C3′-methylene hydrogen phosphonate monomers and related compounds
    3.
    发明授权
    C3′-methylene hydrogen phosphonate monomers and related compounds 失效
    C3'-亚甲基氢膦酸酯单体和相关化合物

    公开(公告)号:US06414135B1

    公开(公告)日:2002-07-02

    申请号:US09349035

    申请日:1999-07-07

    IPC分类号: C07H2100

    CPC分类号: C07H21/00 C07H19/10

    摘要: The present invention is directed to nucleoside monomers wherein the 3′-O atom is replaced with a methylene group. The present invention also provides oligomers comprising a plurality of such monomers which are linked by methylenephosphonate linkages. Further, methods of preparing monomers and oligomers according to the present invention are provided.

    摘要翻译: 本发明涉及其中3'-O原子被亚甲基代替的核苷单体。 本发明还提供了包含多个这样的单体的低聚物,其通过亚甲基膦酸酯键连接。 此外,提供了制备根据本发明的单体和低聚物的方法。

    Derivatized oligonucleotides having improved uptake and other properties
    6.
    发明授权
    Derivatized oligonucleotides having improved uptake and other properties 失效
    具有改善摄取和其他性质的衍生寡核苷酸

    公开(公告)号:US06831166B2

    公开(公告)日:2004-12-14

    申请号:US10073718

    申请日:2002-02-11

    IPC分类号: C07H1900

    摘要: 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.

    摘要翻译: 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。

    Carbamate-derivatized nucleosides and oligonucleosides
    7.
    发明授权
    Carbamate-derivatized nucleosides and oligonucleosides 失效
    氨基甲酸酯衍生的核苷和寡核苷

    公开(公告)号:US06803198B2

    公开(公告)日:2004-10-12

    申请号:US09934138

    申请日:2001-08-21

    IPC分类号: C12Q168

    摘要: Nucleosides and oligonucleosides functionalized to include carbamate functionality, and derivatives thereof. In certain embodiments, the compounds of the invention further include steroids, reporter molecules, reporter enzymes, lipophilic molecules, peptides or proteins attached to the nucleosides through the carbamate group.

    摘要翻译: 功能化为包括氨基甲酸酯官能团的核苷和寡核苷酸及其衍生物。 在某些实施方案中,本发明的化合物还包括通过氨基甲酸酯基团连接到核苷上的类固醇,报道分子,报道酶,亲脂性分子,肽或蛋白质。

    2′-O-aminoethyloxyethyl-modified oligonucleotides
    8.
    发明授权
    2′-O-aminoethyloxyethyl-modified oligonucleotides 有权
    2'-O-氨基乙氧基乙基修饰的寡核苷酸

    公开(公告)号:US06673912B1

    公开(公告)日:2004-01-06

    申请号:US10121135

    申请日:2002-04-11

    IPC分类号: C07H2100

    摘要: 2′-O-Modified ribosyl nucleosides and modified oligomeric compounds containing such nucleosidic monomers are disclosed. Oligomeric compounds are disclosed that have increased binding affinity as shown by molecular modeling experiments. The 2′-O-modified nucleosides of the invention include ring structures that position the sugar moiety of the nucleosides preferentially in 3′ endo geometries.

    摘要翻译: 公开了2'-O-修饰的核糖基核苷和含有这种核苷单体的改性低聚化合物。 公开了具有增强的结合亲和力的低聚化合物,如分子模拟实验所示。 本发明的2'-O-修饰的核苷包括将核苷的糖部分优先置于3'内部几何形状的环结构。

    Oligonucleotides having site specific chiral phosphorothioate internucleoside linkages
    9.
    发明授权
    Oligonucleotides having site specific chiral phosphorothioate internucleoside linkages 有权
    具有位点特异性手性硫代磷酸酯核苷间键的寡核苷酸

    公开(公告)号:US06440943B1

    公开(公告)日:2002-08-27

    申请号:US09352058

    申请日:1999-07-14

    IPC分类号: A61K3170

    CPC分类号: C07H21/00 C07H19/04

    摘要: Novel chiral compounds that mimic and/or modulate the activity of wild-type nucleic acids are disclosed. In general, the compounds are phosphorothioate oligonucleotides wherein the 5′, and the 3′-terminal internucleoside linkages are chirally Sp and internal internucleoside linkages are chirally Rp.

    摘要翻译: 公开了模拟和/或调节野生型核酸活性的新型手性化合物。 通常,化合物是硫代磷酸酯寡核苷酸,其中5'和3'末端核苷间键是手性Sp,内部核苷间键是手性Rp。