Patents by Inventor Konrad Bleicher

Konrad Bleicher has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20250034576
    Abstract: The present invention relates to double stranded oligonucleotides that are complementary to JAK1, leading to modulation of the expression of JAK1. Modulation of JAK1 expression is beneficial for a range of medical disorders including inflammatory bowel disease, organ transplant rejection, graft-versus-host disease, multiple sclerosis, rheumatoid arthritis (RA), juvenile idiopathic arthritis, psoriasis, dermatitis, diabetic nephropathy, systemic lupus erythematosus (SLE), dry eye disease, cancer, myelofibrosis, and asthma. Also included are compositions comprising the double stranded oligonucleotide and methods of treatment using the double stranded oligonucleotide.
    Type: Application
    Filed: June 14, 2024
    Publication date: January 30, 2025
    Inventors: Philipp Friedrich BERNINGER, Konrad BLEICHER, Erik FUNDER, Helle JACOBSEN, Dennis Jul HANSEN, Michael KELLER, Inna Appeldorff LARSEN, Meiling LI, Disa Elisabet TEHLER, Lotte WINTHER, Jesper WORM, Lena WYSS, Tiago Francisco SANTOS FERREIRA
  • Publication number: 20240409939
    Abstract: The present invention relates to combinations of Regulator of telomere elongation helicase 1 (RTEL1) and Far Upstream Element-Binding Protein 1 (FUBP1) inhibitors, such as oligonucleotides (oligomers) that are complementary to RTEL1 or FUBP1, respectively, leading to modulation of the expression of RTEL1 and FUBP1 or modulation of RTEL1 and FUBP1 activity. The invention in particular relates to a combination of an inhibitor of RTEL1 and an inhibitor of FUBP1 for use in treating and/or preventing a disease, preferably a hepatitis B virus (HBV) infection, in particular a chronic HBV infection. The invention in particular relates to the use of a combination of RTEL1 and FUBP1 inhibitors for destabilizing cccDNA, such as HBV cccDNA. Also comprised in the present invention is a pharmaceutical composition, a kit and the use thereof in the treatment and/or prevention of a HBV infection.
    Type: Application
    Filed: June 13, 2024
    Publication date: December 12, 2024
    Inventors: Konrad BLEICHER, Josephine Felber, Erik Funder, Souphalone Luangsay, Tobias Nilsson, Soren Ottosen, Johanna Marie Pose Vicente, Timothy Tellinghuisen
  • Publication number: 20240368593
    Abstract: 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: Application
    Filed: March 27, 2024
    Publication date: November 7, 2024
    Applicant: Roche Innovation Center Copenhagen A/S
    Inventors: Konrad Bleicher, Joerg Duschmalé, Martina Brigitte Duschmalé, Henrik Frydenlund Hansen, Erik Funder, Troels Koch, Meiling Li, Adrian Schaeublin, Xi Shu, Yong Wu
  • Publication number: 20240336920
    Abstract: Described are antisense oligonucleotides comprising one or more ?-L-threofuranosyl (TNA) nucleosides as well as methods to modulate the properties of antisense oligonucleotides by the introduction of TNA nucleosides. These are particularly applicable for antisense gapmer oligonucleotides.
    Type: Application
    Filed: June 20, 2024
    Publication date: October 10, 2024
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Jessica Marine Aurore BASTIEN, Konrad BLEICHER, Helle CHRISTIANSEN, Erich KOLLER, Meiling LI, Helle NYMARK, Adrian SCHAEUBLIN, Steffen SCHMIDT
  • Patent number: 12012466
    Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
    Type: Grant
    Filed: July 15, 2021
    Date of Patent: June 18, 2024
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
  • Publication number: 20240050516
    Abstract: The present invention provides compounds of formula (I) wherein X1, X2, R1 to R6 and A are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by bacteria.
