Patents by Inventor Olaf Kinzel

Olaf Kinzel 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).

  • Amide substituted thiazoles as modulators of RORyt
    Patent number: 9845319
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R5, A1, A2, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: December 19, 2017
    Assignee: Janssen Pharmaceutiuca NV
    Inventors: Steven Goldberg, Hariharan Venkatesan, Virginia Tanis, Maud Urbanski, Aihua Wang, David Kummer, Christoph Steeneck, Christian Gege, Olaf Kinzel, Gerald Kleymann, Thomas Hoffmann, Anne M. Fourie, Xiaohua Xue
  • FXR (NR1H4) binding and activity modulating compounds
    Patent number: 9820979
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: December 5, 2016
    Date of Patent: November 21, 2017
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Olaf Kinzel, Christoph Steeneck, Claus Kremoser
  • TRIFLUOROMETHYL ALCOHOLS AS MODULATORS OF RORyt
    Publication number: 20170327492
    Abstract: The present invention comprises methods of making 5-(2,3-dichloro-4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2-hydroxy-2-methylpropyl)-4-(R1-1-carbonyl)thiazole-2-carboxamide, wherein R1 is defined in the specification.
    Type: Application
    Filed: July 31, 2017
    Publication date: November 16, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Steven Goldberg, Hariharan Venkatesan, Olaf Kinzel, Christian Gege, Christoph Steeneck, Gerald Kleymann, Thomas Hoffmann
  • Pyrrolo carboxamides as modulators of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR?, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
    Patent number: 9815851
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: November 14, 2017
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • NOVEL FXR (NR1H4) MODULATING COMPOUNDS
    Publication number: 20170298068
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Application
    Filed: December 16, 2015
    Publication date: October 19, 2017
    Inventors: CHRISTIAN GEGE, Claus Kremoser, Olaf Kinzel, Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Aaron C. Schmitt, William J. Watkins, Jianjun Xu
  • Hydroxy containing FXR (NR1H4) modulating compounds
    Patent number: 9751874
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: September 5, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Christian Gege, Olaf Kinzel, Claus Kremoser, Aaron C. Schmitt
  • NOVEL FXR (NR1H4) BINDING AND ACTIVITY MODULATING COMPOUNDS
    Publication number: 20170143684
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Application
    Filed: December 5, 2016
    Publication date: May 25, 2017
    Inventors: Olaf Kinzel, Christoph Steeneck, Claus Kremoser
  • FXR (NR1H4) binding and activity modulating compounds
    Patent number: 9539244
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: August 12, 2015
    Date of Patent: January 10, 2017
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Olaf Kinzel, Christoph Steeneck, Claus Kremoser
  • Carboxamide or sulfonamide substituted nitrogen-containing 5-membered heterocycles as modulators for the orphan nuclear receptor ROR?
    Patent number: 9458104
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 29, 2013
    Date of Patent: October 4, 2016
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Christian Gege, Olaf Kinzel, Christoph Steeneck, Gerald Kleymann, Thomas Hoffmann
  • HYDROXY CONTAINING FXR (NR1H4) MODULATING COMPOUNDS
    Publication number: 20160176861
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Application
    Filed: December 16, 2015
    Publication date: June 23, 2016
    Inventors: Christian Gege, Olaf Kinzel, Claus Kremoser, Aaron C. Schmitt
  • AMIDE SUBSTITUTED THIAZOLES AS MODULATORS OF RORyt
    Publication number: 20160122335
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R5, A1, A2, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 30, 2015
    Publication date: May 5, 2016
    Applicant: Janssen Pharmaceutica NV
    Inventors: Steven Goldberg, Hariharan Venkatesan, Virginia Tanis, Maud Urbanski, Aihua Wang, David Kummer, Christoph Steeneck, Christian Gege, Olaf Kinzel, Gerald Kleymann, Thomas Hoffmann
  • TRIFLUOROMETHYL ALCOHOLS AS MODULATORS OF RORyt
    Publication number: 20160122336
    Abstract: The present invention comprises compounds of Formula I. wherein: X, A1, A2, A3, A4, R1, R2, and R3 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 30, 2015
    Publication date: May 5, 2016
    Applicant: Janssen Pharmaceutica NV
    Inventors: Steven Goldberg, Hariharan Venkatesan, Virginia Tanis, Olaf Kinzel, Christian Gege, Christoph Steeneck, Gerald Kleymann, Thomas Hoffmann
  • THIAZOLES AS MODULATORS OF RORyt
    Publication number: 20160120850
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R7, R8, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 30, 2015
    Publication date: May 5, 2016
    Applicant: Janssen Pharmaceutica NV
    Inventors: Steven Goldberg, Christoph Steeneck, Christian Gege, Olaf Kinzel, Gerald Kleymann, Thomas Hoffmann
  • CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED NITROGEN-CONTAINING 5-MEMBERED HETEROCYCLES AS MODULATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR GAMMA
    Publication number: 20150344423
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: May 29, 2013
    Publication date: December 3, 2015
    Inventors: Christian GEGE, Olaf KINZEL, Christoph STEENECK, Gerald KLEYMANN, Thomas HOFFMANN
  • NOVEL FXR (NR1H4) BINDING AND ACTIVITY MODULATING COMPOUNDS
    Publication number: 20150342930
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Application
    Filed: August 12, 2015
    Publication date: December 3, 2015
    Inventors: Olaf Kinzel, Christoph Steeneck, Claus Kremoser
  • FXR (NR1H4) binding and activity modulating compounds
    Patent number: 9139539
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: September 22, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Olaf Kinzel, Christoph Steeneck, Claus Kremoser
  • CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED THIAZOLES AND RELATED DERIVATIVES AS MODULATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR[GAMMA]
    Publication number: 20150175562
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide or sulfonamide containing cyclic compounds of Formula (1), (1?), (100), (100?), (200) and (200?) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: May 29, 2013
    Publication date: June 25, 2015
    Inventors: Christian Gege, Christoph Steeneck, Olaf Kinzel, Gerald Kleymann, Thomas Hoffmann
  • FXR (NR1H4) binding and activity modulating compounds
    Patent number: 8952042
    Abstract: The present invention relates to compounds of formula (1): where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: February 10, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Claus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
  • Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-? (ROR-?, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
    Patent number: 8946446
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: February 3, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR?, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune disease
    Patent number: 8940722
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: January 27, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Olaf Kinzel, Christoph Steeneck, Gerald Kleymann, Michael Albers, Thomas Hoffmann, Claus Kremoser, Sanja Perovic-Ottstadt, Thomas Schlüter