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    COMPOUNDS FOR TARGETING DRUG DELIVERY AND ENHANCING SIRNA ACTIVITY
    1.
    发明公开
    COMPOUNDS FOR TARGETING DRUG DELIVERY AND ENHANCING SIRNA ACTIVITY 有权
    靶向药物递送和增强SIRNA活性的化合物

    公开(公告)号：EP2998289A1

    公开(公告)日：2016-03-23

    申请号：EP15181729.3

    申请日：2012-06-08

    申请人： NITTO DENKO CORPORATION

    发明人： Sridhar, C. Nagarajan ,  Karmali, Priya ,  Payne, Joseph E. ,  Hou, Zheng ,  Gaudette, John A. ,  Knopov, Victor ,  Witte, Richard P. ,  Ahmadian, Mohammad ,  Perelman, Loren A. ,  Tanaka, Yasunobu ,  Akopian, Violetta ,  Niitsu, Yoshiro

    IPC分类号： C07C237/08 ,  A61K31/16 ,  A61P1/16 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04 ,  A61K9/127

    CPC分类号： C07C237/08 ,  A61K9/1271 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

    摘要： Here described are compounds of formula I:

    wherein R 1 and R 2 is independently selected from a group consisting of C 10 to C 18 alkyl, C 12 to C 18 alkenyl, and oleyl group; wherein R 3 and R 4 are independently selected from a group consisting of C 1 to C 6 alkyl, and C 2 to C 6 alkanol; wherein X is selected from a group consisting of -CH 2 -, -S-, and -O- or absent; wherein Y is selected from -(CH 2 ) n , -S(CH 2 ) n , - O(CH 2 ) n -, thiophene, -SO 2 (CH 2 ) n -, and ester, wherein n = 1-4; wherein a = 1-4; wherein b=1-4; wherein c=1-4; and wherein Z is a counterion; and compounds consisting of the structure
    (targeting molecule) m -linker-(targeting molecule) n ,
    wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including one or both of these compounds which are useful for the delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

    摘要翻译： 这里描述的是式I的化合物：其中R 1和R 2独立地选自由C 10至C 18烷基，C 12至C 18烯基和油烯基组成的组; 其中R3和R4独立地选自C1-C6烷基和C2-C6链烷醇; 其中X选自-CH 2 - ， - S-和-O-或不存在; 其中Y选自 - （CH2）n，-S（CH2）n，-O（CH2）n-，噻吩，-SO2（CH2）n-和酯，其中n = 1-4; 其中a = 1-4; 其中b = 1-4; 其中c = 1-4; 并且其中Z是抗衡离子; 和由结构（靶向分子）m-连接体 - （靶向分子）n组成的化合物，其中靶向分子是在靶细胞上具有特定受体的类视黄醇或脂溶性维生素; 其中m和n独立地为0,1,2或3; 并且其中接头包含聚乙二醇（PEG）或PEG-样分子，以及包含用于递送治疗剂的这些化合物中的一种或两种的组合物和药物制剂; 以及使用这些组合物和药物制剂的方法。