发明名称 PSEUDONUCLEOSIDES AND PSEUDONUCLEOTIDES AND THEIR POLYMERS
摘要 Pseudonucleosides and pseudonucleotides are useful in the synthesis of oligomers which contain these components as a means to derivatize the resulting oligonucleotide to useful substituents such as chelators, intercalators, or lipophilic compounds. In general, these pseudonucleotide components are of the formula: <IMAGE> (1) wherein each Y is independently O or S; each X is independently H, PO3-2, an activated nucleotide synthesis coupling moiety, a protecting group, a nucleoside, a nucleotide or a nucleotide sequence, or comprises a solid support; F is a functional group capable of linking an additional moiety or said group already reacted to effect the binding of said additional moiety; &squ& is an organic backbone which does not contain additional F or Y-X substituents and which is either achiral even when the Y-X substituents are different, or is a single enantiomer of a chiral compound; with the proviso that at least one X is a nucleoside, nucleotide, nucleotide sequence, an activated nucleotide synthesis coupling moiety, or comprises a solid support, or F represents said functional group already reacted with an additional group. Oligonucleotides having the pseudonucleoside at the 3' terminus are particularly stable in vivo.
申请公布号 AU7579991(A) 申请公布日期 1991.09.18
申请号 AU19910075799 申请日期 1991.02.20
申请人 GILEAD SCIENCES, INC. 发明人 KUEI-YING LIN;MARK MATTEUCCI
分类号 A61K47/48;C07C215/14;C07C217/10;C07C219/06;C07C225/34;C07C233/18;C07C233/36;C07D219/12;C07H21/00;C07J51/00 主分类号 A61K47/48
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