Patents Assigned to Bayer Pharma Aktiengesellschaft
  • ANALOGUES OF 3-(5-METHYL-1,3-THIAZOL-2-YL)-N-{(1R)-1-[2-(TRIFLUORO-METHYL)PYRIMIDIN-5-YL]ETHYL}BENZAMIDE
    Publication number: 20230013419
    Abstract: The present invention covers P2X3 inhibitor compounds of general formula (I) in which R1 and R2 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: June 25, 2020
    Publication date: January 19, 2023
    Applicants: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Antje ROTTMANN, Oliver Martin FISCHER, Kai THEDE, Simon Anthony HERBERT, Ursula GANZER, Andrea ROTGERI, Elisabeth POOK
  • Preparative process
    Patent number: 11542245
    Abstract: The present invention relates to a process for preparing 4-{[(2S)-2-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl}butanoyl]amino}-2-fluorobenzamide (I) or 4-({(2S)-2-[4-{5-chloro-2-[4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl]phenyl}-5-methoxy-2-oxopyridin-1(2H)-yl]butanoyl}amino)-2-fluorobenzamide (II) from 2,5-dimethoxypyridine (III), 1-(2-bromo-4-chlorophenyl)-4-chloro-1H-1,2,3-triazole (X-Cl) or 1-(2-bromo-4-chlorophenyl)-4-(trifluoromethyl)-1H-1,2,3-triazole (X-CF3), 4-amino-2-fluorbenzamide (XIII) and (2R)-2-aminobutanoic acid (XVII).
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: January 3, 2023
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Julian Egger, Daniel Goetz, Michal Sowa
  • 2-(morpholin-4-yl)-1,7-naphthyridines
    Patent number: 11529356
    Abstract: The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), 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 a hyperproliferative disease as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: August 21, 2020
    Date of Patent: December 20, 2022
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Lars Wortmann, Ulrich Lücking, Julien Lefranc, Hans Briem, Marcus Koppitz, Knut Eis, Franz Von Nussbaum, Benjamin Bader, Antje Margret Wengner, Gerhard Siemeister, Wilhelm Bone, Philip Lienau, Joanna Grudzinska-Goebel, Dieter Moosmayer, Uwe Eberspächer, Hans Schick
  • DIHYDROOXADIAZINONES
    Publication number: 20220396554
    Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I) in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: July 14, 2022
    Publication date: December 15, 2022
    Applicants: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Manuel ELLERMANN, Stefan Nikolaus GRADL, Charlotte Christine KOPITZ, Martin LANGE, Adrian TERSTEEGEN, Philip LIENAU, Christa HEGELE-HARTUNG, Detlev SÜLZLE, Timothy A. LEWIS, Heidi GREULICH, Xiaoyun WU, Matthew MEYERSON, Alex BURGIN
  • 2-phenylpyrimidine-4-carboxamides as AHR inhibitors
    Patent number: 11524944
    Abstract: The present invention covers 2-phenylpyrimidine-4-carboxamide compounds of general formula (I): (I) 5 in which X, Y, Z, R1, R2, R4, R5 and R6 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 16, 2018
    Date of Patent: December 13, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, Deutsches Krebsforschungszentrum
    Inventors: Julien Lefranc, Norbert Schmees, Ulrike Röhn, Ludwig Zorn, Judith Günther, Ilona Gutcher, Lars Röse, Benjamin Bader, Detlef Stöckigt, Michael Platten
  • Aromatic sulfonamide derivatives
    Patent number: 11524938
    Abstract: Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.
