Patents by Inventor Boris Kroeplien

Boris Kroeplien 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).

  • MODULATOR ASSAY
    Publication number: 20230194541
    Abstract: It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. Anew assay for identifying compounds with this mechanism of action is also disclosed.
    Type: Application
    Filed: August 30, 2022
    Publication date: June 22, 2023
    Inventors: James Philip O'CONNELL, John Robert PORTER, Alastair LAWSON, Boris KROEPLIEN, Stephen Edward RAPECKI, Timothy John NORMAN, Graham John WARRELLOW
  • Method of identifying potential inhibitors of APO TNF? trimers
    Patent number: 11674967
    Abstract: A new, stable trimeric TNF? structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNF?/TNFR1 interaction. Membrane-bound TNF? is not affected in its ability to signal through TNFR2, and thus the new structure of TNF? may be used in therapies which do not significantly raise the risk of infection or malignancy.
    Type: Grant
    Filed: September 4, 2020
    Date of Patent: June 13, 2023
    Assignee: UCB BIOPHARMA SRL
    Inventors: James Philip O'Connell, John Robert Porter, Alastair Lawson, Boris Kroeplien, Stephen Edward Rapecki, Timothy John Norman, Graham John Warrellow, Tracy Lynn Arakaki, Alex Buntin Burgin, William Ross Pitt, Mark Daniel Calmiano, David Andreas Schubert, Daniel John Lightwood, Rebecca Jayne Munro
  • Method for identifying a modulator of the TNF? or CD40L interaction with their cognate receptors
    Patent number: 11448655
    Abstract: It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. A new assay for identifying compounds with this mechanism of action is also disclosed.
    Type: Grant
    Filed: May 26, 2020
    Date of Patent: September 20, 2022
    Assignee: UCB BIOPHARMA SRL
    Inventors: James Philip O'Connell, John Robert Porter, Alastair Lawson, Boris Kroeplien, Stephen Edward Rapecki, Timothy John Norman, Graham John Warrellow
  • MECHANISM OF ACTION
    Publication number: 20210140972
    Abstract: The invention is in the field of TNF signalling. Compounds have been identified which are capable of modulating signalling of TNF trimers through receptors. Methods of identifying such compounds are therefore provided. The compounds themselves have utility in therapy.
    Type: Application
    Filed: October 16, 2020
    Publication date: May 13, 2021
    Inventors: James Philip O'CONNELL, John Robert PORTER, Alastair LAWSON, Boris KROEPLIEN, Stephen Edward RAPECKI, Timothy John NORMAN, David James MCMILLAN, Graham John WARRELLOW, Daniel Christopher BROOKINGS, Rikki Peter ALEXANDER
  • NOVEL TNFa STRUCTURE FOR USE IN THERAPY
    Publication number: 20210088530
    Abstract: A new, stable trimeric TNF? structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNF?/TNFR1 interaction. Membrane-bound TNF? is not affected in its ability to signal through TNFR2, and thus the new structure of TNF? may be used in therapies which do not significantly raise the risk of infection or malignancy.
    Type: Application
    Filed: September 4, 2020
    Publication date: March 25, 2021
    Inventors: James Philip O'CONNELL, John Robert PORTER, Alastair LAWSON, Boris KROEPLIEN, Stephen Edward RAPECKI, Timothy John NORMAN, Graham John WARRELLOW, Tracy Lynn ARAKAKI, Alex Buntin BURGIN, William Ross PITT, Mark Daniel CALMIANO, David Andreas SCHUBERT, Daniel John LIGHTWOOD, Rebecca Jayne MUNRO
  • Methods of identifying signaling modulators of the trimeric TNFa
    Patent number: 10883996
    Abstract: The invention is in the field of TNF signalling. Compounds have been identified which are capable of modulating signalling of TNF trimers through receptors. Methods of identifying such compounds are therefore provided. The compounds themselves have utility in therapy.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: January 5, 2021
    Assignee: UCB BIOPHARMA SRL
    Inventors: James Philip O'Connell, John Robert Porter, Alastair Lawson, Boris Kroeplien, Stephen Edward Rapecki, Timothy John Norman, David James McMillan, Graham John Warrellow, Daniel Christopher Brookings, Rikki Peter Alexander
  • MODULATOR ASSAY
    Publication number: 20200400678
    Abstract: It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. A new assay for identifying compounds with this mechanism of action is also disclosed.
