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).

  • Thiophosphoramidites
    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
  • Orthogonal protecting groups for the preparation of stereodefined phosphorothioate oligonucleotides
    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
  • 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
  • PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
    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
  • Peptide macrocycles against
    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
  • 5`S-LNA nucleotides and oligonucleotides
    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
  • 5?S-LNA nucleotides and oligonucleotides
    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
  • PHOSPHONOACETATE GAPMER OLIGONUCLEOTIDES
    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
  • NOVEL PHOSPHORAMIDITES
    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
  • OLIGONUCLEOTIDE SYNTHESIS
    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
  • 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
  • Peptide macrocycles against Acinetobacter baumannii
    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
  • Peptide macrocycles and use thereof in the treatment of bacterial infections
    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
  • 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
  • Anti-bacterial peptide macrocycles and use thereof
    Patent number: 11066443
    Abstract: The present invention relates to compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof for the use in the treatment or prevention of infections and resulting diseases caused by Pseudomonas aeruginosa.
    Type: Grant
    Filed: April 9, 2018
    Date of Patent: July 20, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Kurt Amrein, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Claudia Zampaloni
  • ORTHOGONAL PROTECTING GROUPS FOR THE PREPARATION OF STEREODEFINED PHOSPHOROTHIOATE OLIGONUCLEOTIDES
    Publication number: 20210179658
    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: Application
    Filed: March 20, 2018
    Publication date: June 17, 2021
    Inventors: Konrad Bleicher, Dennis Jul Hansen, Erik Daa Funder
  • 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 COMPRISING A PHOSPHORODITHIOATE INTERNUCLEOSIDE LINKAGE
    Publication number: 20200339982
    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 medicament.
    Type: Application
    Filed: December 21, 2018
    Publication date: October 29, 2020
    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
  • GAPMER OLIGONUCLEOTIDES COMPRISING A PHOSPHORODITHIOATE INTERNUCLEOSIDE LINKAGE
    Publication number: 20200332289
    Abstract: The present invention relates to a gapmer oligonucleotide comprising at 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 medicament.
    Type: Application
    Filed: December 21, 2018
    Publication date: October 22, 2020
    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
  • STEREODEFINED SUB-MOTIF OPTIMISATION METHODS
    Publication number: 20200318103
    Abstract: The present invention relates to methods for identifying improved stereodefined phosphorothioate oligonucleotide variants of antisense oligonucleotides utilising sub-libraries of partially stereodefined oligonucleotides. The methods allow for the efficient identification of stereodefined variants with improved properties, such as enhanced in vitro or in vivo activity, enhanced efficacy, enhanced specific activity, reduced toxicity, altered biodistribution, enhanced cellular or tissue uptake, and/or enhanced target specificity (reduced off-target effects).
    Type: Application
    Filed: April 13, 2020
    Publication date: October 8, 2020
    Inventors: Konrad Bleicher, Henrik Frydenlund Hansen, Troels Koch, Nanna Albaek, Erik Daa Funder