Patents Assigned to Roche Innovation Center Copenhagen A/S
  • Oligonucleotide conjugation process
    Patent number: 11555050
    Abstract: 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: Grant
    Filed: February 28, 2020
    Date of Patent: January 17, 2023
    Assignee: Roche Innovation Center Copenhagen A/S
    Inventors: Dennis Jul Hansen, Christoph Rosenbohm, Michael Meldgaard
  • OLIGONUCLEOTIDES COMPRISING A PHOSPHORODITHIOATE INTERNUCLEOSIDE LINKAGE
    Publication number: 20230002762
    Abstract: 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: Application
    Filed: April 14, 2022
    Publication date: January 5, 2023
    Applicant: ROCHE INNOVATION CENTER COPENHAGEN A/S
    Inventors: 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
  • Rapid unylinker cleavage
    Patent number: 11542294
    Abstract: 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: Grant
    Filed: March 22, 2018
    Date of Patent: January 3, 2023
    Assignee: Roche Innovation Center Copenhagen A/S
    Inventors: Michael Meldgaard, Marianne B. Mogensen, Dennis Jul Hansen
  • Antisense oligonucleotides targeting alpha-synuclein and uses thereof
    Patent number: 11447775
    Abstract: 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: Grant
    Filed: January 11, 2019
    Date of Patent: September 20, 2022
    Assignees: Bristol-Myers Squibb Company, Roche Innovation Center Copenhagen A/S
    Inventors: 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
  • ALPHA-SYNUCLEIN ANTISENSE OLIGONUCLEOTIDES AND USES THEREOF
    Publication number: 20220119811
    Abstract: 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: Application
    Filed: January 11, 2019
    Publication date: April 21, 2022
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: 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
  • Stereodefining L-monomers
    Patent number: 11267843
    Abstract: 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: Grant
    Filed: March 2, 2017
    Date of Patent: March 8, 2022
    Assignee: Roche Innovation Center Copenhagen A/S
    Inventors: Nanna Albaek, Jacob Ravn, Erik Daa Funder
  • Enhanced coupling of stereodefined oxazaphospholidine phosphoramidite monomers to nucleoside or oligonucleotide
    Patent number: 11261209
    Abstract: 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: Grant
    Filed: May 9, 2017
    Date of Patent: March 1, 2022
    Assignee: Roche Innovation Center Copenhagen A/S
    Inventors: Jacob Ravn, Erik Daa Funder
  • QUALITY CONTROL OF LNA OLIGONUCLEOTIDE THERAPEUTICS USING MASSIVELY PARALLEL SEQUENCING
    Publication number: 20220002796
    Abstract: 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: Application
    Filed: May 6, 2019
    Publication date: January 6, 2022
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Mads JENSEN, Jonas VIKESAA, Lukasz KIELPINSKI, Lars JOENSON, Filippo SLADOJEVICH
  • OLIGONUCLEOTIDES FOR MODULATING MYH7 EXPRESSION
    Publication number: 20210371860
    Abstract: 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: Application
    Filed: May 7, 2019
    Publication date: December 2, 2021
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Peter HAGEDORN, Richard OLSON, Marianne JENSEN, Annapurna PENDRI, Brian ANDERSON, Sean Carl LITTLE, Linda Jane BRISTOW, John Ryan THOMPSON, Ron AMMAR
  • Oligonucleotide conjugates
    Patent number: 11155816
    Abstract: 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: Grant
    Filed: May 8, 2018
    Date of Patent: October 26, 2021
    Assignee: Roche Innovation Center Copenhagen A/S
    Inventors: Nanna Albaek, Henrik Hansen, Susanne Kammler, Jacob Ravn, Henrik Orum
  • OLIGONUCLEOTIDES COMPRISING A PHOSPHOROTRITHIOATE INTERNUCLEOSIDE LINKAGE
