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    AZA nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
    8.
    发明授权
    AZA nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases 有权
    AZA核苷，其制备及用作RNA病毒聚合酶的抑制剂

    公开(公告)号：US07560434B2

    公开(公告)日：2009-07-14

    申请号：US11157867

    申请日：2005-06-22

    申请人： Yarlagadda S. Babu ,  Pooran Chand ,  Ajit K. Ghosh ,  Pravin L. Kotian ,  V. Satish Kumar

    发明人： Yarlagadda S. Babu ,  Pooran Chand ,  Ajit K. Ghosh ,  Pravin L. Kotian ,  V. Satish Kumar

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07D487/04 ,  C07D491/048 ,  C07F9/6561

    摘要： Compounds represented by the formula: and pharmaceutically acceptable salts thereof and prodrugs thereof; wherein R1 is H, CH3, C2H5, C3H7 R2 is H, CH3, C2H5, C3H7, CH═CH2, CH2—OH, CH2F, CF3 R′2 is H, OH, NH2, NH-alkyl, F, N3, OCH3, O—C(O)CH(NH2)alkyl R3 is H, CH3, C2H5, C3H7 R′3 is H, OH, NH2, NH-alkyl, F, N3, OCH3, O—C(O)CH(NH2)alkyl R4 is H, CH3, C2H5, C3H7 At least one of R2, R3, or R4has to be other than H, when X═NH in B R6 is H, CH3, C2H5, R7 is selected from H, alkyl, alkenyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl, aminoacids, CH2CH2SC(O)alkyl; and B is represented by the following structure: X is independently NR6, O, S, R8 and R9 independently is H, NH2, OH, SH, F, Cl, Br, I, aryl, heterocycle, alkyl, alkene, alkyne, S-alkyl, S-aryl, S(O)-alkyl, SO2-alkyl, SO2NH2, SO2NH-alkyl, SO2NH-aryl, NH-alkyl, NH-aryl, N(alkyl)2, N(aryl)2, O-alkyl, O-aryl, O-heterocycle, NH-(CH2)n-aryl, NH—C(O)-alkyl, NH—C(O)-aryl are useful for inhibiting viral RNA polymerases and treating patients suffering from diseases caused by various RNA viruses.

    摘要翻译： 由下式表示的化合物及其药学上可接受的盐及其前药; 其中R1是H，CH3，C2H5，C3H7R2是H，CH3，C2H5，C3H7，CH-CH2，CH2-OH，CH2F，CF3R'2是H，OH，NH2，NH-烷基，F，N3，OCH3 ，OC（O）CH（NH2）烷基R3是H，CH3，C2H5，C3H7，R'3是H，OH，NH2，NH-烷基，F，N3，OCH3，OC（O）CH（NH2） H，CH 3，C 2 H 5，C 3 H 7当R 6中的X-NH为H时，R 2，R 3或R 4中的至少一个为H，当H，CH 3，C 2 H 5，R 7选自H，烷基，烯基，芳基，酰氧基烷基 ，和新戊酰氧基烷基，氨基酸，CH 2 CH 2 SC（O）烷基; 并且B由以下结构表示：X独立地是NR6，O，S，R8和R9独立地是H，NH2，OH，SH，F，Cl，Br，I，芳基，杂环，烷基，烯烃，炔， - 烷基，S-芳基，S（O） - 烷基，SO 2 - 烷基，SO 2 NH 2，SO 2 NH-烷基，SO 2 NH-芳基，NH-烷基，NH-芳基，N（烷基）2，N（芳基） 烷基，O-芳基，O-杂环，NH-（CH2）n-芳基，NH-C（O） - 烷基，NH-C（O） - 芳基可用于抑制病毒RNA聚合酶和治疗患有疾病的患者 通过各种RNA病毒。