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130 条记录 (耗时 0.064 秒)

    Piperidine compounds
    81.
    发明授权
    Piperidine compounds 失效
    哌啶化合物

    公开(公告)号：US5994377A

    公开(公告)日：1999-11-30

    申请号：US955564

    申请日：1997-10-17

    申请人： Choung U. Kim ,  Matthew A. Williams

    发明人： Choung U. Kim ,  Matthew A. Williams

    IPC分类号： A61K31/44 ,  C07D211/72 ,  C07D211/74 ,  C07D211/68 ,  A61K31/435

    CPC分类号： C07D211/74 ,  A61K31/44 ,  C07D211/72

    摘要： Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

    摘要翻译： 描述了新的化合物。 化合物通常包含酸性基团，碱性基团，取代的氨基或N-酰基和具有任选羟基化的烷烃部分的基团。 还描述了包含本发明抑制剂的药物组合物。 还描述了怀疑含有神经氨酸酶的样品中抑制神经氨酸酶的方法。 还描述了抗原物质，聚合物，抗体，本发明化合物与标记物的缀合物，以及用于检测神经氨酸酶活性的测定方法。

    Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
    82.
    发明授权
    Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability 有权
    具有增加的口服生物利用度的抗病毒膦酰基甲氧基核苷酸类似物

    公开(公告)号：US5977089A

    公开(公告)日：1999-11-02

    申请号：US187763

    申请日：1998-11-06

    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： 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 -C.sub.12 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： 提供了包含具有结构-OC（R 2）2 OC（O）X（R）a的碳酸酯和/或氨基甲酸酯的抗病毒膦基甲氧基核苷酸类似物的酯的化合物，其中R2独立地是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，芳基烯基或芳基烷基，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。

    Thiepane compounds
    83.
    发明授权
    Thiepane compounds 失效
    噻哩啶化合物

    公开(公告)号：US5705524A

    公开(公告)日：1998-01-06

    申请号：US473876

    申请日：1995-06-07

    申请人： Lawrence R. McGee ,  Choung U. Kim ,  Norbert W. Bischofberger ,  Steven Krawczyk

    发明人： Lawrence R. McGee ,  Choung U. Kim ,  Norbert W. Bischofberger ,  Steven Krawczyk

    IPC分类号： C07D337/04 ,  C07D495/04 ,  A61K31/38

    CPC分类号： C07D495/04 ,  C07D337/04

    摘要： Tri- and tetra substituted thiepane and compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.

    摘要翻译： 公开了三 - 和四取代的硫代环烷和作为免疫原，治疗，诊断和其他工业目的使用的组合物。 组合物抑制病毒酶的蛋白水解活性，并且可用于抑制这些酶以及用于检测这些酶的测定。 其中抗原性多肽与组合物结合的实施方案可用于产生针对硫替平半抗原或多肽的抗体。 本发明的标记的thiepane可用作诊断试剂。