Novel bicyclic nucleosides and oligomers prepared therefrom
AssigneeUniversitäT Bern
InventorsChristian Leumann, Damien Evéquoz
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Abstract
Oligomers can be prepared from bicyclic nucleoside. The nucleosides can be a compound of formula (I) in which each of T1 and T2 is independently OR1 or OR2; R1 is H or a hydroxyl protecting group, R2 is a phosphorus moiety; and Bx is a nucleobase. The compounds, bicyclic nucleosides and oligomers are useful for the prevention, treatment or diagnosis of muscular dystrophy.
Claims22
A compound of formula (I):
- wherein
- T1 and T2 are each independently selected from the group consisting of OR1 and OR2;
- wherein
- R1 is H or a hydroxyl protecting group, and
- R2 is a phosphorus moiety;
- and wherein
- Bx is a nucleobase.
An oligomer comprising at least one monomer subunit as a compound of formula (IV)
- wherein
- either T3 or T4 is independently a nucleosidic linkage group;
- and when T3 is a nucleoside linkage group,
- T4 is selected from the group consisting of OR1, OR2, a 5′ terminal group, a 7′ terminal group and a nucleosidic linkage group, and
- when T4 is a nucleosidic linkage group,
- T3 is selected from the group consisting of ORi, OR2, a 5′ terminal group, a 7′ terminal group and a nucleosidic linkage group, and
- wherein R1 is selected from H and hydroxyl protecting group, and R2 is a phosphorus moiety;
- and
- Bx is a nucleobase.
The oligomer of claim wherein the oligomer comprises a nucleic acid sequence, wherein said nucleic acid sequence consists of at least two contiguous monomer subunits of compounds of formula (VI), wherein said nucleic acid sequence is flanked on its 5′ terminus and on its 7′ terminus each by at least one nucleotide or nucleoside that is different from the compound of formula (IV), wherein the 5′ terminus of said nucleic acid sequence is linked to a 3′ terminus of the nucleotide or nucleoside that is different from the compound of formula (IV), and wherein the 7′ terminus of said nucleic acid sequence is linked to a 5′ terminus of the nucleotide or nucleoside that is different from the compound of formula (IV).
(canceled)
Dependencies are inferred from the claim text.