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US 6,268,490 B1Granted
Bicyclonucleoside and oligonucleotide analogues
AssigneeTakeshi Imanishi
InventorsTakeshi Imanishi, Satoshi Obika
Life of this patent
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Abstract
An oligo- or polynucleotide analogue having one or more structures of the general formula where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is disclosed. The use of this analogue provides an oligonucleotide analogue antisense molecule, which is minimally hydrolyzable with an enzyme in vivo, has a high sense strand binding ability, and is easily synthesized.
Claims8
A nucleoside analogue of the following formula (I)
- where B is a pyrimidine or purine nucleic acid base, and X and Y are identical or different, and each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aralkyl group, an aryl group, an acyl group, or a silyl group, or an amidite derivative thereof.
An oligonucleotide or polynucleotide analogue having one or more structures or the formula (Ia)
- where B is a pyrimidine or purine nucleic acid base.
An oligonucleotide or polynucleotide analogue of the formula (II)
- where B1 and B are identical or different, and each represents a pyrimidine or purine nucleic acid base, R is a hydrogen atom, a hydroxyl group, a halogen atom, or an alkoxy group,
- W1 and W2 are identical or different, and each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aralkyl group, an aryl group, an acyl group, a silyl group, a phosphoric acid residue, a naturally occurring nucleoside or a synthetic nucleoside bound via a phosphodiester bond, or an oligonucleotide or polynucleotide containing the nucleoside, n1 or n2 are identical or different, and each denotes an integer of 0 to 50, provided that n1 and n2 are not both zero, and that not all of the n2 are zero at the same time, n3 denotes an integer of 1 to 50, provided that when n1 and/or n2 are or is 2 or more, B1 and B need not be identical, and R need not be identical.
Dependencies are inferred from the claim text.