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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。
    • 5. 发明授权
    • Biodegradable polyacetals
    • 可生物降解聚缩醛
    • US06878374B2
    • 2005-04-12
    • US10375705
    • 2003-02-25
    • Lei YuSang VanShouping JiKenji Matsumoto
    • Lei YuSang VanShouping JiKenji Matsumoto
    • A61K47/48C08G65/00C08G73/02A61K39/44C08F283/00
    • C08G73/0213A61K47/59C08G65/002
    • A polymer comprising recurring units represented by formula (I): wherein X is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VZ, where R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 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 —(CH2)2—, —(CH2)2—O—(CH2)2—, —(CH2)2—O—(CH2)2—, and —(CH2)3—NHC(O)—(CH2)6—C(O)NH—(CH2)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VZ,其中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,其中V是不稳定的连接基团,并且其中Z被选择 由聚(乙烯亚胺),聚(丙烯亚胺),聚(赖氨酸),PAMAM树枝状聚合物,八胺树枝状聚合物和十六胺树枝状聚合物组成的组中; 其中Y选自 - (CH 2)2 - , - (CH 2)2 -O-(CH 2)2 - , - (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。