Nucleotide analogues as precursor molecules for antivirals
    1.
    发明授权
    Nucleotide analogues as precursor molecules for antivirals 有权
    核苷酸类似物作为抗病毒药物的前体分子

    公开(公告)号:US08884011B2

    公开(公告)日:2014-11-11

    申请号:US12514285

    申请日:2007-11-08

    IPC分类号: C07F9/02 C07F9/6561

    CPC分类号: C07F9/65616

    摘要: This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for testing and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H-phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.

    摘要翻译: 本发明涉及式(I)的嘌呤或嘧啶膦酸酯化合物或其药学上可接受的盐; 其中B,X和R 1 -R 3如本文中的类别和子类所定义。 这些化合物可以用作抗病毒前体。 本发明还涉及这些化合物的治疗组合物及其用于制备用于测试和/或预防患者病毒感染的药物的用途。 本发明还提供了制备这些化合物的方法。 特别地,本发明提供了式(II)的H-次膦酸盐前体中间体,其中B是如本文所定义的嘌呤或嘧啶碱基,R 1选自氢原子和甲基,乙基,羟甲基,羟乙基和 C 1-6卤代烷基。

    NOVEL NUCLEOTIDE ANALOGUES AS PRECUSOR MOLECULES FOR ANTIVIRALS
    2.
    发明申请
    NOVEL NUCLEOTIDE ANALOGUES AS PRECUSOR MOLECULES FOR ANTIVIRALS 有权
    新型核苷酸类似物作为抗病毒剂的分子分子

    公开(公告)号:US20100099869A1

    公开(公告)日:2010-04-22

    申请号:US12514285

    申请日:2007-11-08

    IPC分类号: C07F9/02

    CPC分类号: C07F9/65616

    摘要: This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for testing and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H-phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.

    摘要翻译: 本发明涉及式(I)的嘌呤或嘧啶膦酸酯化合物或其药学上可接受的盐; 其中B,X和R 1 -R 3如本文中的类别和子类所定义。 这些化合物可以用作抗病毒前体。 本发明还涉及这些化合物的治疗组合物及其用于制备用于测试和/或预防患者病毒感染的药物的用途。 本发明还提供了制备这些化合物的方法。 特别地,本发明提供了式(II)的H-次膦酸盐前体中间体,其中B是如本文所定义的嘌呤或嘧啶碱基,R 1选自氢原子和甲基,乙基,羟甲基,羟乙基和 C 1-6卤代烷基。

    Nucleoside aryl phosphoramidates and their use as anti-viral agents for the treatment of hepatitis C virus
    6.
    发明授权
    Nucleoside aryl phosphoramidates and their use as anti-viral agents for the treatment of hepatitis C virus 失效
    核苷芳基氨基磷酸酯及其作为抗病毒药物用于治疗丙型肝炎病毒的用途

    公开(公告)号:US08658616B2

    公开(公告)日:2014-02-25

    申请号:US12516253

    申请日:2007-11-23

    CPC分类号: C07H19/20

    摘要: Compounds having the general formula (I): are provided which have enhanced inhibitory potency and are thus useful in methods of prophylaxis or treatment of a viral infection such as hepatitis C virus. The compounds are phosphoramidate derivatives of nucleoside compounds derived from bases such as adenine and guanine. The glycoside moiety of the nucleoside compound can be substituted at the ss-2′ position with methyl and the phosphoramidate group can be 1-naphthyl linked by —O— to the P atom. These compounds can be administered as pharmaceutical compositions, and methods for their preparation are also provided.

    摘要翻译: 提供具有通式(I)的化合物,其具有增强的抑制效力,因此可用于预防或治疗病毒感染如丙型肝炎病毒的方法。 这些化合物是衍生自诸如腺嘌呤和鸟嘌呤的碱的核苷化合物的氨基磷酸衍生物。 核苷化合物的糖苷部分可以在β-2'位被甲基取代,氨基磷酸酯基可以通过-O-连接到P原子上的1-萘基。 这些化合物可以作为药物组合物施用,并且还提供了它们的制备方法。

    Imidazo[4,5-d]pyrimidines, their uses and methods of preparation
    8.
    发明授权
    Imidazo[4,5-d]pyrimidines, their uses and methods of preparation 有权
    咪唑并[4,5-d]嘧啶,其用途和制备方法

    公开(公告)号:US07790730B2

    公开(公告)日:2010-09-07

    申请号:US11190751

    申请日:2005-07-26

    摘要: The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one compound having the general formula (A): wherein U is N or C; X is selected from C1-C10 alkylene, C2-10 alkenylene or C2-10 alkynylene, where each may include one or more intrachain heteroatoms selected from O, S, or NR11, provided any such heteroatom is not adjacent to the N in the ring; R3 is selected from aryl, aryloxy, arylthio, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl-N(R10)—, or heterocycle, where each said substituent is optionally substituted with at least one R17, provided that for cycloalkenyl the double bond is not adjacent to a nitrogen; and the other substituents are described in the specification. The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula, their pharmaceutically acceptable formulations and their use as a medicine or to treat or prevent viral infections.

    摘要翻译: 本发明涉及用于治疗或预防病毒感染的药物组合物,其包含至少一种具有通式(A)的化合物作为活性成分:其中U为N或C; X选自C1-C10亚烷基,C2-10亚烯基或C2-10亚炔基,其中每个可以包括一个或多个选自O,S或NR 11的链内杂原子,条件是任何这样的杂原子不与环中的N相邻 ; R 3选自芳基,芳氧基,芳硫基,环烷基,环烯基,环炔基,芳基-N(R 10) - 或杂环,其中每个所述取代基任选被至少一个R 17取代,条件是对于环烯基,双键不相邻 到氮气 并且其它取代基在说明书中描述。 本发明还涉及制备具有上述通式的本发明化合物及其药学上可接受的制剂及其作为药物的用途或用于治疗或预防病毒感染的化合物的方法。