Compounds and methods for synthesis and therapy
    72.
    发明授权
    Compounds and methods for synthesis and therapy 有权
    用于合成和治疗的化合物和方法

    公开(公告)号:US06225341B1

    公开(公告)日:2001-05-01

    申请号:US09288091

    申请日:1999-04-08

    IPC分类号: A61K3135

    CPC分类号: C07D309/28 Y02P20/55

    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。

    Imidazo[4,5-d]pyrimidines, their uses and methods of preparation
    76.
    发明申请
    Imidazo[4,5-d]pyrimidines, their uses and methods of preparation 审中-公开
    咪唑并[4,5-d]嘧啶,其用途和制备方法

    公开(公告)号:US20090208456A1

    公开(公告)日:2009-08-20

    申请号:US11658625

    申请日:2005-07-26

    摘要: The present invention relates to pharmaceutical compositions for the treatment of prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyrimidine having the general formula (A), wherein the 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预防病毒感染的药物组合物,其包含作为活性成分的至少一种具有通式(A)的咪唑并[4,5-c]嘧啶,其中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。

    Antiviral phosphonomethyoxy nucleotide analogs having increased oral
bioavarilability
    78.
    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

    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。