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    Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
    2.
    发明授权
    Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability 失效
    具有增加的口服生物可变性的抗病毒膦酰基氧基核苷酸类似物

    公开(公告)号：US5922695A

    公开(公告)日：1999-07-13

    申请号：US900746

    申请日：1997-07-25

    申请人： Murty N. Arimilli ,  Kenneth C. Cundy ,  Joseph P. Dougherty ,  Choung U. Kim ,  Reza Oliyai ,  Valentino J. Stella

    发明人： Murty N. Arimilli ,  Kenneth C. Cundy ,  Joseph P. Dougherty ,  Choung U. Kim ,  Reza Oliyai ,  Valentino J. Stella

    IPC分类号： C07F9/6512 ,  C07F9/6561 ,  A61K31/675

    CPC分类号： C07F9/65616 ,  C07F9/65121

    摘要： Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure --OC(R.sup.2).sub.2 OC(O)X(R).sub.a, wherein R.sup.2 independently is H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR.sup.3 in which R.sup.3 is C.sub.1 -C12 alkyl; X is N or O; R is independently H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, --O--, --N.dbd., --NR.sup.4 --, --N(R.sup.4).sub.2 -- or OR.sup.3, R.sup.4 independently is --H or C.sub.1 -C.sub.8 alkyl, provided that at least one R is not H; and a is 1 or 2, with the proviso that when a is 2 and X is N, (a) two R groups can be taken together to form a carbocycle or oxygen-containing heterocycle, or (b) one R additionally can be OR.sup.3. The compounds are useful as intermediates for the preparation of antiviral compounds or oligonucleotides, or are useful for administration directly to patients for antiviral therapy or prophylaxis. Embodiments are particularly useful when administered orally.

    摘要翻译： 提供新的化合物，其包含抗病毒膦基甲氧基核苷酸类似物与具有结构-OC（R 2）2 OC（O）X（R）a的碳酸酯和/或氨基甲酸酯的酯，其中R2独立地为H，C1-C12烷基，芳基，烯基 炔基，烷基芳基，炔基芳基，烷芳基，芳基炔基，芳基烯基或芳烷基，其未被取代或被卤素，叠氮基，硝基或OR 3取代，其中R 3是C 1 -C 12烷基; X为N或O; R是独立的H，C 1 -C 12烷基，芳基，烯基，炔基，链烯基芳基，炔基芳基，烷芳基，芳基炔基，芳基烯基或芳烷基，其未被取代或被卤素，叠氮基，硝基，-O - ， - N = - ， - N（R4）2-或OR3，R4独立地是-H或C1-C8烷基，条件是至少一个R不是H; 和a为1或2，条件是当a为2且X为N时，（a）两个R基团可以一起形成碳环或含氧杂环，或（b）一个R另外可以是OR 3 。 该化合物可用作制备抗病毒化合物或寡核苷酸的中间体，或可用于直接给患者施用抗病毒治疗或预防。 当口服给药时，实施方案特别有用。

    9-(2-phosphonylmethoxyethyl) guanine
    4.
    发明授权
    9-(2-phosphonylmethoxyethyl) guanine 失效
    9-（2-膦酰基甲氧基乙基）鸟嘌呤

    公开(公告)号：US5869467A

    公开(公告)日：1999-02-09

    申请号：US412398

    申请日：1995-03-28

    申请人： Antonin Holy ,  Ivan Rosenberg ,  Erik D. A. De Clercq

    发明人： Antonin Holy ,  Ivan Rosenberg ,  Erik D. A. De Clercq

    IPC分类号： A61K31/66 ,  A61K31/675 ,  A61P31/12 ,  C07F9/6512 ,  C07F9/6561

    CPC分类号： C07F9/65121 ,  C07F9/65616

    摘要： This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyolic bases and their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.

    摘要翻译： 本发明涉及新的核苷酸类似物，并且解决了它们用作生物活性化合物的技术问题。 本发明的主题是嘧啶和嘌呤碱基的N-（2-膦酰基甲氧基乙基）和N-（3-羟基-2-膦酰基甲氧基丙基）衍生物，其可以从异源碱基及其N-（2-羟乙基）或N-（ 2,3-二羟丙基）衍生物。 根据本发明的一些化合物显示出明显的抗病毒活性，或者可以通过化学转化转化成这些活性化合物。