Substituted purines and oligonucleotide cross-linking
    5.
    发明授权
    Substituted purines and oligonucleotide cross-linking 失效
    取代嘌呤和寡核苷酸交联

    公开(公告)号:US06232463B1

    公开(公告)日:2001-05-15

    申请号:US09128508

    申请日:1998-08-04

    IPC分类号: C07H2102

    CPC分类号: C07H19/16 C07H19/20 C07H21/00

    摘要: This invention is directed to novel purine-based compounds for inclusion into oligonucleotides. The compounds of the invention, when incorporated into oligonucleotides are especially useful as “antisense” agents—agents that are capable of specific hybridization with a nucleotide sequence of an RNA. The compounds of the invention may also be used for cross-linking oligonucleotides. Oligonucleotides are used for a variety of therapeutic and diagnostic purposes, such as treating diseases, regulating gene expression in experimental systems, assaying for RNA and for RNA products through the employment of antisense interactions with such RNA, diagnosing diseases, modulating the production of proteins, and cleaving RNA in site specific fashions. The compounds of the invention include novel heterocyclic bases, nucleosides, and nucleotides. when incorporated into oligonucleotides, the compounds of the invention can be useful for modulating the activity of RNA.

    摘要翻译: 本发明涉及用于包含在寡核苷酸中的新型基于嘌呤的化合物。 当掺入寡核苷酸时,本发明的化合物特别可用作能够与RNA的核苷酸序列特异性杂交的“反义”试剂。 本发明的化合物也可用于交联寡核苷酸。 寡核苷酸用于各种治疗和诊断目的,例如通过使用与这种RNA的反义相互作用来治疗疾病,调节实验系统中的基因表达,测定RNA和RNA产物,诊断疾病,调节蛋白质的产生, 并在现场具体时尚中切割RNA。 本发明化合物包括新的杂环碱基,核苷和核苷酸。 当掺入寡核苷酸时,本发明的化合物可用于调节RNA的活性。

    Conformationally constrained L-nucleosides
    8.
    发明授权
    Conformationally constrained L-nucleosides 有权
    构象约束的L-核苷

    公开(公告)号:US06525191B1

    公开(公告)日:2003-02-25

    申请号:US09569183

    申请日:2000-05-11

    申请人: Kanda S. Ramasamy

    发明人: Kanda S. Ramasamy

    IPC分类号: C07H19056

    CPC分类号: C07H19/056 C07H19/04

    摘要: L-nucleosides are conformationally constrained by at least one additional ring formed by a bridge connecting at least two atoms within a sugar moiety of the nucleoside. While a single additional ring is formed by bridging C1-C4 atoms, two additional rings are formed by bridging both C1-C2, and C3-C4 atoms, or C1-C3 and C2-C4 atoms by bridges having the general structure A—B—Z. The conformationally constrained nucleosides may be incorporated into oligonucleotides and dinucleotides, and it is contemplated that compositions including the conformationally constrained nucleosides may have superior viral inhibitory or antineoplastic properties.

    摘要翻译: L-核苷由至少一个通过连接至核苷糖的糖部分中的至少两个原子的桥形成的另外的环构型约束。 虽然通过桥接C1-C4原子形成单个另外的环,但是通过用具有一般结构A-B-Z的桥桥接C1-C2和C3-C4原子,或C1-C3和C2-C4原子,形成另外两个环。 可以将构象约束的核苷掺入寡核苷酸和二核苷酸,并且预期包含构象约束的核苷的组合物可具有优异的病毒抑制或抗肿瘤性质。

    Nucleoside compounds
    9.
    发明授权
    Nucleoside compounds 有权
    核苷化合物

    公开(公告)号:US06495677B1

    公开(公告)日:2002-12-17

    申请号:US09594410

    申请日:2000-06-16

    IPC分类号: C07H1904

    摘要: Nucleosides, novel nucleoside analog compounds and their novel prodrug forms are disclosed. The novel compounds, prodrugs, or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.

    摘要翻译: 公开了核苷,新型核苷类似物化合物及其新型前体药物形式。 其新颖化合物,前体药物或其药学上可接受的酯或盐可用于药物组合物中,并且此类组合物可用于治疗感染,感染,肿瘤或自身免疫性疾病。 新化合物也可用于调节免疫系统的方面,包括调节1型和2型活性。