    Type: Grant
    Filed: October 9, 2020
    Date of Patent: December 13, 2022
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Stefan Werner, Stefanie Mesch, Arwed Cleve, Nico Bräuer, Simon Anthony Herbert, Markus Koch, Henrik Dahllöf, Maren Osmers, Elizabeth Hardaker, Anton Lishchynskyi
  • SUBSTITUTED INDAZOLES, METHODS FOR THE PRODUCTION THEREOF, PHARMACEUTICAL PREPARATIONS THAT CONTAIN SAID NEW SUBSTITUTED INDAZOLES, AND USE OF SAID NEW SUBSTITUTED INDAZOLES TO PRODUCE DRUGS
    Publication number: 20220388982
    Abstract: The present application relates to novel substituted indazoles, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis and endometriosis-associated pain and other endometriosis-associated symptoms such as dysmenorrhoea, dyspareunia, dysuria and dyschezia, of lymphoma, rheumatoid arthritis, spondyloarthritis (especially psoriatic spondyloarthritis and Bekhterev's disease), lupus erythematosus, multiple sclerosis, macular degeneration, COPD, gout, fatty liver disorders, insulin resistance, neoplastic disorders and psoriasis.
    Type: Application
    Filed: July 20, 2022
    Publication date: December 8, 2022
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich BOTHE, Holger SIEBENEICHER, Nicole SCHMIDT, Reinhard NUBBEMEYER, Ulf BÖMER, Judith GÜNTHER, Holger STEUBER, Martin LANGE, Christian STEGMANN, Andreas SUTTER, Alexandra RAUSCH, Christian FRIEDRICH, Peter HAUFF
  • PROCESS FOR PREPARING BENZOTHIOPHEN-2YL BORONATE
    Publication number: 20220356194
    Abstract: A process for preparing the benzothiophen-2-yl boronate of formula (VI) which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of proliferative disorders, such as cancer and tumor diseases.
    Type: Application
    Filed: March 10, 2022
    Publication date: November 10, 2022
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Jörg GRIES, Johannes PLATZEK
  • Gadolinium chelate compounds for use in magnetic resonance imaging
    Patent number: 11491245
    Abstract: A compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[({2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl}amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclo dodecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.
    Type: Grant
    Filed: July 27, 2020
    Date of Patent: November 8, 2022
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Markus Berger, Jessica Lohrke, Christoph-Stephan Hilger, Gregor Jost, Thomas Frenzel, Detlev Suelzle, Johannes Platzek, Olaf Panknin, Hubertus Pietsch
  • Macrocyclic indole derivatives
    Patent number: 11492358
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I) in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: February 26, 2021
    Date of Patent: November 8, 2022
    Assignees: The Broad Institute, Inc., Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Clara Christ, Kai Thede, Joachim Kuhnke, Manfred Moewes, Knut Eis, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning, Philip Lienau, Ulrike Sack, Arne Scholz, Michael H. Serrano-Wu, Christopher Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Laura Furst, Guo Wei, Patrick Ryan McCarren
  • Macrocyclic chlorine substituted indole derivatives
    Patent number: 11478451
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: October 25, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc.
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Moenning, Katrin Nowak-Reppel, Chris Lemke, Michael H. Serrano-Wu, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven J. Ferrara, Laura Furst, Guo Wei, Patrick R. McCarren, Rebecca Ann Harvey, Daniel Payne, Thomas Pesnot, Craig Wilson
  • Antibody drug conjugates (ADCS) having enzymatically cleavable groups
    Patent number: 11478554
    Abstract: The invention relates to novel binder-drug conjugates (ADCs) having improved properties, to active metabolites of these ADCs and to processes for their preparation. The present invention furthermore relates to the use of these conjugates for the treatment and/or prevention of diseases and to the use of these conjugates for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases.
    Type: Grant
    Filed: September 1, 2021
    Date of Patent: October 25, 2022
    Assignees: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER AKTIENGESELLSCHAFT
    Inventors: Hans-Georg Lerchen, Anne-Sophie Rebstock, Beatrix Stelte-Ludwig, Dennis Kirchhoff, Lisa Dietz, Christoph Mahlert, Simone Greven, Stephan Märsch, Sandra Berndt, Anette Sommer, Stefanie Hammer
  • 7-substituted 1-aryl-naphthyridine-3-carboxylic acid amides and use thereof
    Patent number: 11472803
    Abstract: The present application relates to novel 7-substituted 1-arylnaphthyridine-3-carboxamides, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prevention of diseases, and to their use for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders and/or renal disorders.
