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    • 6. 发明授权
    • Derivatized oligonucleotides having improved uptake and other properties
    • 具有改善摄取和其他性质的衍生寡核苷酸
    • US06831166B2
    • 2004-12-14
    • US10073718
    • 2002-02-11
    • Muthiah ManoharanPhillip Dan CookClarence Frank Bennett
    • Muthiah ManoharanPhillip Dan CookClarence Frank Bennett
    • C07H1900
    • C07H21/04C07J1/00C12N2710/20022H04J2203/0042H04J2203/006
    • Linked nucleosides having at least one functionalized nucleoside that bears a substituent such as a steroid molecule, a reporter molecule, a non-aromatic lipophilic molecule, a reporter enzyme, a peptide, a protein, a water soluble vitamin, a lipid soluble vitamin, an RNA cleaving complex, a metal chelator, a porphyrin, an alkylator, a pyrene, a hybrid photonuclease/intercalator, or an aryl azide photo-crosslinking agent exhibit increased cellular uptake and other properties. The substituent can be attached at the 2′-position of the functionalized nucleoside via a linking group. If at least a portion of the remaining liked nucleosides are 2′-deoxy-2′-fluoro, 2′-O-methoxy, 2′-O-ethoxy, 2′-O-propoxy, 2′-O-aminoalkoxy or 2′-O-allyloxy nucleosides, the substituent can be attached via a linking group at any of the 3′ or the 5′ positions of the nucleoside or on the heterocyclic base of the nucleoside or on the inter-nucleotide linkage linking the nucleoside to an adjacent nucleoside.
    • 具有至少一个具有取代基的官能化核苷的连接核苷,例如类固醇分子,报道分子,非芳族亲脂性分子,报道酶,肽,蛋白质,水溶性维生素,脂溶性维生素, RNA切割复合物,金属螯合剂,卟啉,烷基化剂,芘,混合光子核酸酶/嵌入剂或芳基叠氮化物光交联剂表现出增加的细胞摄取和其它性质。 取代基可以通过连接基团连接在官能化核苷的2'-位上。 如果至少一部分剩余的核苷类为2'-脱氧-2'-氟,则2'-O-甲氧基,2'-O-乙氧基,2'-O-丙氧基,2'-O-氨基烷氧基或2 '-O-烯丙氧基核苷,取代基可以通过连接基团在核苷的3'或5'位置或核苷的杂环碱基上或连接核苷与核苷酸之间的核苷酸间连接 相邻核苷。