Lipid
    3.
    发明申请
    Lipid 审中-公开
    脂质

    公开(公告)号:US20100297023A1

    公开(公告)日:2010-11-25

    申请号:US12520261

    申请日:2007-12-21

    摘要: 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.

    摘要翻译: 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。

    Novel Liposome Nanoparticles for Tumor Magnetic Resonance Imaging
    4.
    发明申请
    Novel Liposome Nanoparticles for Tumor Magnetic Resonance Imaging 审中-公开
    用于肿瘤磁共振成像的新型脂质体纳米颗粒

    公开(公告)号:US20130129636A1

    公开(公告)日:2013-05-23

    申请号:US13511126

    申请日:2010-11-19

    IPC分类号: A61K49/18

    摘要: The present invention provides novel liposomes comprising Gd.DOTA.DSA (gadolinium(III)2-{4,7-bis-carboxymethyl-10-[(N,N-distearylamidomethyl-N′-amido-methyl]-1,4,7,10-tetra-azacyclododec-1-yl}-acetic acid), characterised in that said liposome further comprises a neutral, fully saturated phospholipid component (e.g. DSPC (1,2-distearoyl-sn-glycero-3-phosphocholine]), which are of particular use in the preparation of magnetic resonance contrast agents for enhancing a magnetic resonance image of tumours in a mammal.

    摘要翻译: 本发明提供了包含Gd.DOTA.DSA(钆(III)2- {4,7-双 - 羧甲基-10 - [(N,N-二硬脂酰氨基甲基-N'-酰氨基 - 甲基] 7,10-四氮杂环十二烷-1-基} - 乙酸),其特征在于所述脂质体还包含中性完全饱和的磷脂组分(例如DSPC(1,2-二硬脂酰-sn-甘油-3-磷酸胆碱)) ,其特别用于制备用于增强哺乳动物肿瘤的磁共振图像的磁共振造影剂。