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    • 5. 发明申请
    • Lipid
    • 脂质
    • US20100297023A1
    • 2010-11-25
    • US12520261
    • 2007-12-21
    • Andrew David MillerPatrick ArbuthnotMichael JorgensenMichael KellerNazila KamalyAbderrahim AissaouiMaya Thanou
    • Andrew David MillerPatrick ArbuthnotMichael JorgensenMichael KellerNazila KamalyAbderrahim AissaouiMaya Thanou
    • A61K47/18C07C237/22A61K31/713A61K48/00A61K49/10C12N5/02
    • 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) R3R4N—[Y]q—(CpH2p)—X-Linker-NR1R2 (I) wherein R3 and R4 are independently selected from H and hydrocarbyl groups; q is an integer selected from 1 to 10; Y represents a group (CnH2n)NR5, 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 R5 is independently selected from H and hydrocarbyl groups; p is an integer selected from 1 to 10; X is an optional group selected from —NR7—, —C(═O)—NR8—, —NR9—C(═O)—, —C(═O)—, —O—, and NR10—C(=0)0-, wherein each R7, R8, R9 and R10 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 —(OCH2CH2)1-10, —NR6-(CvH2v)—C(═O)—, wherein R6 is H or a hydrocarbyl group and v is an integer selected from 1 to 11, and —C(=0)-(CH2)0-10—CH2—C(=0)-; R1 is selected from acyclic groups having from 4 to 30 carbon atoms; and R2 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)R3R4N- [Y] q-(CpH2p)-X-连接子-NR1R2(I)的脂质,其中R3和R4独立地选自H和烃基; q是选自1至10的整数; Y表示基团(C 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,条件是对于至少一个单元Y,n为2,和(iii)每个R 5独立地选自H和烃基; p是选自1至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 )0-,其中每个R 7,R 8,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,肽残基和式 - (OCH 2 CH 2)1-10,-NR 6 - (CvH2v)-C(= O) - ,其中R6是H或烃基,v是选自1至11的整数,和-C(= O) - (CH 2)0-10-CH 2 -C = 0) - ; R1选自具有4至30个碳原子的无环基团; 并且R 2选自H和具有4至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。