Mediated cellular delivery of LNA oligonucleotides
First Claim
Patent Images
1. A compound of formula I:
-
OLIGO-L-CHEL
(I)wherein “
OLIGO”
designates an oligonucleotide composition containing one or two LNA monomers within each three nucleotide segment, “
CHEL”
is 2,2′
;
6′
,2″
-terpyridine, and “
L”
is a linking moiety.
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Abstract
The present invention relates to novel modified oligomeric compounds and to methods of making and using such compounds. The invention further relates to methods of enhancing the cellular uptake of oligomeric compounds comprising conjugating a metal chelator to those.
52 Citations
10 Claims
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1. A compound of formula I:
-
OLIGO-L-CHEL
(I)wherein “
OLIGO”
designates an oligonucleotide composition containing one or two LNA monomers within each three nucleotide segment, “
CHEL”
is 2,2′
;
6′
,2″
-terpyridine, and “
L”
is a linking moiety. - View Dependent Claims (2, 3, 4, 5, 10)
-
-
6. A method of synthesizing a compound of formula I
OLIGO-L-CHEL-
(I)wherein “
OLIGO”
designates an oligonucleotide composition containing an LNA monomer at every third nucleotide, “
CHEL”
is 2,2′
;
6′
,2″
-terpyridine, and “
L”
is a linking moiety, comprising the following steps;a) coupling said linking moiety with a suitable solid phase protecting group to the 5′
-end of an oligonucleotide composition attached to a solid phase at the 3′
end,b) cleaving off said solid phase protecting group using a suitable reagent, c) conjugating to said linking moiety 2,2′
;
6′
,2″
-terpyridine, andd) deprotecting said 3′
end.
-
-
7. A method of synthesizing a compound of formula I
OLIGO-L-CHEL-
(I)wherein “
OLIGO”
designates an oligonucleotide composition containing one or two LNA monomers within each three nucleotide segment, “
CHEL”
is 2,2′
;
6′
,2″
-terpyridine, and “
L”
is a linking moiety, comprising the following steps;a) attaching said linking moiety to a solid phase, b) synthesizing an oligonucleotide composition comprising said linking moiety, c) deprotecting said oligonucleotide composition from said solid phase, and d) conjugating to said linking moiety 2,2′
;
6′
,2″
-terpyridine.
-
-
8. A kit comprising a compound of formula I
OLIGO-L-CHEL-
(I)wherein “
OLIGO”
designates an oligonucleotide composition containing one or two LNA monomers within each three nucleotide segment, “
CHEL”
is 2,2′
;
6′
,2″
-terpyridine, and “
L”
is a linking moiety for use in diagnostics.
-
-
9. A method of synthesizing a compound of formula I
OLIGO-L-CHEL-
(I)wherein “
OLIGO”
designates an oligonucleotide composition containing one or two LNA monomers within each three nucleotide segment, “
CHEL”
is 2,2′
;
6,2″
-terpyridine, and “
L”
is a linking moiety, comprising the following steps;a) coupling said linking moiety with a suitable solid phase protecting group to the 5-end of an oligonucleotide composition attached to a solid phase at the 3′
end,b) cleaving off said solid phase protecting group using a suitable reagent, c) conjugating to said linking moiety 2,2′
;
6′
,2″
-terpyridine, andd) deprotecting said 3′
end.
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Specification
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Current AssigneeQiagen GmbH (Qiagen NV)
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Original AssigneeExiqon A/S (Qiagen NV)
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InventorsMoeller, Soeren, Bryld, Torsten, Rasmussen, Soeren Vestergaard
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Primary Examiner(s)VIVLEMORE, TRACY ANN
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Application NumberUS12/523,678Publication NumberTime in Patent Office1,383 DaysField of SearchNoneUS Class Current536/23.1CPC Class CodesA61P 31/12 AntiviralsA61P 35/00 Antineoplastic agentsA61P 43/00 Drugs for specific purposes...C07H 21/00 Compounds containing two or...
