CPG-OLIGONUCLEOTIDE ANALOGUES CONTAINING HYDROPHOBIC T-ANALOGUES WITH STRENGTHENED IMMUNITY AND MULTI-ACTIVITY

摘要

1. An oligonucleotide containing the sequence R1YZR2, where R1 and R2 are selected from the group consisting of a lipophilic substituted nucleotide analog (L), a nucleotide and a bond, where at least one of R1 and R2 is a lipophilic substituted nucleotide analog (L), where Y represents a pyrimidine nucleotide, and where Z represents purine, pyrimidine or a residue lacking a nitrogenous base. ! 2. The oligonucleotide according to claim 1, where L contains a 5- or 6-membered ring analog of the nucleic base. ! 3. The oligonucleotide according to claim 1, where L contains a group of formula I! ! where A, B, X, D, E and F are selected from C (carbon) or N (nitrogen), possibly bearing hydrogen or a substituent; ! n is 0 or 1; ! dashed lines indicate possible double bonds; ! where at least one substituent is not selected from the group consisting of oxo, thio, hydroxy, mercapto, imino, amino, methyl and hydrogen, and where in the aggregate of atoms A, B, X, D, E and F there are no more than 3 nitrogen atoms (N). ! 4. The oligonucleotide according to claim 3, where:! 1) n is 1; or ! 2) n is 0; or ! 3) all atoms A, B, X, D, E, F are carbon (C); or ! 4) one of the atoms A, B, X, D, E, F is nitrogen (N); or ! 5) two atoms A, B, X, D, E, F represent nitrogen (N); or ! 6) three atoms A, B, X, D, E, F represent nitrogen (N); or ! 7) at least one of the atoms A, B, X, D, E, F is substituted by a representative of the group consisting of F, Cl, Br, I, alkyl, alkenyl, alkynyl, halogenated alkyl, halogenated alkenyl, cycloalkyl, O- groups alkyl, O-alkenyl, -NH-alkyl, -N (alkyl) 2, -S-alkyl, -SO-alkyl, -SO2-alkyl, nitro, cyano, carboxyether, phenyl, thiophenyl, benzyl, oxo, thio, hydroxy , mercapto and imino, where at least one substituent is not oxo, �