FIELD: chemistry.
SUBSTANCE: invention relates to novel compounds of formula (I) and oligonucleotides obtained therefrom. In particular, present invention relates to a compound of formula (I)
where one of T1 and T2 is OR1 or OR2; and the other of T1 and T2 is OR1 or OR2; where R1 is H or a hydroxyl-protective group, wherein said hydroxyl-protective group is independently selected in each case from acetyl, benzyl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl, trityl, 4-monomethoxytrityl, 4,4'-dimethoxytrityl (DMTr), 4,4',4''-trimethoxytrityl (TMTr), 9-phenylxanthine-9-yl (pixyl) and 9-(p-methoxyphenyl)xanthin-9-yl (MOX), and R2 is a phosphorus-containing moiety, wherein said phosphorus-containing moiety is a phosphoramidite moiety of formula (X)
where R5 is C1-C9 alkyl substituted with cyano; R6 and R7 are independently C1-C9 alkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, where said heterocyclic ring is selected from pyrrolidinyl, piperidinyl or morpholinyl, where said heterocyclic ring is optionally substituted with C1-C3 alkyl; and where Bx is a purine base or a pyrimidine base.
EFFECT: novel oligonucleotides are obtained, which can be used as an antisense agent for preventing or treating a disease, where said disease is muscular dystrophy, preferably Duchenne muscular dystrophy.
24 cl, 12 tbl, 59 ex, 12 dwg
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