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).

  • 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
  • PEPTIDE MACROCYCLES AND USE THEREOF IN THE TREATMENT OF BACTERIAL INFECTIONS
    Publication number: 20200040032
    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: Application
    Filed: October 8, 2019
    Publication date: February 6, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Konrad BLEICHER, Jérôme HERT, Carsten KROLL, Fabian DEY
  • ANTI-BACTERIAL PEPTIDE MACROCYCLES AND USE THEREOF
    Publication number: 20200040031
    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: Application
    Filed: April 9, 2018
    Publication date: February 6, 2020
    Inventors: Alexander Alanine, Kurt Amrein, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Claudia Zampaloni
  • PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
    Publication number: 20190321440
    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: April 19, 2019
    Publication date: October 24, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Konrad BLEICHER, Daniella CHEANG, Patrick DI GIORGIO, Taishan HU, Christian JENNY, Patrizio MATTEI, Petra SCHMITZ, Theodor STOLL
  • PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
    Publication number: 20190300569
    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: Application
    Filed: March 19, 2019
    Publication date: October 3, 2019
    Applicant: 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: 20190292213
    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 27, 2017
    Publication date: September 26, 2019
    Inventors: Konrad Bleicher, Joerg Duschmalé, Goutam Saha, Juber Abdulhamid Shaikh
  • PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
    Publication number: 20180362578
    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: June 12, 2018
    Publication date: December 20, 2018
    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
  • Lipidated incretin receptor ligand human immunoglobulin Fc-region fusion polypeptides
    Patent number: 10137170
    Abstract: Herein is reported a fusion polypeptide comprising i) one, two, three or four incretin receptor ligand polypeptides, and ii) one human immunoglobulin Fc-region, wherein at least one of the incretin receptor ligand polypeptides comprises an amino acid that is covalently conjugated to a lipid, and wherein each of the one, two, three or four incretin receptor ligand polypeptides is covalently conjugated by a peptide bond to a terminus of the human immunoglobulin Fc-region, whereby to each terminus of the human immunoglobulin Fc-region only a single incretin receptor ligand polypeptide is conjugated.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: November 27, 2018
    Assignees: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION, HOFFMANN-LA ROCHE INC.
    Inventors: Sara Belli, Konrad Bleicher, Richard D. Dimarchi, Eike Hoffmann, Eric A. Kitas, Anish A. Konkar
  • Peptide macrocycles against acinetobacter baumannii
    Patent number: 10030047
    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: October 27, 2016
    Date of Patent: July 24, 2018
    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
  • Peptides as oxytocin agonists
    Patent number: 9957298
    Abstract: The present compounds compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrome.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: May 1, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Konrad Bleicher, Christophe Grundschober
  • Peptides as oxytocin agonists
    Patent number: 9868766
    Abstract: The invention relates to compounds of formula wherein variables are defined herein. It has been found that the present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrom.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: January 16, 2018
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Caterina Bissantz, Konrad Bleicher, Christophe Grundschober
  • PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
    Publication number: 20170233437
    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: October 27, 2016
    Publication date: August 17, 2017
    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
  • PROCESSES FOR THE PREPARATION OF OXYTOCIN ANALOGUES
    Publication number: 20170174725
    Abstract: Provided herein is a process for the preparation of oxytocin receptor agonists that have the potential to be used for the treatment of neurological disorders.
    Type: Application
    Filed: February 7, 2017
    Publication date: June 22, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Anton Cueni, Kurt Puentener, Junichi Shiina
  • PEPTIDES AS OXYTOCIN AGONISTS
    Publication number: 20170081368
    Abstract: The present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post-traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrome.
    Type: Application
    Filed: December 5, 2016
    Publication date: March 23, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Konrad Bleicher, Kanchan Chakraborty, Christophe Grundschober, Goutam Saha
  • LIPIDATED INCRETIN RECEPTOR LIGAND HUMAN IMMUNOGLOBULIN FC-REGION FUSION POLYPEPTIDES
    Publication number: 20160310575
    Abstract: Herein is reported a fusion polypeptide comprising i) one, two, three or four incretin receptor ligand polypeptides, and ii) one human immunoglobulin Fc-region, wherein at least one of the incretin receptor ligand polypeptides comprises an amino acid that is covalently conjugated to a lipid, and wherein each of the one, two, three or four incretin receptor ligand polypeptides is covalently conjugated by a peptide bond to a terminus of the human immunoglobulin Fc-region, whereby to each terminus of the human immunoglobulin Fc-region only a single incretin receptor ligand polypeptide is conjugated.
    Type: Application
    Filed: December 19, 2014
    Publication date: October 27, 2016
    Inventors: Sara BELLI, Konrad BLEICHER, Richard D. DIMARCHI, Eike HOFFMANN, Eric A. KITAS, Anish A. KONKAR
  • PEPTIDES AS OXYTOCIN AGONISTS
    Publication number: 20150284434
    Abstract: The invention relates to compounds of formula wherein variables are defined herein. It has been found that the present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrom.
    Type: Application
    Filed: June 18, 2015
    Publication date: October 8, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Caterina Bissantz, Konrad Bleicher, Christophe Grundschober
  • Nitrogen containing heteroaryl compounds
    Patent number: 8703768
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
  • Nitrogen containing heteroaryl compounds
    Patent number: 8623866
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: January 7, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
  • Nitrogen-containing heteroaryl derivatives
    Patent number: 8470820
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: June 25, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento, Eric Vieira