    Type: Application
    Filed: October 12, 2023
    Publication date: February 15, 2024
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Konrad BLEICHER, Daniella CHEANG, Patrick DI GIORGIO, Taishan HU, Christian JENNY, Patrizio MATTEI, Petra SCHMITZ, Theodor STOLL
  • Patent number: 11819532
    Abstract: The present invention provides compounds of formula (I) wherein X1, X2, R1 to R6 and A are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by bacteria.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: November 21, 2023
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Daniella Cheang, Patrick Di Giorgio, Patrizio Mattei, Petra Schmitz, Theodor Stoll
  • Patent number: 11597926
    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: Grant
    Filed: December 21, 2018
    Date of Patent: March 7, 2023
    Assignee: 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
  • Patent number: 11591362
    Abstract: 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: Grant
    Filed: March 20, 2018
    Date of Patent: February 28, 2023
    Assignee: Roche Innovation Center Copenhagen A/S
    Inventors: Konrad Bleicher, Dennis Jul Hansen, Erik Daa Funder
  • 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
  • Publication number: 20220411468
    Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
    Type: Application
    Filed: July 15, 2021
    Publication date: December 29, 2022
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
  • Patent number: 11505573
    Abstract: The present invention provides compounds of formula (I) wherein X, L1 and R1 to R10 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
    Type: Grant
    Filed: March 19, 2019
    Date of Patent: November 22, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Daniella Cheang, Patrick Di Giorgio, Taishan Hu, Patrizio Mattei, Petra Schmitz, Theodor Stoll
  • Publication number: 20220363706
    Abstract: The invention relates to a compound of formula (I) wherein R2 and R4 are joined and together form a group, such a —CH2O—. The compound of formula (I) can be used in the manufacture of 5'S-LNA oligonucleotides as antisense drugs.
    Type: Application
    Filed: July 18, 2022
    Publication date: November 17, 2022
    Inventors: Konrad Bleicher, Joerg Duschmalé, Goutam Saha, Juber Abdulhamid Shaikh
  • Patent number: 11390641
    Abstract: The invention relates to a compound of formula (I) wherein R2 and R4 are joined and together form a group, such a —CH2O—. The compound of formula (I) can be used in the manufacture of 5?S-LNA oligonucleotides as antisense drugs.
    Type: Grant
    Filed: July 24, 2017
    Date of Patent: July 19, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Joerg Duschmalé, Goutam Saha, Juber Abdulhamid Shaikh
  • Publication number: 20220112493
    Abstract: The invention relates to a single-stranded antisense gapmer oligonucleotide comprising at least one dinucleoside of formula (I) wherein (A1), (A2) and A are as defined in the description and in the claims. The oligonucleotide according to the invention can be used as a medicament.
    Type: Application
    Filed: August 18, 2021
    Publication date: April 14, 2022
    Inventors: Konrad BLEICHER, Jessica Marine Aurore BASTIEN
  • Publication number: 20220073916
    Abstract: The invention relates to a compound of formula (II) wherein X, Y, R5, Rx, Ry and Nu are as defined in the description and in the claims. The compound of formula (II) can be used in the manufacture of medicaments.
    Type: Application
    Filed: August 18, 2021
    Publication date: March 10, 2022
    Inventors: Konrad BLEICHER, Jessica Marine Aurore BASTIEN
  • Publication number: 20210309690
    Abstract: The invention relates to a process for the manufacture of an oligonucleotide comprising at least one non-chiral phosphorothioate intemucleoside linkage of formula (I) wherein R1 is as defined in the description and in the claims.
    Type: Application
    Filed: July 25, 2017
    Publication date: October 7, 2021
    Inventors: Konrad Bleicher, Joerg Duschmalé, Goutam Saha, Juber Abdulhamid Shaikh
  • 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
  • Patent number: 11098080
    Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: August 24, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
  • Patent number: 11091514
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R8?, R9, R9?, X1, X2, X3, X4, X5, X6, X7, X8, X9 and X10 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baurnannii.
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: August 17, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Jérôme Hert, Carsten Kroll, Fabian Dey