- Patent Title: Potent LNA oligonucleotides for the inhibition of HIF-1A expression
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Application No.: US15243646Application Date: 2016-08-22
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Publication No.: US09938527B2Publication Date: 2018-04-10
- Inventor: Majken Westergaard , Charlotte Albaek Thrue , Frank Rasmussen , Henrik Frydenlund Hansen
- Applicant: ROCHE INNOVATION CENTER COPENHAGEN A/S
- Applicant Address: DK
- Assignee: Roche Innovation Center Copenhagen A/S
- Current Assignee: Roche Innovation Center Copenhagen A/S
- Current Assignee Address: DK
- Main IPC: C12N15/113
- IPC: C12N15/113 ; C07H21/04 ; A61K45/06 ; A61N5/10 ; A61K31/7088 ; C12N15/11

Abstract:
The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5′-(Tx)GxGxcsasasgscsastscscsTxGxT-3′ and 5′-(Gx)TxTxascstsgscscststscsTxTxA-3′, wherein capital letters designate a beta-D-oxy-LNA nucleotide analog, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analog or a 2-deoxynucleotide, subscript “s” designates a phosphorothioate link between neighboring nucleotides/LNA nucleotide analogs, and subscript “x” designates either a phosphorothioate link or a phosphorodiester link between neighboring nucleotides/LNA nucleotide analogs, and wherein the sequence is optionally extended by up to five 2-deoxynucleotide units. The LNA oligonucleotides are useful for modulating the expression of hypoxia-inducible factor-1a (HIF-1a), e.g. in the treatment of cancer diseases, inhibiting angiogenesis, inducing apoptosis, preventing cellular proliferation, or treating an angiogenic disease, e.g. diabetic retinopathy, macular degeneration (ARMD), psoriasis, rheumatoid arthritis and other inflammatory diseases.
Public/Granted literature
- US20160355819A1 POTENT LNA OLIGONUCLEOTIDES FOR THE INHIBITION OF HIF-1A EXPRESSION Public/Granted day:2016-12-08
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