    Type: Application
    Filed: May 26, 2020
    Publication date: December 24, 2020
    Inventors: James Philip O'CONNELL, John Robert PORTER, Alastair LAWSON, Boris KROEPLIEN, Stephen Edward RAPECKI, Timothy John NORMAN, Graham John WARRELLOW
  • Treatment of autoimmune and inflammatory disorders with asymmetric TNF alpha trimers
    Patent number: 10775385
    Abstract: A new, stable trimeric TNF? structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNF?/TNFR1 interaction. Membrane-bound TNF? is not affected in its ability to signal through TNFR2, and thus the new structure of TNF? may be used in therapies which do not significantly raise the risk of infection or malignancy.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: September 15, 2020
    Assignee: UCB BIOPHARMA SRL
    Inventors: James Philip O'Connell, John Robert Porter, Alastair Lawson, Boris Kroeplien, Stephen Edward Rapecki, Timothy John Norman, Graham John Warrellow, Tracy Lynn Arakaki, Alex Buntin Burgin, William Ross Pitt, Mark Daniel Calmiano, David Andreas Schubert, Daniel John Lightwood, Rebecca Jayne Wootton
  • TNF receptor signaling modulator assay
    Patent number: 10705094
    Abstract: It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. A new assay for identifying compounds with this mechanism of action is also disclosed.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: July 7, 2020
    Assignee: UCB BIOPHARMA SRL
    Inventors: James Philip O'Connell, John Robert Porter, Alastair Lawson, Boris Kroeplien, Stephen Edward Rapecki, Timothy John Norman, Graham John Warrellow
  • Substituted benzo[b][1,4]oxazines and pyrido[3,2-b][1,4]oxazines as modulators of tumor necrosis factor activity
    Patent number: 10287299
    Abstract: A series of substituted 3,4-dihydro-2H-.1,4-benzoxazin-3-one derivatives, and analogs thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neuradegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: May 14, 2019
    Assignee: UCB Biopharma SPRL
    Inventors: Gareth Neil Brace, Prafulkumar Tulshibhai Chovatia, Gregory Foulkes, James Andrew Johnson, Severine Danielle Jones, Boris Kroeplien, Fabien Claude Lecomte, Pui Leng Loke, Martin Alexander Lowe, Ajay Mandal, Timothy John Norman, Christopher Francis Palmer, Yolanda Pérez-Fuertes, John Robert Porter, Donald Smyth, Giancarlo Trani, Muhammed Uddin, Zhaoning Zhu
  • Tetrahydrobenzimidazole derivatives as modulators of TNF activity
    Patent number: 10093652
    Abstract: A series of substituted 4,5,6,7-tetrahydrobenzimidazole derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: October 9, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Jag Paul Heer, Victoria Elizabeth Jackson, Boris Kroeplien, Fabien Claude Lecomte, John Robert Porter
  • Fused tricyclic imidazole derivatives as modulators of TNF activity
    Patent number: 10087179
    Abstract: A series of fused tricyclic imidazole derivatives, in particular dihydro-1H-cyclopenta[4,5]imidazo[1,2-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: October 2, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Rikki Peter Alexander, Gareth Neil Brace, Julien Alistair Brown, Mark Daniel Calmiano, Prafulkumar Tulshibhai Chovatia, Michael Deligny, Ellen Olivia Gallimore, Jag Paul Heer, Victoria Elizabeth Jackson, Boris Kroeplien, Malcolm MacCoss, Joanna Rachel Quincey, Yogesh Anil Sabnis, Dominique Louis Léon Swinnen, Zhaoning Zhu, Uwe Heinelt, Volkmar Wehner
  • NOVEL TNFalpha STRUCTURE FOR USE IN THERAPY
    Publication number: 20180231562
    Abstract: A new, stable trimeric TNF? structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNF?/TNFR1 interaction. Membrane-bound TNF? is not affected in its ability to signal through TNFR2, and thus the new structure of TNF? may be used in therapies which do not significantly raise the risk of infection or malignancy.
