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    • 8. 发明申请
    • LIPID
    • WO2008078102A2
    • 2008-07-03
    • PCT/GB2007004967
    • 2007-12-21
    • IMUTHES LTDUNIV WITWATERSRANDMILLER ANDREW DAVIDARBUTHNOT PATRICKJORGENSEN MICHAELKELLER MICHAELKAMALY NAZILAAISSAOUI ABDERRAHIMTHANOU MAYA
    • MILLER ANDREW DAVIDARBUTHNOT PATRICKJORGENSEN MICHAELKELLER MICHAELKAMALY NAZILAAISSAOUI ABDERRAHIMTHANOU MAYA
    • A61K9/127A61K47/34A61K47/48C07C237/22C07F9/10C07J41/00C08G73/02C12N15/11C12N15/88
    • C07C237/22A01K2267/0337A61K9/1272A61K47/34A61K47/543A61K47/6907A61K47/6911A61K48/0025C12N15/111C12N15/88C12N2310/14C12N2320/32C12N2730/10111Y10T428/2984
    • The present invention provides a lipid of the formula (I) R 3 R 4 N-[Y] q -(C p H 2p )-X-Linker-NR 1 R 2 (I) wherein R 3 and R 4 are independently selected from H and hydrocarbyl groups; q is an integer selected from 1 to 10; Y represents a group (C n H 2n )NR 5 , wherein (i) when q is 1, n is 2, or (ii) when q is greater than 1, each Y may be the same or different and each n is an integer independently selected from 1 to 10, with the proviso that for at least one unit Y, n is 2, and (iii) each R 5 is independently selected from H and hydrocarbyl groups; p is an integer selected from 1 to 10; X is an optional group selected from -NR 7 -, -C(=O)-N R 8 -, -NR 9 -C(=O)-, -C(=O)-, -O-, and -NR 10 -C(=0)0-, wherein each R 7 , R 8 , R 9 and R 10 is independently selected from H and hydrocarbyl groups, Linker is an optional group selected from amino acid residues, peptide residues and groups of the formula -(OCH 2 CH 2 ) 1-10 , -NR 6 -(CvH 2v )-C(=O)-, wherein R 6 is H or a hydrocarbyl group and v is an integer selected from 1 to 11, and -C(=0)-(CH 2 ) 0-10 -CH 2 -C(=0)-; R 1 is selected from acyclic groups having from 4 to 30 carbon atoms; and R 2 is selected from H and acyclic groups having from 4 to 30 carbon atoms. Said lipids can be used in a delivery vehicle (e.g. micelle or liposome) for the delivery of one or more (therapeutic or diagnostic) agents.
    • 本发明提供式(I)的脂类R 3 R 4 N - [Y] q - (C p 其中R 3是氢原子,其中R 3,R 2,R 2,R 2,R 2,R 2, 和R 4独立地选自H和烃基; q是从1至10的整数; Y表示一个基团(C n H n H 2n)NR 5,其中(i)当q为1时,n为2或(ii )当q大于1时,每个Y可以相同或不同,并且每个n是独立地选自1至10的整数,条件是对于至少一个单元Y,n是2,和(iii)每个R 5个独立地选自H和烃基; p是从1到10的整数; X是选自-NR 7 - , - C(= O)-NR 8 - , - NR 9 -C( = O) - , - C(= O) - , - O-和-NR 10 -C(= O)O-,其中每个R 7,R R 9,R 9和R 10独立地选自H和烃基,连接子是选自氨基酸残基,肽残基的任选基团 和式 - (OCH 2 CH 2 CH 2)1 - , - NR 6 - (C v H C(= O) - ,其中R 6为H或烃基,v为选自1至11的整数,且-C(= O ) - (CH 2 0-10 -CH 2 -C(= O) - ; R 1选自具有4至30个碳原子的无环基团; R 2选自H和具有4-30个碳原子的无环基。 所述脂质可用于递送载体(例如胶束或脂质体)中以递送一种或多种(治疗或诊断)试剂。