Patents by Inventor Simon Holton

Simon Holton 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).

  • AMIDO-SUBSTITUTED CYCLOHEXANE DERIVATIVES
    Publication number: 20180148418
    Abstract: The present invention relates to amido-substituted cyclohexane compounds of general formula (I), in which A, R4, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredient.
    Type: Application
    Filed: May 2, 2016
    Publication date: May 31, 2018
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Knut EIS, Jens ACKERSTAFF, Sarah WAGNER, Philipp BUCHGRABER, Detlev SÜLZLE, Simon HOLTON, Eckhard BENDER, Volkhart LI, Ningshu LIU, Franziska SIEGEL, Philip LIENAU, Michaela BAIRLEIN, Franz VON NUSSBAUM, Simon Anthony HERBERT, Marcus KOPPITZ
  • 2,3-benzodiazepines
    Patent number: 9890147
    Abstract: What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumor disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.
    Type: Grant
    Filed: August 13, 2013
    Date of Patent: February 13, 2018
    Assignee: Bayer Pharma Aktiengesellshaft
    Inventors: Stephan Siegel, Stefan Bäurle, Arwed Cleve, Bernard Haendler, Amaury Ernesto Fernandez-Montalvan, Ursula Mönning, Sabine Krause, Pascale Lejeune, Norbert Schmees, Matthias Busemann, Simon Holton, Joachim Kuhnke
  • Amido-substituted azole compounds
    Patent number: 9884063
    Abstract: The present invention relates to amido-substituted azole compounds of general formula (I), in which X1, X2, R1, R2, R4, R5, R7 and R8 are as defined in the claims which are inhibitors of TNKS1 and/or TNKS2, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: April 1, 2015
    Date of Patent: February 6, 2018
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Knut Eis, Jens Ackerstaff, Sarah Wagner, Daniel Basting, Stefan Golz, Eckhard Bender, Volkhart Min-Jian Li, Philip Lienau, Ningshu Liu, Franziska Siegel, Marcus Bauser, Detlev Sülzle, Simon Holton, Michaela Bairlein, Philipp Buchgraber, József Bálint
  • BENZYL SUBSTITUTED INDAZOLES AS BUB1 KINASE INHIBITORS
    Publication number: 20170305882
    Abstract: Compounds of formula (I) and their use as pharmaceuticals.
    Type: Application
    Filed: September 17, 2015
    Publication date: October 26, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Anne MENGEL, Hans-Georg LERCHEN, Thomas MÜLLER, Lars BÄRFACKER, Marion HITCHCOCK, Arwed CLEVE, Hans BRIEM, Gerhard SIEMEISTER, Wilhelm BONE, Amaury Ernesto FERNÁNDEZ-MONTÁLVAN, Jens SCHRÖDER, Ursula MÖNNING, Simon HOLTON
  • DIAMINOHETEROARYL SUBSTITUTED INDAZOLES
    Publication number: 20170283396
    Abstract: Compounds of formula (I) which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: March 28, 2017
    Publication date: October 5, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Christoph-Stephan HILGER, Marion HITCHCOCK, Hans BRIEM, Gerhard SIEMEISTER, Amaury Ernesto FERNANDEZ-MONTALVAN, Jens SCHRÖDER, Simon HOLTON, Cornelia PREUßE, Karsten DENNER
  • SUBSTITUTED CYCLOALKENOPYRAZOLES AS BUB1 INHIBITORS FOR THE TREATMENT OF CANCER
    Publication number: 20170275267
    Abstract: Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death.
    Type: Application
    Filed: March 8, 2017
    Publication date: September 28, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Marion HITCHCOCK, Christoph-Stephan HILGER, Anne MENGEL, Hans BRIEM, Simon HOLTON, Vera PÜTTER, Gerhard SIEMEISTER, Stefan PRECHTL, Amaury Ernesto FERNANDEZ-MONTALVAN, Christian STEGMANN, Cornelia PREUßE, Mark Jean GNOTH
  • BENZYL SUBSTITUTED INDAZOLES AS BUB1 INHIBITORS
    Publication number: 20170273980
    Abstract: Compounds of formula (I) as defined herein and their use as pharmaceuticals.
