Patents Assigned to Roche Innovation Center Copenhagen A/S
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Patent number: 11555050Abstract: The present invention relates to the field of oligonucleotide conjugates and to methods of synthesis thereof. In the present method a low-water content solvent environment allows a more efficient conjugation, reducing the amount of conjugate moiety needed and increasing the conjugation reaction speed.Type: GrantFiled: February 28, 2020Date of Patent: January 17, 2023Assignee: Roche Innovation Center Copenhagen A/SInventors: Dennis Jul Hansen, Christoph Rosenbohm, Michael Meldgaard
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Publication number: 20230002762Abstract: The present invention relates to an oligonucleotide comprising at least one phosphorodithioate internucleoside linkage of formula (I) (I) as defined in the description and in the claim. The oligonucleotide of the invention can be used as a medicement.Type: ApplicationFiled: April 14, 2022Publication date: January 5, 2023Applicant: ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Konrad Bleicher, Henrik Frydenlund HANSEN, Troels KOCH, Jesper WORM, Adrian SCHAEUBLIN, Erik FUNDER, Joerg DUSCHMALÉ, Lars JOENSON, Meiling LI, Martina Brigitte DUSCHMALÉ, Yong WU, Xi SHU
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Patent number: 11542294Abstract: Methods for cleaving oligonucleotides from a solid support are described as are methods for synthesizing an oligonucleotide on a solid support and subsequently cleaving the oligonucleotide from the solid support. In the methods, the 3? nucleoside of the oligonucleotide attached to the solid support is a LNA nucleoside. The method entail treating the bound oligonucleotide with a concentrated ammonium hydroxide solution for about 30 minutes to about 6 hours.Type: GrantFiled: March 22, 2018Date of Patent: January 3, 2023Assignee: Roche Innovation Center Copenhagen A/SInventors: Michael Meldgaard, Marianne B. Mogensen, Dennis Jul Hansen
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Patent number: 11447775Abstract: The present disclosure relates to antisense oligonucleotides, which target SNCA mRNA (e.g., at an intron exon junction) in a cell, leading to reduced expression of SNCA protein. Reduction of SNCA protein expression is beneficial for the treatment of certain medical disorders, e.g., a neurological disorder.Type: GrantFiled: January 11, 2019Date of Patent: September 20, 2022Assignees: Bristol-Myers Squibb Company, Roche Innovation Center Copenhagen A/SInventors: Richard E. Olson, Angela M. Cacace, Jere E. Meredith, Jr., Nino Devidze, James K. Loy, Carl J. Baldick, Annapurna Pendri, Ivar M. McDonald, Peter Hagedorn, Marianne Lerbech Jensen
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Publication number: 20220119811Abstract: The present disclosure relates to antisense oligonucleotides, which target Alpha-synuclein (SNCA) transcript in a cell, leading to reduced expression of SNCA protein. Reduction of SNCA protein expression is beneficial for the treatment of certain medical disorders, e.g., a neurological disorder such as a synucleinopathy.Type: ApplicationFiled: January 11, 2019Publication date: April 21, 2022Applicant: Roche Innovation Center Copenhagen A/SInventors: Peter HAGEDORN, Richard E. OLSON, Angela M. CACACE, Marianne Lerbach JENSEN, Jeffrey M. BROWN, Jere E. MEREDITH, JR., Annapurna PENDRI, Ivar M. MCDONALD, Martin GILL
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Patent number: 11267843Abstract: Stereodefined phosphorothioate oligonucleotides, related nucleoside monomers and methods of synthesis of both are described. The disclosed isobutyryl protected L-LNA-G monomers have following Formula 50 or 51 where R3 is independently CH2ODMTr or CH2OMMTr and R8, when present, is cyanoethyl. The monomers have improved solubility and stability characteristics, resulting in improved efficacy in oligonucleotide synthesis.Type: GrantFiled: March 2, 2017Date of Patent: March 8, 2022Assignee: Roche Innovation Center Copenhagen A/SInventors: Nanna Albaek, Jacob Ravn, Erik Daa Funder
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Patent number: 11261209Abstract: The present invention relates to the synthesis of stereo-defined phosphorothioate oligonucleotides of formula I: Wherein Z, R1, R5, R6 and R9 are as defined herein. Phosphorothioate oligonucleotides are useful as therapeutics.Type: GrantFiled: May 9, 2017Date of Patent: March 1, 2022Assignee: Roche Innovation Center Copenhagen A/SInventors: Jacob Ravn, Erik Daa Funder
