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    • 3. 发明授权
    • Acid-sensitive polyacetals and methods
    • 酸敏聚缩醛和方法
    • US07048925B2
    • 2006-05-23
    • US10651394
    • 2003-08-28
    • Sang VanNitnara ViroonchatapanShouping JiLei Yu
    • Sang VanNitnara ViroonchatapanShouping JiLei Yu
    • A61K39/44C08F283/00
    • C08G4/00C07C229/22C08G73/028
    • Polyacetals comprising a recurring units represented by a formula selected from the group consisting of formula (I) and (II): wherein A comprises at least one acetal group; B is selected from the group consisting of —CH—, —CH(CH3)—, CH2CH—, —CH2C(CH3)—, —CH(CH3)CH—, and —CHCH(CH3)CH(CH3)—; Z is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VU; V is a linker group; U is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, hexadecaamine dendrimer, enhancer, and targeting receptor; R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 aryl; D is a linkage selected from the group consisting of carboxylic amide, carboxylic ester, urea, and urethane; and G is selected from the group consisting of C4 to C20 alkyl, C6-C10 aryl, and —(OCH2CH2)n—, where n is in the range of 1 to about 250, are useful in nucleic acid delivery applications. In preferred embodiments, complexes formed between polyacetals of the formulae (I) or (II) and polynucleotides are useful as transfection reagents.
    • 包含由选自式(I)和(II)的式所表示的重复单元的聚缩醛:其中A包含至少一个缩醛基; B选自-CH-,-CH(CH 3 CH 3) - ,CH 2 CH-,-CH 2 C (CH 3) - , - CH(CH 3 CH 3)CH - 和-CHCH(CH 3 CH 3)CH(CH 3) ) - ; Z选自C(O)OR 1,C(O)SR 1,C(O)NR 1 R 2和VU; V是连接基团; U选自聚(亚乙基亚胺),聚(丙烯亚胺),聚(赖氨酸),PAMAM树枝状聚合物,八胺树枝状聚合物,十六胺树枝状聚合物,增强剂和靶向受体; R 1和R 2各自各自独立地选自氢,C 1至C 10烷基 和C 6至C 10芳基; D是选自羧酸酰胺,羧酸酯,脲和氨基甲酸酯的连接体; 并且G选自C 4〜C 20烷基,C 6 -C 10芳基,C 6〜 和 - (OCH 2 CH 2 CH 2)n - ,其中n在1至约250的范围内,可用于核酸 交付应用程序。 在优选的实施方案中,在式(I)或(II)的聚缩醛和多核苷酸之间形成的络合物可用作转染试剂。
    • 4. 发明申请
    • ACID-SENSITIVE POLYACETALS AND METHODS
    • 酸敏感聚合物和方法
    • US20050049387A1
    • 2005-03-03
    • US10651394
    • 2003-08-28
    • Sang VanNitnara ViroonchatapanShouping JiLei Yu
    • Sang VanNitnara ViroonchatapanShouping JiLei Yu
    • C07C229/22C08G4/00C08G73/02C08G63/02
    • C08G4/00C07C229/22C08G73/028
    • Polyacetals comprising a recurring units represented by a formula selected from the group consisting of formula (I) and (II): wherein A comprises at least one acetal group; B is selected from the group consisting of —CH—, —CH(CH3)—, CH2CH—, —CH2C(CH3)—, —CH(CH3)CH—, and —CHCH(CH3)CH(CH3)—; Z is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VU; V is a linker group; U is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, hexadecaamine dendrimer, enhancer, and targeting receptor; R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 aryl; D is a linkage selected from the group consisting of carboxylic amide, carboxylic ester, urea, and urethane; and G is selected from the group consisting of C4 to C20 alkyl, C6-C10 aryl, and —(OCH2CH2)n—, where n is in the range of 1 to about 250, are useful in nucleic acid delivery applications. In preferred embodiments, complexes formed between polyacetals of the formulae (I) or (II) and polynucleotides are useful as transfection reagents.
    • 包含由选自式(I)和(II)的式所表示的重复单元的聚缩醛:其中A包含至少一个缩醛基; B选自-CH-,-CH(CH 3) - ,CH 2 CH - , - CH 2 C(CH 3) - , - CH(CH 3)CH-和-CHCH(CH 3)CH(CH 3) Z选自C(O)OR 1,C(O)SR 1,C(O)NR 1 R 2和VU; V是连接基团; U选自聚(亚乙基亚胺),聚(丙烯亚胺),聚(赖氨酸),PAMAM树枝状聚合物,八胺树枝状聚合物,十六胺树枝状聚合物,增强剂和靶向受体; R 1和R 2各自独立地选自氢,C 1至C 10烷基和C 6至C 10芳基; D是选自羧酸酰胺,羧酸酯,脲和氨基甲酸酯的连接体; 并且G选自C 4 -C 20烷基,C 6 -C 10芳基和 - (OCH 2 CH 2)n - ,其中n在1至约250的范围内,可用于核酸递送应用。 在优选的实施方案中,在式(I)或(II)的聚缩醛和多核苷酸之间形成的络合物可用作转染试剂。