公开(公告)号：US20080199960A1

公开(公告)日：2008-08-21

申请号：US11596238

申请日：2005-05-13

申请人： Rudolph L. Juliano ,  Hyunmin Kang ,  Anna Astriab-Fisher ,  Piet Herdewijn ,  Patrick Chaltin ,  Arthur Van Aerschot

发明人： Rudolph L. Juliano ,  Hyunmin Kang ,  Anna Astriab-Fisher ,  Piet Herdewijn ,  Patrick Chaltin ,  Arthur Van Aerschot

IPC分类号： C12N15/00 ,  C12N5/00

CPC分类号： C12N15/1138 ,  C07H21/04 ,  C12N15/111 ,  C12N2310/11 ,  C12N2310/14 ,  C12N2310/321 ,  C12N2310/322 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/3513 ,  C12N2310/3515 ,  C12N2310/53 ,  C12N2320/32 ,  C12N2320/51 ,  C12N2310/3521 ,  C12N2310/3525 ,  C12N2310/3527

摘要： The presently disclosed subject matter relates to the delivery of oligonucleotides to cells through the delivery of a composition or reagent comprising a hybridization complex comprising a first antisense oligonucleotide which is modified to have a higher stability against degradation, and a second sense oligonucleotide which is prone to degradation. The presently disclosed subject matter furthermore relates to dendrimeric bioconjugates and compositions or reagents comprising them, wherein the bioconjugate comprises a conjugate moiety coupled to a dendrimeric structure and to their use to deliver oligomeric compounds including oligonucleotides or duplexes, as described above, to cells for modulation of gene expression (i.e. antisense or antigene therapy/research, RNA interference).

摘要翻译： 目前公开的主题涉及通过递送包含杂交复合物的组合物或试剂递送寡核苷酸，所述杂交复合物包含经修饰以具有较高抗降解稳定性的第一反义寡核苷酸，以及易于 降解。 目前公开的主题还涉及含有它们的树枝状聚合生物共轭物和组合物或试剂，其中生物缀合物包含与树枝状大分子结构偶联的缀合物部分，以及它们用于将如上所述的寡核苷酸或双链体的寡聚化合物递送至用于调制的细胞 的基因表达（即反义或反向治疗/研究，RNA干扰）。

公开(公告)号：US20080261905A1

公开(公告)日：2008-10-23

申请号：US11718793

申请日：2005-11-08

申请人： Piet Herdewijn ,  Arthur Van Aerschot ,  Jing Wang ,  Rudy Juliano

发明人： Piet Herdewijn ,  Arthur Van Aerschot ,  Jing Wang ,  Rudy Juliano

IPC分类号： A61K31/70 ,  C07H21/00 ,  C07H21/04 ,  C12N5/06 ,  C07D311/00 ,  A61P43/00

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 having 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-substituted or O-alkylated altritol, cyclohexenyl, ribo-cyclohexenyl and O-substituted or O-alkylated ribo-cyclohexenyl nucleotides. The present invention also relates to novel modified nucleosides or nucleotides and to the use of the 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具有至少一个所述修饰的核苷酸用于进行RNA干扰的单链或双链寡核苷酸的用途。 修饰的核苷酸选自含6个元素的核苷酸，如己糖醇，阿糖醇，O-取代或O-烷基化的三羟甲基纤维素，环己烯基，核 - 环己烯基和O-取代或O-烷基化的核糖核苷酸。 本发明还涉及新的修饰的核苷或核苷酸，以及在单链或双链寡核苷酸中用于RNA干扰，反义治疗或其它应用的新的修饰的核苷和核苷酸的用途。

公开(公告)号：US20100009865A1

公开(公告)日：2010-01-14

申请号：US12443098

申请日：2007-10-01

申请人： Piet Herdewijn ,  Arthur Van Aerschot ,  Mikhail Abramov

发明人： Piet Herdewijn ,  Arthur Van Aerschot ,  Mikhail Abramov

IPC分类号： C40B30/04 ,  C40B50/18

CPC分类号： C07H19/06 ,  C07H19/16 ,  C07H21/00

摘要： The present invention provides for oligonucleotide arrays wherein the oligonucleotides comprise six-membered sugar-ring nucleosides, especially tetrahydropyran nucleosides, more specifically altritol nucleosides. The present invention also provides for the use of said oligonucleotide arrays for detecting target molecules in samples (diagnostic or experimental use). The present invention also provides for a method of detecting target molecules in samples by using said oligonucleotide arrays comprising six-membered sugar-ring nucleosides.

摘要翻译： 本发明提供了寡核苷酸阵列，其中寡核苷酸包含六元糖环核苷，特别是四氢吡喃核苷，更具体地说是阿糖醇核苷。 本发明还提供了用于检测样品中靶分子（诊断或实验用途）的所述寡核苷酸阵列的用途。 本发明还提供了通过使用包含六元糖环核苷的所述寡核苷酸阵列来检测样品中靶分子的方法。

公开(公告)号：US07049332B2

公开(公告)日：2006-05-23

申请号：US10468541

申请日：2001-02-23

申请人： Erik De Clercq ,  Arthur Van Aerschot ,  Piet Herdewijn ,  Irene Lagoja ,  Christophe Pannecoucque

发明人： Erik De Clercq ,  Arthur Van Aerschot ,  Piet Herdewijn ,  Irene Lagoja ,  Christophe Pannecoucque

IPC分类号： A61K31/415 ,  C07D233/38

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： 所述衍生物由通式（I）表示：其中m = 0或1，n = 0或 1，R 1选自氢，甲基或乙基，R 2选自氢，SH或-SR 0 O，其中R 0 > 0 是甲基，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基环，其中 取代被理解为选自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， 被理解为一个或两个选自H，F，Cl，Br，I，甲基，乙基或异丙基的取代基。 本发明还涉及式（I）化合物作为具有生物活性，特别是针对病毒感染的试剂的用途。