C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 21/00 (2006.01) C12Q 1/68 (2006.01)
Patent
CA 2201963
Novel oligonucleotides are provided having cationic internucleoside linkages. The cationic internucleoside linkage has structure (I), wherein W, X, Y, Z, R1, R2 and R3 are as defined herein, P* represents an asymetric phosphorus atom capable of existing in two distinct stereoisomeric configurations, and further wherein the internucleoside linkage is stereouniform. Certain of these oligonucleotides may have alternating anionic and cationic internucleoside linkages, which are not necessarily stereouniform. A method for synthesizing the compounds are provided as well, as are methods for using the compounds, e.g., as antisense molecules and in nucleic acid hybridization assays.
On décrit des nouveaux oligonucléotides présentant des liaisons internucléosides cationiques, lesquelles possèdent la structure (I) dans laquelle W, X, Y, Z, R?1¿, R?2¿ et R?3¿ ont la signification donnée dans la description, P* représente un atome de phosphore asymétrique pouvant exister dans deux configurations stéréo-isomères distinctes, et dans laquelle la liaison internucléoside est stéréo-uniforme. Certains de ces oligonucléotides peuvent présenter des liaisons internucléosides anioniques et cationiques alternantes, lesquelles ne sont pas nécessairement stéréo-uniformes. On décrit également un procédé de synthèse de ces composés, de même que des procédés d'utilisation de ceux-ci, par exemple en tant que molécules antisens et dans des dosages par hybridation d'acides nucléiques.
Balasubramaniam Tanjore Narayanaswamy
Horn Thomas
Letsinger Robert L.
Borden Ladner Gervais Llp
Chiron Corporation
Northwestern University
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