公开(公告)号：EP0885237A1

公开(公告)日：1998-12-23

申请号：EP97905245.0

申请日：1997-02-24

申请人： Novartis AG

发明人： BAXTER, Anthony David ,  COLLINGWOOD, Stephen Paul ,  DOUGLAS, Mark Edward ,  TAYLOR, Roger John

IPC分类号： C12N15 ,  A61K31 ,  A61K48 ,  A61P31 ,  A61P35 ,  C07H21

CPC分类号： C07H21/00

摘要： An oligonucleotide analogue having 10 to 200 natural and/or synthetic nucleoside units, linked by internucleoside linkages, at least one of the internucleoside linkages being of formula (I), where the indicated methylene group is attached to a 3' carbon atom of a nucleoside, the indicated oxygen atom is attached to a 5' carbon atom of an adjacent nucleoside, R1 is hydrogen, hydroxy, O-, thiol, S-, -NH2 or a group of formula R1a, -OR1a, -SR1a, -NHR1b or -NR1bR1c where R1a is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C3 to C8 cycloalkyl, C6 to C10 aryl or C7 to C13 aralkyl group and R1b and R1c are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C3 to C8 cycloalkyl, C6 to C10 aryl or C7 to C13 aralkyl group or R1b and R1c together with the nitrogen atom to which they are attached denote a five- or six-membered heterocyclic ring, and X is oxygen or sulphur.

摘要翻译： 具有10至200个通过核苷间键连接的天然和/或合成的核苷单元的寡核苷酸类似物，其中所述核苷间键中的至少一个是式（I），其中所示的亚甲基连接至核苷的3'碳原子 所示氧原子连接到相邻核苷的5'碳原子上，R 1是氢，羟基，O-，硫醇，S - ， - NH 2或式R 1a，-OR 1a，-SR 1a，-NHR 1b或 -NR1bR1c，其中R1a为未取代或取代的C1至C10烷基，C2至C10烯基，C3至C8环烷基，C6至C10芳基或C7至C13芳烷基，R1b和R1c各自独立地为未取代或取代的C1至C10烷基， C2至C10烯基，C3至C8环烷基，C6至C10芳基或C7至C13芳烷基或R1b和R1c与它们所连接的氮原子一起表示五元或六元杂环，并且X为氧或 硫。