发明授权
US5977089A 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
- 专利标题: Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
- 专利标题(中): 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
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申请号: US187763申请日: 1998-11-06
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公开(公告)号: US5977089A公开(公告)日: 1999-11-02
- 发明人: Murty N. Arimilli , Kenneth C. Cundy , Joseph P. Dougherty , Choung U. Kim , Reza Oliyai , Valentino J. Stella
- 申请人: Murty N. Arimilli , Kenneth C. Cundy , Joseph P. Dougherty , Choung U. Kim , Reza Oliyai , Valentino J. Stella
- 申请人地址: CA Foster City
- 专利权人: Gilead Sciences, Inc.
- 当前专利权人: Gilead Sciences, Inc.
- 当前专利权人地址: CA Foster City
- 主分类号: C07F9/6512
- IPC分类号: C07F9/6512 ; C07F9/6561 ; A61K31/675
摘要:
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 -C.sub.12 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.
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