Patent Evaluation: Detection and Modulation of Gene Expression by Oligonucleotides

Summary

Novelty: Antisense oligonucleotides are claimed and are stated to have increased resistance to nucleases. Novel synthetic methods create oligonucleotides which are non toxic and may be able to hybridize to either DNA or RNA. The oligonucleotides may be used in therapy to modulate or turn off gene or protein expression.

Biology: No biological data are presented.

Chemistry: The bases can be either ether, or phosphothiorate, linked. The major innovation is the addition of substituents on the 5 and 6 positions of the pyrimidine rings. These can be methyl, hydroxyl, ether, benzyl, nitro or halogen.