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    • 4. 发明申请
    • BIODEGRADABLE POLYACETALS
    • 生物可降解聚酯
    • WO2004076557A1
    • 2004-09-10
    • PCT/US2004/005363
    • 2004-02-24
    • NITTO DENKO CORPORATIONYU, LeiVAN, SangJI, ShoupingMATSUMOTO, Kenji
    • YU, LeiVAN, SangJI, ShoupingMATSUMOTO, Kenji
    • C08L59/00
    • C08G73/0213A61K47/59C08G65/002
    • A polymer comprising recurring units represented by formula (I); wherein X is selected from the group consisting of C(O)OR 1 , C(O)SR 1 , C(O)NR 1 R 2 , and VZ, where R 1 and R 2 are each individually selected from the group consisting of hydrogen, C 1 to C 10 alkyl, and C 6 to C 10 aryl, where V is a labile linker group, and where Z is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, and hexadecaamine dendrimer; and wherein Y is selected from the group consisting of -(CH 2 ) 2 -, -(CH 2 ) 2 -O-(CH 2 ) 2 -, -(CH 2 ) 2 -O-(CH 2 ) 2 -O-(CH 2 ) 2 -, and -(CH 2 ) 3 -NHC(O)-(CH 2 ) 6 -C(O)NH-(CH 2 ) 3 - is useful in nucleic acid delivery applications. Polyacetals of the formula (I) are preferably made by reacting appropriate diols and divinyl ethers. In preferred embodiments, complexes formed between polyacetals of the formula (I) and polynucleotides are useful as transfection reagents.
    • 一种包含由式(I)表示的重复单元的聚合物; 其中X选自C(O)OR 1,C(O)SR 1,C(O)NR 1 R 2和V Z,其中R 1和R 各自独立地选自氢,C1至C10烷基和C6至C10芳基,其中V是不稳定的连接基团,其中Z选自聚(乙烯亚胺),聚(乙烯亚胺) 丙烯亚胺),聚(赖氨酸),PAMAM树枝状聚合物,八胺树枝状聚合物和十六胺树枝状聚合物; 并且其中Y选自 - (CH 2)2 - , - (CH 2)2 -O-(CH 2)2 - , - (CH 2)2 -O - (CH 2)2 -O - (CH 2)2 - 和 - (CH 2)3 -NHC(O) - (CH 2)6 -C(O)NH-(CH 2)3 - 可用于核酸递送应用。 式(I)的聚缩醛优选通过使适当的二醇和二乙烯基醚反应来制备。 在优选的实施方案中,在式(I)的聚缩醛和多核苷酸之间形成的络合物可用作转染试剂。