    Publication number: 20210292358
    Abstract: 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: Application
    Filed: July 30, 2019
    Publication date: September 23, 2021
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Konrad Bleicher, Troels KOCH, Adrian SCHAEUBLIN, Joerg Jakob Andreas DUSCHMALE, Martina Brigitte DUSCHMALE, Meiling LI, Erich KOLLER
  • MASSIVELY PARALLEL DISCOVERY METHODS FOR OLIGONUCLEOTIDE THERAPEUTICS
    Publication number: 20210269851
    Abstract: 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: Application
    Filed: May 6, 2019
    Publication date: September 2, 2021
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Mads JENSEN, Lars JOENSON, Lukasz KIELPINSKI, Jonas VIKESAA, Filippo SLADOJEVICH
  • MICRORNA-134 BIOMARKER
    Publication number: 20210270845
    Abstract: 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: Application
    Filed: February 23, 2021
    Publication date: September 2, 2021
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Jesper Worm, Lukasz Kielpinski
  • Antisense oligomers targeting PCSK9
    Patent number: 11091764
    Abstract: 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: Grant
    Filed: September 4, 2019
    Date of Patent: August 17, 2021
    Assignee: ROCHE INNOVATION CENTER COPENHAGEN A/S
    Inventors: Nanna Albæk, Maj Hedtjärn, Marie Wickstrom Lindholm, Niels Fisker Nielsen, Andreas Petri, Jacob Ravn
  • OLIGONUCLEOTIDES COMPRISING A PHOSPHOROTRITHIOATE INTERNUCLEOSIDE LINKAGE
    Publication number: 20210221837
    Abstract: 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: Application
    Filed: July 29, 2019
    Publication date: July 22, 2021
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Konrad BLEICHER, Joerg Jakob Andreas DUSCHMALÉ, Martina Brigitte DUSCHMALÉ, Troels KOCH, Erich KOLLER, Meiling LI, Adrian SCHAEUBLIN
  • CAMK2D antisense oligonucleotides and uses thereof
    Patent number: 11058767
    Abstract: 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: Grant
    Filed: February 21, 2019
    Date of Patent: July 13, 2021
    Assignees: BRISTOL-MYERS SQUIBB COMPANY, ROCHE INNOVATION CENTER COPENHAGEN A/S
    Inventors: Richard E. Olson, Brian R. Anderson, Peter Hagedorn, Marianne Lerbech Jensen, Ivar M. McDonald, Stephen E. Mercer
  • Antisense Oligonucleotides Targeting Alpha-Synuclein and Uses Thereof
    Publication number: 20210180065
    Abstract: 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: Application
    Filed: February 2, 2021
    Publication date: June 17, 2021
    Applicants: Bristol-Myers Squibb Company, Roche Innovation Center Copenhagen A/S
    Inventors: 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
  • NOVEL THIOPHOSPHORAMIDITES
    Publication number: 20210115438
    Abstract: 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: Application
    Filed: December 21, 2018
    Publication date: April 22, 2021
    Applicant: ROCHE INNOVATION CENTER COPENHAGEN A/S
    Inventors: Konrad BLEICHER, Joerg DUSCHMALÉ, Martina Brigitte DUSCHMALÉ, Henrik Frydenlund HANSEN, Troels KOCH, Meiling LI, Adrian SCHAEUBLIN, Xi SHU, Yong WU
  • OLIGONUCLEOTIDES FOR MODULATING GSK3B EXPRESSION
    Publication number: 20210095275
    Abstract: 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: Application
    Filed: January 10, 2019
    Publication date: April 1, 2021
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Peter HAGEDORN, Lykke PEDERSEN
  • OLIGONUCLEOTIDES FOR MODULATING ERC1 EXPRESSION
    Publication number: 20210095276
    Abstract: 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: Application
    Filed: January 15, 2019
    Publication date: April 1, 2021
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Peter HAGEDORN, Lykke PEDERSEN