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61. 发明授权

US6043230A Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability 有权
标题翻译：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。

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