发明名称 Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
摘要 Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure -OC(R2)2OC(O)X(R)a, wherein R2 independently is H, C1-C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR3 in which R3 is C1-C12 alkyl; X is N or O; R is independently H, C1-C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, -O-, -N=, -NR4-, -N(R4)2- or OR3, R4 independently is -H or C1-C8 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 OR3. 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.
申请公布号 US5922695(A) 申请公布日期 1999.07.13
申请号 US19970900746 申请日期 1997.07.25
申请人 GILEAD SCIENCES, INC. 发明人 ARIMILLI, MURTY N.;CUNDY, KENNETH C.;DOUGHERTY, JOSEPH P.;KIM, CHOUNG U.;OLIYAI, REZA;STELLA, VALENTINO J.
分类号 C07F9/6512;C07F9/6561;(IPC1-7):A61K31/675;C07F9/651;C07F9/656 主分类号 C07F9/6512
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