发明公开
EP2854813A4 PYRAZOLOTRIAZOLYL NUCLEOSIDE ANALOGUES AND OLIGONUCLEOTIDES COMPRISING THEM
有权
吡唑并三唑核苷寡核苷酸与寡核苷酸的关系
- 专利标题: PYRAZOLOTRIAZOLYL NUCLEOSIDE ANALOGUES AND OLIGONUCLEOTIDES COMPRISING THEM
- 专利标题(中): 吡唑并三唑核苷寡核苷酸与寡核苷酸的关系
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申请号: EP13798069申请日: 2013-05-30
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公开(公告)号: EP2854813A4公开(公告)日: 2016-01-27
- 发明人: TRUFFERT JEAN-CHRISTOPHE , LEFOIX MYRIAM , HILDESHEIM JEAN , KLEINMAN TIRTSA
- 申请人: BIO LAB LTD
- 专利权人: BIO LAB LTD
- 当前专利权人: BIO LAB LTD
- 优先权: US201261653528 2012-05-31
- 主分类号: A61K31/53
- IPC分类号: A61K31/53 ; C07D487/04
摘要:
The present invention relates to pyrazolotriazolyl nucleoside analogues, oligonucleotide comprising them, and uses thereof. Further the invention relates to a method for reducing gene expression in a cell comprising transfecting the cell with such an oligonucleotide. It has been found, in accordance with the present invention, that certain pyrazolotriazolyl-based nucleoside analogues such as 8-[3′-(2-cyanoethyl)-(N,Ndiisopropyl)]-phosphoramidite-(2′-deoxy-5′-dimethoxytrity 1-13-D-ribofuranozyl)-4-{N-benzoylamino)-pyrazolo[1,5a]-1,3,5-triazine, can be incorporated into oligonucleotides, substituting natural purine nucleosides and imparting acid stability and nuclease stability to the oligonucleotide. Furthermore, oligonucleotides comprising one or more such nucleoside analogues are capable of hybridizing with oligonucleotides having complementary sequences thereto in which no such analogues are incorporated.
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