Patents Assigned to Roche Innovation Center Copenhagen A/S
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Patent number: 12180478Abstract: 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: July 27, 2022Date of Patent: December 31, 2024Assignees: 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: 20240368593Abstract: The present invention relates to a gapmer oligonucleotide comprising at least one phosphorodithioate internucleoside linkage of formula (I) as defined in the description and in the claims. The oligonucleotide of the invention can be used as a medicement.Type: ApplicationFiled: March 27, 2024Publication date: November 7, 2024Applicant: Roche Innovation Center Copenhagen A/SInventors: Konrad Bleicher, Joerg Duschmalé, Martina Brigitte Duschmalé, Henrik Frydenlund Hansen, Erik Funder, Troels Koch, Meiling Li, Adrian Schaeublin, Xi Shu, Yong Wu
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Patent number: 11814407Abstract: The present invention relates to methods of synthesis of stereodefined oligonucleotides wherein the protected 5?-hydroxy terminus of a nucleoside or oligonucleotide attached to a solid support is first unprotected, followed by coupling an oxazaphospholidine phosphoramidite monomer to the now deprotected 5?-hydroxy terminus, oxidizing the resultant phosphite triester intermediate with a sulfurizing reagent, and optionally washing the product. The method of synthesis of the present invention described above may be repeated to optionally elongate the stereodefined oligonucleotide being synthesized until the elongation cycle is intentionally terminated via deprotecting and cleavaging the resulting stereodefined oligonucleotide from the solid support. The oxazaphospholidine phosphoramidite monomer to be coupled in the present invention may optionally be chosen from Formula 1a and 1b.Type: GrantFiled: June 26, 2018Date of Patent: November 14, 2023Assignee: ROCHE INNOVATION CENTER COPENHAGEN A/SInventors: Dennis Jul Hansen, Erik Daa Funder
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Publication number: 20230323421Abstract: The invention relates to antisense oligonucleotides which alter the splicing of XBP1 pre-mRNA. The antisense oligonucleotides have applications in enhancing the level and/or quality of protein expression in cells and in mammalian protein expression systems, such as heterologous protein expression systems, such as enhancing antibody expression in CHO cells. The antisense oligonucleotides also have applications in therapy, such as for the treatment or prevention of proteopathological diseases.Type: ApplicationFiled: June 22, 2023Publication date: October 12, 2023Applicant: Roche Innovation Center Copenhagen A/SInventors: Styliani TOURNAVITI, Jonas VIKESAA, Shan-Hua CHUNG
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Patent number: 11739332Abstract: 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: July 16, 2021Date of Patent: August 29, 2023Assignee: 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: 20230193260Abstract: 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: July 27, 2022Publication date: June 22, 2023Applicants: 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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Patent number: 11667660Abstract: The present invention relates to a method for preparing stereodefined phosphorothioate oligonucleotides, especially locked stereodefined phosphorothioate oligonucleotides with a high yield, using pyridinium acidic salts as a coupling activator.Type: GrantFiled: April 27, 2021Date of Patent: June 6, 2023Assignee: Roche Innovation Center Copenhagen A/SInventors: Dennis Jul Hansen, Erik Daa Funder
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Patent number: 11597926Abstract: 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: GrantFiled: December 21, 2018Date of Patent: March 7, 2023Assignee: 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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Patent number: 11591362Abstract: The present invention relates to the field of stereodefined phosphorothioate oligonucleotides and to stereodefining nucleoside monomers comprising an amine containing chiral auxiliary group, and methods of orthogonally protecting the nitrogen of chiral auxiliaries during oligonucleotide synthesis, preventing post elongation chain cleavage, increasing yield and purity of stereodefined phosphorothioate oligonucleotides.Type: GrantFiled: March 20, 2018Date of Patent: February 28, 2023Assignee: Roche Innovation Center Copenhagen A/SInventors: Konrad Bleicher, Dennis Jul Hansen, Erik Daa Funder
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Patent number: 11591594Abstract: Recent advancements in LNA oligonucleotides include the use of amine linkers to link an LNA antisense oligonucleotide to a conjugate group. For example please see WO2014/I18267. The present invention originates from the identification of a problem when de-protecting LNA oligonucleotides which comprise an aliphatic amine group and DMF protected LNA G nucleoside, which results in the production of a +28 Da impurity. This problem is solved by using acyl protection groups on the exocyclic nitrogen of the LNA-G residue, rather than the standard DMF protection group.Type: GrantFiled: March 6, 2020Date of Patent: February 28, 2023Assignee: Roche Innovation Center Copenhagen A/SInventors: Dennis Jul Hansen, Joerg Hoernschemeyer, Jacob Ravn, Christoph Rosenbohm
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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