    Type: Application
    Filed: September 17, 2015
    Publication date: September 28, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Anne MENGEL, Hans-Georg LERCHEN, Manfred MÖWES, Thomas MÜLLER, Lars BÄRFACKER, Marion HITCHCOCK, Arwed CLEVE, Joachim KUHNKE, Hans BRIEM, Gerhard SIEMEISTER, Wilhelm BONE, Amaury Ernesto FERNANDEZ-MONTALVAN, Jens SCHRÖDER, Ursula MÖNNING, Simon HOLTON
  • HETEROARYL SUBSTITUTED INDAZOLES
    Publication number: 20170275268
    Abstract: Compounds of formula (I), which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: March 10, 2017
    Publication date: September 28, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Marion HITCHCOCK, Anne MENGEL, Christoph-Stephan HILGER, Lars BÄRFACKER, Hans BRIEM, Gerhard SIEMEISTER, Amaury Ernesto FERNANDEZ-MONTALVAN, Jens SCHRÖDER, Simon HOLTON, Cornelia PREUßE, Ursula MÖNNING
  • Substituted benzylpyrazoles
    Patent number: 9765058
    Abstract: Compounds of formula (I), and their use as pharmaceuticals.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: September 19, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Gerhard Siemeister, Wilhelm Bone, Amaury Ernesto Fernandez-Montalvan, Jens Schröder, Simon Holton, Cornelia Preuβe, Ursula Mönning
  • SUBSTITUTED BENZYLINDAZOLES FOR USE AS BUB1 KINASE INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISEASES
    Publication number: 20170260198
    Abstract: Compounds of formula (1) which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: February 21, 2017
    Publication date: September 14, 2017
    Applicants: Bayer Intellectual Property GmbH, Bayer Pharma Aktiengesellschaft
    Inventors: Marion HITCHCOCK, Anne MENGEL, Vera PÜTTER, Gerhard SIEMEISTER, Antje Margret WENGNER, Hans BRIEM, Knut EIS, Volker SCHULZE, Amaury Ernesto FERNANDEZ-MONTALVAN, Stefan PRECHTL, Simon HOLTON, Jörg FANGHÄNEL, Philip LIENAU, Cornelia PREUSSE, Mark Jean GNOTH
  • Heteroaryl substituted pyrazoles
    Patent number: 9745285
    Abstract: Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: August 29, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Anne Mengel, Marion Hitchcock, Anja Richter, Lars Bärfacker, Hans Briem, Gerhard Siemeister, Wilhelm Bone, Amaury Ernesto Fernandez-Montalvan, Jens Schröder, Simon Holton, Cornelia Preuβe, Ursula Mönning
  • Heteroaryl substituted pyrazoles
    Patent number: 9682974
    Abstract: Compounds of formula (I), processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: October 27, 2014
    Date of Patent: June 20, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Anne Mengel, Anja Richter, Marion Hitchcock, Hans Briem, Gerhard Siemeister, Wilhelm Bone, Amaury Ernesto Fernandez-Montalvan, Jens Schröder, Simon Holton, Cornelia Preuβe, Ursula Mönning
  • Triazolopyridines
    Patent number: 9676766
    Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: June 13, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Ulf Bömer
  • Substituted benzylpyrazoles
    Patent number: 9643953
    Abstract: Compounds of formula (I) and their use as pharmaceutical.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: May 9, 2017
    Assignees: BAYER INTELLECTUAL PROPERTY GMBH, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Knut Eis, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Simon Holton, Mark Jean Gnoth, Cornelia Preuβe
  • 3-AMINO-1,5,6,7-TETRAHYDRO-4H-INDOL-4-ONES
    Publication number: 20170101391
    Abstract: Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: June 17, 2015
    Publication date: April 13, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Keith GRAHAM, Ulrich KLAR, Hans BRIEM, Marion HITCHCOCK, Lars BÄRFACKER, Knut EIS, Volker SCHULZE, Gerhard SIEMEISTER, Wilhelm BONE, Jens SCHRÖDER, Simon HOLTON, Philip LIENAU, René TEMPEL, Helmut SONNENSCHEIN, Jozsef BÁLINT, Heinz GRAUBAUM
  • Substituted triazolopyridines
    Patent number: 9555022
    Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: January 31, 2017
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Marcus Koppitz, Detlef Stöckigt, Olaf Prien
  • AMIDO-SUBSTITUTED AZOLE COMPOUNDS
    Publication number: 20170020886
    Abstract: The present invention relates to amido-substituted azole compounds of general formula (I), in which X1, X2, R1, R2, R4, R5, R7 and R8 are as defined in the claims which are inhibitors of TNKS1 and/or TNKS2, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: April 1, 2015
    Publication date: January 26, 2017
    Inventors: Knut EIS, Jens ACKERSTAFF, Sarah WAGNER, Daniel BASTING, Stefanü GOLZ, Eckhard BENDER, Volkhart Min-Jian LI, Philip LIENAU, Ningshu LIU, Franziska SIEGEL, Marcus BAUSER, Detlev SÜLZLE, Simon HOLTON, Michaela BAIRLEIN, Philipp BUCHGRABER, Jözsef BÁLINTT
  • HETEROARYL SUBSTITUTED PYRAZOLES
    Publication number: 20160326159
    Abstract: Compounds of formula (I), processes for their preparation and their use as pharmaceuticals.
    Type: Application
    Filed: October 27, 2014
    Publication date: November 10, 2016
    Inventors: Anne MENGEL, Anja RICHTER, Marion HITCHCOCK, Hans BRIEM, Gerhard SIEMEISTER, Wilhelm BONE, Amaury Ernesto FERNANDEZ-MONTALVAN, Jens SCHRÖDER, Simon HOLTON, Cornelia PREUßE, Ursula MÖNNING
  • Substituted benzylpyrazoles
    Patent number: 9422268
    Abstract: Compounds of formula (I) and their use as pharmaceutical.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: August 23, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Knut Eis, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Simon Holton, Mark Jean Gnoth, Cornelia Preuβe
  • Substituted cycloalkenopyrazoles as BUB1 inhibitors for the treatment of cancer
    Patent number: 9416125
    Abstract: Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: August 16, 2016
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Marion Hitchcock, Christoph-Stephan Hilger, Anne Mengel, Hans Briem, Simon Holton, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Cornelia Preuβe, Mark Jean Gnoth