l'atome d'hydrogène ou des radicaux de 6 à 23 atomes de carbone alkyle ou alcényle, linéaires ou ramifiés, à la condition que R8, R9 ne puissent correspondre simultanément à l'atome d'hydrogène; 3) et l'un des radicaux R5, R6 pouvant en outre correspondre à l'atome d'hydrogène et son utilisation en thérapie génique.
• Lipid complexes for transferring at least a therapeutically active substance, in particular a polynucleotide into a target cell and use in gene therapy
  申请人：Transgene S.A.

  公开号：US06291423B1

  公开（公告）日：2001-09-18

  The invention concerns a complex comprising at least a lipid and at least a therapeutically active substance useful for transferring said substance into a target cell, characterised in that said lipid is of formula (I): in which: n1, n2, identical or different are whole numbers between 0 and 1; R1, R2, identical or different are: a) selected among the group consisting of a hydrogen atom and alkyl radicals with 1 to 6 carbon atoms optionally substituted, independently of one another, by a hydroxyl radical; or b) in one particular case for which n1=n2=1, R1 and R2 can form together a divalent alkylene chain of 2 to 3 carbon atoms (C2-C3); R3, R4, identical or different are alkyl radicals of 1 to 6 carbon atoms or can together form a divalent alkylene chain of 2 to 3 carbon atoms (C2-C3); m, p, identical or different are whole numbers between 1 and 10; R5, R6, identical or different are selected in the group consisting of radicals of formula: 1) R7 C(═O)—X— in which: X=NH, O, S; R7 is an alkyl or alkenyl radical of 6 to 23 carbon atoms (C6-C23), linear or branched; 2) R8R9NC(═O)— in which: R8, R9, identical or different are selected among the group consisting of the hydrogen atom or alkyl or alkenyl radicals of 6 to 23 carbon atoms, linear or branched, provided that R8, R9, cannot simultaneously correspond to the hydrogen atom; 3) and one of the radicals R5, R6 can moreover correspond to the hydrogen atom. The invention also concerns the use of said complex in gene therapy.

  该发明涉及至少包含一种脂质和至少一种有治疗活性的物质的复合物，用于将该物质转运到靶细胞中，其特征在于所述脂质的化学式为（I）：其中：n1、n2为0到1之间的整数；R1、R2相同或不同，选自由氢原子和烷基基团（含1到6个碳原子，可选地独立地被羟基基团取代）的群中；或在一个特定情况下，当n1=n2=1时，R1和R2可以共同形成2到3个碳原子（C2-C3）的二价烷基链；R3、R4相同或不同，为1到6个碳原子的烷基基团，或者共同形成2到3个碳原子（C2-C3）的二价烷基链；m、p相同或不同为1到10之间的整数；R5、R6相同或不同，选自下列基团的群中：1）R7C(═O)—X—其中：X=NH、O、S；R7为6到23个碳原子（C6-C23）的直链或支链烷基或烯基基团；2）R8R9NC(═O)—其中：R8、R9相同或不同，选自氢原子或6到23个碳原子的直链或支链烷基或烯基基团，前提是R8、R9不能同时对应于氢原子；3）并且其中一个基团R5、R6还可以对应于氢原子。该发明还涉及在基因治疗中使用所述复合物。