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公开(公告)号：EP1812569A2
公开(公告)日：2007-08-01
申请号：EP05804121.1
申请日：2005-11-08
IPC分类号： C12N15/11
CPC分类号： C12N15/111 , A61K31/712 , C07D487/04 , C12N15/1138 , C12N2310/14 , C12N2310/323 , C12N2320/51 , C12N2330/30
摘要： The present invention relates to the use of modified nucleotides and single or double stranded oligonucleotides comprising at least one of said modified nucleotides for performing RNA interference. The modified nucleotides are selected from 6-membered ring containing nucleotides such as hexitol, altritol, O-subsituted or O-alkylated altritol, cyclohexenyl, ribo-cyclohexenyl and O-subsituted or O-alkylated ribo-cyclohexenyl nucleotides. The present invention also relates to novel modified nucleosides or nucleotides and to the use of said novel modified nucleosides and nucleotides in single or double stranded oligonucleotides for RNA interference, antisense therapy or other applications.
摘要翻译： 本发明涉及修饰的核苷酸和包含至少一个所述修饰的核苷酸的单链或双链寡核苷酸用于进行RNA干扰的用途。 修饰的核苷酸选自含有6员环的核苷酸，例如己糖醇，阿卓糖醇，O-取代的或O-烷基化的阿卓糖醇，环己烯基，核 - 环己烯基和O-取代的或O-烷基化的核 - 环己烯基核苷酸。 本发明还涉及新的修饰的核苷或核苷酸以及所述新的修饰的核苷和核苷酸在单链或双链寡核苷酸中用于RNA干扰，反义治疗或其他应用的用途。
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公开(公告)号：EP1370539A1
公开(公告)日：2003-12-17
申请号：EP01919343.2
申请日：2001-02-23
发明人： DE CLERCQ, Erik , VAN AERSCHOT, Arthur , HERDEWIJN, Piet , LAGOJA, Irene , PANNECOUCQUE, Christophe
IPC分类号： C07D233/84 , A61K31/415 , C07D233/90 , C07D233/54 , A61P31/12 , A61P31/18
CPC分类号： C07D233/54
摘要： An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or -SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl. This invention further relates to the use of compounds of formula (I) as agents having biological activity, especially against viral infections.
摘要翻译： 一种N-氨基咪唑或N-氨基咪唑硫酮衍生物，其药学上可接受的盐，互变异构体，异构体，酯或糖基化产物，所述衍生物由通式（I）表示：其中m = 0或1，n = 0或 1，R1选自氢，甲基或乙基，R2选自氢，SH或-SR0，其中R0为甲基，苄基或葡萄糖残基; Q选自1-萘基，2-萘基，联苯基，2-吡啶基，3-吡啶基，4-吡啶基，2-嘧啶基，4-嘧啶基，5-嘧啶基，噻吩基或取代或未取代的苯环，其中 取代理解为选自H，F，Cl，Br，I，甲基，乙基或异丙基的一个或两个取代基; L选自1-萘基，2-萘基，联苯基，2-吡啶基，3-吡啶基，4-吡啶基，2-嘧啶基，4-嘧啶基，5-嘧啶基，噻吩基或取代或未取代的苯环， 理解为选自H，F，Cl，Br，I，甲基，乙基或异丙基的一个或两个取代基。 本发明进一步涉及式（I）化合物作为具有生物活性，特别是抗病毒感染的药剂的用途。
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公开(公告)号：EP1370539B1
公开(公告)日：2011-11-09
申请号：EP01919343.2
申请日：2001-02-23
发明人： DE CLERCQ, Erik , VAN AERSCHOT, Arthur , HERDEWIJN, Piet , LAGOJA, Irene , PANNECOUCQUE, Christophe
IPC分类号： C07D233/84 , A61K31/415 , C07D233/90 , C07D233/54 , A61P31/12 , A61P31/18
CPC分类号： C07D233/54
摘要： An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or -SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl. This invention further relates to the use of compounds of formula (I) as agents having biological activity, especially against viral infections.
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