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Publication number: 20220002796Abstract: The invention relates to the field of therapeutic oligonucleotide analytics, and provides methods for primer based parallel sequencing of therapeutic oligonucleotides which provide sequence based quality information which may be used in conjunction with or in place of present chromatography or mass spectroscopic methods, and may be used, for example, in oligonucleotide therapeutic discovery, manufacture, quality assurance, therapeutic development, and patient monitoring.Type: ApplicationFiled: May 6, 2019Publication date: January 6, 2022Applicant: Roche Innovation Center Copenhagen A/SInventors: Mads JENSEN, Jonas VIKESAA, Lukasz KIELPINSKI, Lars JOENSON, Filippo SLADOJEVICH
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Publication number: 20210371860Abstract: The present invention relates to antisense oligonucleotides that are capable of modulating expression of MYH7 in a target cell. The oligonucleotides hybridize to MYH7 mRNA. The present invention further relates to conjugates of the oligonucleotide and pharmaceutical compositions and methods for treatment of hypertrophic cardiomyopathy using the oligonucleotide.Type: ApplicationFiled: May 7, 2019Publication date: December 2, 2021Applicant: Roche Innovation Center Copenhagen A/SInventors: Peter HAGEDORN, Richard OLSON, Marianne JENSEN, Annapurna PENDRI, Brian ANDERSON, Sean Carl LITTLE, Linda Jane BRISTOW, John Ryan THOMPSON, Ron AMMAR
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Patent number: 11155816Abstract: The invention relates to the field of oligonucleotide therapeutics, and in particular to the use of a cleavable, e.g. a phosphodiester region covalently attached to a conjugate, a targeting group or blocking group to enhance the properties of the oligonucleotides, for example to improve the therapeutic index.Type: GrantFiled: May 8, 2018Date of Patent: October 26, 2021Assignee: Roche Innovation Center Copenhagen A/SInventors: Nanna Albaek, Henrik Hansen, Susanne Kammler, Jacob Ravn, Henrik Orum
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Publication number: 20210292358Abstract: The present invention relates to an oligonucleotide comprising at least one phosphorotrithioa to internucleoside linkage of formula (I), wherein (A1), (A2) and R are as defined in the description and in the claim. The oligonucleotide of the invention can be used as a medicament.Type: ApplicationFiled: July 30, 2019Publication date: September 23, 2021Applicant: Roche Innovation Center Copenhagen A/SInventors: Konrad Bleicher, Troels KOCH, Adrian SCHAEUBLIN, Joerg Jakob Andreas DUSCHMALE, Martina Brigitte DUSCHMALE, Meiling LI, Erich KOLLER
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Publication number: 20210269851Abstract: The invention relates to the field of therapeutic oligonucleotide analytics and discovery, and provides methods for primer based parallel sequencing of modified oligonucleotides which provide sequence based quality information which may be used in oligonucleotide therapeutic discovery, manufacture, quality assurance, therapeutic development, and patient monitoring.Type: ApplicationFiled: May 6, 2019Publication date: September 2, 2021Applicant: Roche Innovation Center Copenhagen A/SInventors: Mads JENSEN, Lars JOENSON, Lukasz KIELPINSKI, Jonas VIKESAA, Filippo SLADOJEVICH
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Publication number: 20210270845Abstract: The invention relates to the field of secondary markers for microRNA activity, and in particular the invention relates to the identification of Serpine1 as a mRNA which is repressed by microRNA-134 in neuronal cells, and the use of Serpine1 mRNA or protein as a biomarker for microRNA-134 modulation, such as a biomarker for antisense oligonucleotide inhibitors of microRNA-134.Type: ApplicationFiled: February 23, 2021Publication date: September 2, 2021Applicant: Roche Innovation Center Copenhagen A/SInventors: Jesper Worm, Lukasz Kielpinski