    Type: Application
    Filed: October 22, 2015
    Publication date: August 16, 2018
    Inventors: James Philip O'CONNELL, John Robert PORTER, Alastair LAWSON, Boris KROEPLIEN, Stephen Edward RAPECKI, Timothy John NORMAN, Graham John WARRELLOW, Tracy Lynn ARAKAKI, Alex Buntin BURGIN, William Ross PITT, Mark Daniel CALMIANO, David Andreas SCHUBERT, Daniel John LIGHTWOOD, Rebecca Jayne WOOTTON
  • Indazole Derivatives as Modulators of TNF Activity
    Publication number: 20180222868
    Abstract: A series of substituted indazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Application
    Filed: June 7, 2016
    Publication date: August 9, 2018
    Inventors: Prafulkumar Tulshibhai Chovatia, Martin Clive Hutchings, Boris Kroeplien, James Thomas Reuberson
  • MECHANISM OF ACTION
    Publication number: 20180203016
    Abstract: The invention is in the field of TNF signalling. Compounds have been identified which are capable of modulating signalling of TNF trimers through receptors. Methods of identifying such compounds are therefore provided. The compounds themselves have utility in therapy.
    Type: Application
    Filed: October 22, 2015
    Publication date: July 19, 2018
    Inventors: James Philip O'CONNELL, John Robert PORTER, Alastair LAWSON, Boris KROEPLIEN, Stephen Edward RAPECKI, Timothy John NORMAN, David James MCMILLAN, Graham John WARRELLOW, Daniel Christopher BROOKINGS, Rikki Peter ALEXANDER
  • Fused imidazole and pyrazole derivatives as modulators of TNF activity
    Patent number: 10004737
    Abstract: A series of substituted benzimidazole, imidazo[1,2-?]pyridine and pyrazolo[1,5-?]pyridine derivatives, and analogs thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: June 26, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Julien Alistair Brown, Mark Daniel Calmiano, Elizabeth Pearl Jones, Boris Kroeplien, James Thomas Reuberson, Matthew Duncan Selby, Michael Alan Shaw, Zhaoning Zhu
  • MODULATOR ASSAY
    Publication number: 20180172702
    Abstract: It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. A new assay for identifying compounds with this mechanism of action is also disclosed.
    Type: Application
    Filed: October 22, 2015
    Publication date: June 21, 2018
    Inventors: James Philip O'CONNELL, John Robert PORTER, Alastair LAWSON, Boris KROEPLIEN, Stephen Edward RAPECKI, Timothy John NORMAN, Graham John WARRELLOW
  • Purine derivatives as modulators of TNF activity
    Patent number: 9988383
    Abstract: A series of substituted purine derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: June 5, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Victoria Elizabeth Jackson, Boris Kroeplien, Martin Alexander Lowe, John Robert Porter
  • Benzoxazinone Derivatives and Analogues Thereof as Modulators of TNF Activity
    Publication number: 20180134728
    Abstract: A series of substituted 3,4-di-hydro-2H-.1,4-benzoxazin-3-one derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Application
    Filed: June 7, 2016
    Publication date: May 17, 2018
    Inventors: Gareth Neil Brace, Prafulkumar Tulshibhai Chovatia, Gregory Foulkes, James Andrew Johnson, Severine Danielle Jones, Boris Kroeplien, Fabien Claude Lecomte, Pui Leng Loke, Martin Alexander Lowe, Ajay Mandal, Timothy John Norman, Christopher Francis Palmer, Yolanda Pérez-Fuertes, John Robert Porter, Donald Smyth, Giancarlo Trani, Muhammed Uddin, Zhaoning Zhu
  • Tetrahydroimidazopyridine derivatives as modulators of TNF activity
    Patent number: 9969728
    Abstract: A series of substituted 5,6,7,8-tetrahydroimidazo[1,2-?]pyridine derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: May 15, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Sabine Defays, Jag Paul Heer, Victoria Elizabeth Jackson, James Andrew Johnson, Boris Kroeplien, John Robert Porter