US 7,696,345 B2 · Polycyclic sugar surrogate-containing oligomeric compounds and compositions for use in gene modulation

Abstract

Compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capable of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers includes a modification comprising a polycyclic sugar surrogate. Oligomer/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleoside of the oligomer has a polycyclic sugar surrogate modification.

Claims24

Dependent claims

An oligomeric compound comprising at least one nucleoside having a bicyclic sugar moiety of the formula:

wherein:
Bx is a heterocyclic base moiety;
P4 is an internucleoside linkage to an adjacent monomer, OH, or a protected hydroxyl group;
X1 is O;
substituents Rc and Rf together designate a biradical selected from —C(RaRb)—O—N(Ra)— or —C(RaRb)—N(Ra)—O—;
Ra and Rb that are not part of the second ring are each H;
Ra and Rb that are part of the second ring are each independently H, C1-C12 alkyl or halogen;
Rg and Rh are each H;
one of Rd and Re is a terminal group or an internucleoside linkage to an adjacent monomer and the other of Rd and Re is H;
and
wherein at least one of P4, Rd or Re is an internucleoside linkage to an adjacent monomer.

8 more elements

An oligonucleotide analogue, as a DNA oligonucleotide or RNA oligonucleotide analogue, containing one or two or more of one or more types of unit structures of nucleoside analogues represented by the following general formula (II), or a pharmacologically acceptable salt thereof, provided that a form of linking between respective nucleosides in the oligonucleotide analogue may contain one or two or more phosphorothioate bonds [—OP(O)(S−)O—] aside from a phosphodiester bond [—OP(O2−)O—] identical with that in a natural nucleic acid, and if two or more of one or more types of these structures are contained, Base may be identical or different between these structures,

where Base represents an aromatic heterocyclic group or aromatic hydrocarbon ring group optionally having a substituent,
R3 represents a hydrogen atom, an alkyl group, an alkenyl group, a cycloalkyl group, an aryl group, an aralkyl group, an acyl group, a sulfonyl group, a silyl group, or a functional molecule unit substituent,
and m denotes an integer of 0 to 2, and n denotes an integer of 1 to 3.

Dependencies are inferred from the claim text.

Facts

Application

10/701,285Filed 4 Nov 2003 · us provisional application

Priority

5 Nov 2002

Published

US 2004/0171570 A12 Sep 2004

Granted

13 Apr 2010

Term ends

Not estimatedThe source records don’t support an estimate.

Classification13 codes

C12N 15/1135
Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming…: against…
C07H 21/04
Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of…: with…
C12N 15/1137
Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming…: against enzymes
C12N 2310/11
Type of nucleic acid: antisense

Polycyclic sugar surrogate-containing oligomeric compounds and compositions for use in gene modulation

Life of this patent

Polycyclic sugar surrogate-containing oligomeric compounds and compositions for use in gene modulation

Life of this patent

Abstract

Claims24