Patents Assigned to Roche Innovation Center Copenhagen A/S
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Patent number: 9790493Abstract: The present invention relates to very short heavily modified oligonucleotides which target and inhibit microRNAs in vivo, and their use in medicaments and pharmaceutical compositions.Type: GrantFiled: October 29, 2014Date of Patent: October 17, 2017Assignee: Roche Innovation Center Copenhagen A/SInventors: Susanna Obad, Sakari Kauppinen, Joacim Elmen, Morten Lindow, Markus Heidenblad
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Patent number: 9738894Abstract: The present invention is directed to novel double-stranded short interfering (siRNA) analogs comprising locked nucleic acid (LNA) monomers. Such compounds induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). The compounds disclosed herein has improved properties compared to non-modified siRNAs and may, accordingly, be useful as therapeutic agents, e.g., in the treatment of various cancer forms. More particularly, the present invention is directed to siRNA analogs comprising a sense strand and an antisense strand, wherein each strand comprises 12-35 nucleotides and wherein the siRNA analogs comprise at least one locked nucleic acid (LNA) monomer.Type: GrantFiled: March 28, 2016Date of Patent: August 22, 2017Assignee: Roche Innovation Center Copenhagen A/SInventors: Joacim Elmen, Claes Wahlestedt, Zicai Liang, Anders M. Sorensen, Henrik Orum, Troels Koch
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Patent number: 9725723Abstract: Disclosed are oligonucleotides which target and hybridize to nucleic acid molecules encoding FGFR3, leading to reduced expression of FGFR3. Reduction in the aberrant expression of FGFR3 is beneficial for the treatment of certain medical disorders, such as achondroplasia.Type: GrantFiled: November 25, 2013Date of Patent: August 8, 2017Assignee: Roche Innovation Center Copenhagen A/SInventors: Maj Hedtjarn, Soren Ottosen
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Patent number: 9708614Abstract: A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.Type: GrantFiled: August 15, 2016Date of Patent: July 18, 2017Assignee: Roche Innovation Center Copenhagen A/SInventors: Signe M. Christensen, Nikolaj Dam Mikkelsen, Miriam Frieden, Henrik Frydenlund Hansen, Troels Koch, Daniel Sejer Pedersen, Christoph Rosenbohm, Charlotte Albaek Thrue, Majken Westergaard
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Patent number: 9566293Abstract: The invention provides for LNA oligomers, for the treatment of a metabolic or liver disorder, wherein the LNA oligomer is administered orally in a unit dose of less than 50 mgs/kg, wherein the LNA oligomer is administered in the presence of a penetration (permeation) enhancer.Type: GrantFiled: October 19, 2015Date of Patent: February 14, 2017Assignee: Roche Innovation Center Copenhagen A/SInventors: Gregroy Hardee, Ellen Marie Straarup, Marie Wickstrom Lindholm, Henrik Orum, Henrik Frydenlund Hansen
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Publication number: 20160355819Abstract: 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 analogue, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analogue or a 2-deoxynucleotide, subscript “s” designates a phosphorothioate link between neighbouring nucleotides/LNA nucleotide analogues, and subscript “x” designates either a phosphorothioate link or a phosphorodiester link between neighbouring nucleotides/LNA nucleotide analogues, 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.Type: ApplicationFiled: August 22, 2016Publication date: December 8, 2016Applicant: ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Majken Westergaard, Charlotte Albaek Thrue, Frank Rasmussen, Henrik Frydenlund Hansen
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Publication number: 20160289677Abstract: The present invention relates to conjugates of antisense oligonucleotides (oligomers) that target the APOB gene at position 2265 to 2277.Type: ApplicationFiled: November 14, 2014Publication date: October 6, 2016Applicant: Roche Innovation Center Copenhagen A/SInventors: Nanna Albaek, Henrik Frydenlund Hansen, Susanne Kammler, Marie Lindholm, Mark Turner, Henrik Orum
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Patent number: 9447138Abstract: 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 analogue, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analogue or a 2-deoxynucleotide, subscript “s” designates a phosphorothioate link between neighbouring nucleotides/LNA nucleotide analogues, and subscript “x” designates either a phosphorothioate link or a phosphorodiester link between neighbouring nucleotides/LNA nucleotide analogues, 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.Type: GrantFiled: March 27, 2013Date of Patent: September 20, 2016Assignee: ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Majken Westergaard, Charlotte Albaek Thrue, Frank Winther Rasmussen, Henrik Frydenlund Hansen
