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    Phosphonic acid based prodrugs of PMEA and its analogues
    75.
    发明授权
    Phosphonic acid based prodrugs of PMEA and its analogues 有权
    基于磷酸的前药PMEA及其类似物

    公开(公告)号：US07214668B2

    公开(公告)日：2007-05-08

    申请号：US10436922

    申请日：2003-05-12

    申请人： K. Raja Reddy ,  Mark D. Erion ,  Michael C. Matelich ,  Joseph J. Kopcho

    发明人： K. Raja Reddy ,  Mark D. Erion ,  Michael C. Matelich ,  Joseph J. Kopcho

    IPC分类号： C07F9/6574 ,  A61K31/675 ,  A61P31/20 ,  A61P31/14 ,  A61P35/00

    CPC分类号： C07F9/65742 ,  C07F9/65616

    摘要： Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, (R)-9-(2-phosphonylmethoxy propyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, 9-(2-phosphonylmethoxy ethyloxy)adenine, 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine, 9-(3-hydroxy-2-phosphonylmethoxypropyl)guanine, and (S)-9-(3-fluoro-2-phosphonyl methoxypropyl)adenine; V is selected from a group consisting of phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-furanyl, 3-furanyl, 2-thienyl, and 3-thienyl, all optionally substituted with 1-3 substituents selected from a group consisting of F, Cl, Br, C1-C3 alkyl, CF3 and OR6; R6 is selected from the group consisting of C1-C3 alkyl, and CF3; and pharmaceutically acceptable salts thereof.

    摘要翻译： 描述了式I的前药，其用途及其中间体及其制备方法：其中：M和V彼此是顺式的，MPO 3 H 2是 选自9-（2-膦酰基甲氧基乙基）腺嘌呤，（R）-9-（2-膦酰基甲氧基丙基）腺嘌呤，9-（2-膦酰基甲氧基乙基）鸟嘌呤，9-（2-膦酰基甲氧基乙氧基）腺嘌呤， 9-（3-膦酰基甲氧基乙基）-2,6-二氨基嘌呤，（S）-1-（3-羟基-2-膦酰基甲氧基丙基）胞嘧啶，（S）-9-（3-羟基-2-膦酰基甲氧基丙基）腺嘌呤， （3-羟基-2-膦酰基甲氧基丙基）鸟嘌呤和（S）-9-（3-氟-2-膦酰基甲氧基丙基）腺嘌呤; V选自苯基，2-吡啶基，3-吡啶基，4-吡啶基，2-呋喃基，3-呋喃基，2-噻吩基和3-噻吩基，全部任选被1-3个选自 由F，Cl，Br，C 1 -C 3烷基，CF 3 3和OR 6构成的基团。 R 6选自C 1 -C 3烷基和CF 3 N; 及其药学上可接受的盐。