Pyrazolotriazolyl nucleoside analogues and oligonucleotides comprising them
Номер патента: EP2854813A1
Опубликовано: 08-04-2015
Автор(ы): Jean Hildesheim, Jean-Christophe TRUFFERT, Myriam Lefoix, Tirtsa KLEINMAN
Принадлежит: BIO LAB Ltd, Bio-Lab Ltd
Опубликовано: 08-04-2015
Автор(ы): Jean Hildesheim, Jean-Christophe TRUFFERT, Myriam Lefoix, Tirtsa KLEINMAN
Принадлежит: BIO LAB Ltd, Bio-Lab Ltd
Реферат: 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 '-dimethoxytri ty 1-13-D-ri bofuranozyl )-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.
Pyrazolotriazolyl nucleoside analogues and oligonucleotides comprising them
Номер патента: WO2013179289A8. Автор: Jean Hildesheim,Tirtsa KLEINMAN,Jean-Christophe TRUFFERT,Myriam Lefoix. Владелец: Bio-Lab Ltd.. Дата публикации: 2014-01-16.