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Patent number: 9428534Abstract: A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.Type: GrantFiled: March 12, 2013Date of Patent: August 30, 2016Assignee: Roche Innovation Center Copenhagen A/SInventors: Signe M. Christensen, Nikolaj Dam Mikkelsen, Miriam Frieden, Henrik Frydenlund Hansen, Troels Koch, Daniel Sejer Pedersen, Christoph Rosenbohm, Charlotte Albaek Thrue, Majken Westergaard
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Patent number: 9364495Abstract: The invention provides for LNA oligomers, for the treatment of a metabolic or liver disorder, wherein the LNA oligomer is administered orally in a unit dose of less than 50 mgs/kg, wherein the LNA oligomer is administered in the presence of a penetration (permeation) enhancer.Type: GrantFiled: October 20, 2010Date of Patent: June 14, 2016Assignee: Roche Innovation Center Copenhagen A/SInventors: Gregroy Hardee, Ellen Marie Straarup, Marie Wickstrom Lindholm, Henrik Orum, Henrik Hansen
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Publication number: 20160130582Abstract: The present invention provides, among other things, oligonucleotide modulators (e.g., inhibitors) of B cell lymphoma/leukemia 11A (BCL11A) and improved methods and composition for treating BCL11A-related diseases, disorders or conditions based on such modulators.Type: ApplicationFiled: May 26, 2014Publication date: May 12, 2016Applicant: ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Maj HEDTJÄRN, Niels Fisker NIELSEN
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Patent number: 9297010Abstract: The present invention is directed to novel double-stranded short interfering (siRNA) analogs comprising locked nucleic acid (LNA) monomers. Such compounds induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). The compounds disclosed herein has improved properties compared to non-modified siRNAs and may, accordingly, be useful as therapeutic agents, e.g., in the treatment of various cancer forms. More particularly, the present invention is directed to siRNA analogs comprising a sense strand and an antisense strand, wherein each strand comprises 12-35 nucleotides and wherein the siRNA analogs comprise at least one locked nucleic acid (LNA) monomer.Type: GrantFiled: February 11, 2014Date of Patent: March 29, 2016Assignee: Roche Innovation Center Copenhagen A/SInventors: Joacim Elmen, Claes Wahlestedt, Zicai Liang, Anders M. Sorensen, Henrik Orum, Troels Koch
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Patent number: 9290758Abstract: The present invention relates to oligomer compounds (oligomers), which target APO-B100 mRNA in a cell, leading to reduced expression of APO-B100. Reduction of APO-B100 expression is beneficial for the treatment of certain medical disorders, such as diseases associated with apolipoproteinB activity, such as in non-limiting example, different types of HDL/LDL cholesterol imbalance; dyslipidemias, e.g., familial combined dyslipidemia (FCHL), acquired hyperlipidemia, hypercholesterolemia, statin-resistant hypercholesterolemia; coronary artery disease (CAD), coronary heart disease (CHD), atherosclerosis.Type: GrantFiled: June 14, 2010Date of Patent: March 22, 2016Assignee: Roche Innovation Center Copenhagen A/SInventors: Niels Fisker Nielsen, Ellen Marie Straarup, Marie Wickstrom Lindholm
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Publication number: 20150291958Abstract: The present invention relates to conjugates of LNA antisense oligonucleotides (oligomers) that target ApoB.Type: ApplicationFiled: November 14, 2013Publication date: October 15, 2015Applicant: Roche Innovation Center Copenhagen A/SInventors: Nanna Albaek, Henrik Frydenlund Hansen, Susanne Kammler, Jacob Ravn, Henrik Orum, Mark Turner, Marie Lindholm
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Patent number: 9133455Abstract: The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 26 nucleobases which are complementary to human microRNAs selected from the group consisting of miR19b, miR21, miR122a, miR155 and miR375. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogs into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC.Type: GrantFiled: April 4, 2014Date of Patent: September 15, 2015Assignee: Roche Innovation Center Copenhagen A/SInventors: Joacim Elmén, Phil Kearney, Sakari Kauppinen
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Patent number: 9034837Abstract: The present invention provides compositions and methods of treatment of HCV infected subjects that are not sensitive to interferon treatment. Further, compositions and methods are provided for prevention of organ transplant rejection. The compositions of the invention comprise an anti microRNA-122 oligonucleotide, and are made for administration to a primate.Type: GrantFiled: April 26, 2010Date of Patent: May 19, 2015Assignee: Roche Innovation Center Copenhagen A/SInventors: Elisabeth S. Hildebrandt-Eriksen, Andreas Petri, Sakari Kauppinen, Niels Abrahamsen, Robert Eldon Lanford