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    Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
    71.
    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：US6043230A

    公开(公告)日：2000-03-28

    申请号：US314606

    申请日：1999-05-19

    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, axido, 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，芳基烯基或芳基烷基，其未被取代或被卤素，轴酰基，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。

    Aromatic compounds
    74.
    发明授权
    Aromatic compounds 失效
    芳香族化合物

    公开(公告)号：US5512596A

    公开(公告)日：1996-04-30

    申请号：US300607

    申请日：1994-09-02

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

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

    IPC分类号： A61K31/045 ,  A61K31/192 ,  C07C65/01 ,  C07D213/79 ,  C07D233/54 ,  C07D239/28 ,  C07D263/32 ,  C07D307/68 ,  C07F9/38 ,  A61K31/19 ,  C07C63/06

    CPC分类号： C07D213/79 ,  A61K31/045 ,  A61K31/192 ,  C07C65/01 ,  C07D233/64 ,  C07D239/28 ,  C07D263/32 ,  C07D307/68 ,  C07F9/3834

    摘要： A composition comprising a compound of the formula: ##STR1## wherein: X is H or OH;Y is a group capable of hydrogen bonding to amino, guanidino, or imidazole function, or a group comprising an acidic hydrogen atom, a protected acidic group, or an anion;E is N or CR.sub.1, wherein R.sub.1 is H, OH, CN, F, Cl, Br, or I;A.sub.4, A.sub.5, and A.sub.6 are each independently N, CH, CR.sub.40 or CZ wherein R.sub.40 is R.sub.43, OR.sub.43, SR.sub.43, S(O)R.sub.43, S(O).sub.2 R.sub.43, or NR.sub.43 R.sub.44 wherein R.sub.43 comprises an alkyl of 1 to 3 carbon atoms, an acyl of 2 to 3 carbon atoms, or an alkyl of 1 to 3 carbon atoms substituted with an acyl of 2 to 3 carbon atoms, and R.sub.44 is H or an alkyl of 1 to 2 carbon atoms, and Z is a group capable of hydrogen bonding to carboxyl, or a group comprising a basic heteroatom, a protected basic heteroatom, or a cation.

    摘要翻译： 一种组合物，其包含下式化合物：其中：X为H或OH; Y是能够键合到氨基，胍基或咪唑官能团的基团，或包含酸性氢原子，被保护的酸性基团或阴离子的基团; E是N或CR1，其中R1是H，OH，CN，F，Cl，Br或I; A4，A5和A6各自独立地为N，CH，CR40或CZ，其中R40为R43，OR43，SR43，S（O）R43，S（O）2R43或NR43R44，其中R43包含1至3个碳原子的烷基 2〜3个碳原子的酰基，或被2〜3个碳原子的酰基取代的1〜3个碳原子的烷基，R44是H或1〜2个碳原子的烷基，Z是能够 与羧基键合的氢键，或包含碱性杂原子，受保护的碱性杂原子或阳离子的基团。