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Patent number: 11091764Abstract: The present invention relates to oligomeric compounds and conjugates thereof that target Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) PCSK9 mRNA in a cell, leading to reduced expression of PCSK9. Reduction of PCSK9 expression is beneficial for a range of medical disorders, such as hypercholesterolemia and related disorders.Type: GrantFiled: September 4, 2019Date of Patent: August 17, 2021Assignee: ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Nanna Albæk, Maj Hedtjärn, Marie Wickstrom Lindholm, Niels Fisker Nielsen, Andreas Petri, Jacob Ravn
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Publication number: 20210221837Abstract: The present invention relates to an oligonucleotide comprising at least one phosphorotrithioate internucleoside linkage of formula (I) as defined herein. The oligonucleotide of the invention can be used as a medicament.Type: ApplicationFiled: July 29, 2019Publication date: July 22, 2021Applicant: Roche Innovation Center Copenhagen A/SInventors: Konrad BLEICHER, Joerg Jakob Andreas DUSCHMALÉ, Martina Brigitte DUSCHMALÉ, Troels KOCH, Erich KOLLER, Meiling LI, Adrian SCHAEUBLIN
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Patent number: 11058767Abstract: The present disclosure relates to antisense oligonucleotides, which target CAMK2D mRNA in a cell, leading to reduced expression of CAMK2D protein. Reduction of CAMK2D protein expression is beneficial for the treatment of certain medical disorders, e.g., cardiovascular-related diseases or disorders.Type: GrantFiled: February 21, 2019Date of Patent: July 13, 2021Assignees: BRISTOL-MYERS SQUIBB COMPANY, ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Richard E. Olson, Brian R. Anderson, Peter Hagedorn, Marianne Lerbech Jensen, Ivar M. McDonald, Stephen E. Mercer
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Publication number: 20210180065Abstract: The present disclosure relates to antisense oligonucleotides, which target SNCA mRNA (e.g., at an intron exon junction) in a cell, leading to reduced expression of SNCA protein. Reduction of SNCA protein expression is beneficial for the treatment of certain medical disorders, e.g., a neurological disorder.Type: ApplicationFiled: February 2, 2021Publication date: June 17, 2021Applicants: Bristol-Myers Squibb Company, Roche Innovation Center Copenhagen A/SInventors: Richard E. OLSON, Angela M. CACACE, Jere E. MEREDITH, JR., Nino DEVIDZE, James K. LOY, Carl J. BALDICK, Annapurna PENDRI, Ivar M. McDONALD, Peter HAGEDORN, Marianne Lerbech JENSEN
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Publication number: 20210115438Abstract: The present invention relates to a compound of formula (II) or (IIb) Wherein X, Y, Rx, Ry, R5 and Nu are as defined in the description and in the claims. The compound of formula (II) can be used in the manufacture of oligonucleotides.Type: ApplicationFiled: December 21, 2018Publication date: April 22, 2021Applicant: ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Konrad BLEICHER, Joerg DUSCHMALÉ, Martina Brigitte DUSCHMALÉ, Henrik Frydenlund HANSEN, Troels KOCH, Meiling LI, Adrian SCHAEUBLIN, Xi SHU, Yong WU
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Publication number: 20210095275Abstract: The present invention relates to antisense oligonucleotides that are capable of reducing expression of GSK3B in a target cell. The antisense oligonucleotides hybridize to GSK3B pre-mRNA. The present invention further relates to conjugates of the antisense oligonucleotide, pharmaceutical salts and pharmaceutical compositions and methods for treatment or alleviation of conditions such as cancer, inflammatory diseases, neurological diseases, neurological injury, neuronal degeneration, psychiatric diseases and Type 2 diabetes.Type: ApplicationFiled: January 10, 2019Publication date: April 1, 2021Applicant: Roche Innovation Center Copenhagen A/SInventors: Peter HAGEDORN, Lykke PEDERSEN
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Publication number: 20210095276Abstract: The present invention relates to antisense oligonucleotides that are capable of reducing expression of ERC1 in a target cell. The oligonucleotides hybridize to ERC1 pre-mRNA. The present invention further relates to conjugates of the oligonucleotide and pharmaceutical compositions and methods for treatment of disease associated with ERC1 overexpression, such as cancer or Dengue virus infection using the antisense oligonucleotide.Type: ApplicationFiled: January 15, 2019Publication date: April 1, 2021Applicant: Roche Innovation Center Copenhagen A/SInventors: Peter HAGEDORN, Lykke PEDERSEN