    Type: Grant
    Filed: January 28, 2021
    Date of Patent: October 18, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Henrik Teller, Alexandros Vakalopoulos, Melissa Boultadakis Arapinis, Alexander Straub, Hanna Tinel, Markus Brechmann, Matthias Beat Wittwer, Maximillian Andreas Kullmann, Till Freudenberger, Thomas Mondritzki, Tobias Marquardt
  • AROMATIC SULFONAMIDE DERIVATIVES
    Publication number: 20220324807
    Abstract: Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.
    Type: Application
    Filed: October 9, 2020
    Publication date: October 13, 2022
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Stefan WERNER, Stefanie MESCH, Arwed CLEVE, Nico BRÄUER, Simon Anthony HERBERT, Markus KOCH, Henrik DAHLLÖF, Maren OSMERS, Elizabeth HARDAKER, Anton LISHCHYNSKYI
  • Sulphur substituted 3-oxo-2,3-dihydropyridazine-4-carboxamides
    Patent number: 11459312
    Abstract: Disclosed are compounds of general formula (I): wherein R1, R2, A, X, Y and Z are as defined herein, methods of preparing the compounds, intermediate compounds useful for preparing the compounds, pharmaceutical compositions and combinations comprising the compounds and the use of the compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 16, 2018
    Date of Patent: October 4, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, Deutsches Krebsforschungszentrum
    Inventors: Ludwig Zorn, Ulrike Röhn, Ilona Gutcher, Lars Röse, Benjamin Bader, Christina Kober, Rafael Carretero, Detlef Stöckigt, Michael Platten
  • Macrocyclic chlorine substituted indole derivatives
    Patent number: 11447504
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: September 20, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc.
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Moenning, Katrin Nowak-Reppel, Jérémie Xavier Mortier, Patrick R. McCarren, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven J. Ferrara, Laura Furst, Guo Wei, Rebecca Ann Harvey, Daniel Payne, Thomas Pesnot, Craig Wilson
  • Specific antibody drug conjugates (ADCs) having KSP inhibitors
    Patent number: 11433140
    Abstract: Specific binder-drug conjugates (ADCs) of kinesin spindle protein inhibitors, effective metabolites of these ADCs, processes for preparing these ADCs, the use of these ADCs for the treatment and/or prevention of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases, are described.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: September 6, 2022
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Hans-Georg Lerchen, Anne-Sophie Rebstock, Beatrix Stelte-Ludwig, Dennis Kirchhoff, Sandra Berndt, Lisa Dietz, Stephan Märsch, Stefanie Hammer
  • 2-METHYL-AZA-QUINAZOLINES
    Publication number: 20220274979
    Abstract: The present invention covers 2-methyl-aza-quinazoline compounds of general formula (I) as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients
    Type: Application
    Filed: April 15, 2019
    Publication date: September 1, 2022
    Applicants: Bayer Pharma Aktiengesellschaft, Bayer Healthcare China
    Inventors: Lars WORTMANN, Brice SAUTIER, Knut EIS, Hans BRIEM, Niels BÖHNKE, Franz VON NUSSBAUM, Roman HILIG, Benjamin BADER, Jens SCHRÖDER, Kirstin PETERSEN, Philip LIENAU, Antje Margret WENGNER, Dieter MOOSMAYER, Qiuwen WANG, Hans SCHICK
  • Substituted pyrrolopyridine-derivatives
    Patent number: 11427578
    Abstract: The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I), in which A, X, R1, R2a, R2b, R3a, R3b, R4a and R4b are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: August 30, 2022
    Assignees: Bayer Pharma Aktiengesellschaft, Bayer Aktiengesellschaft, Deutsches Krebsforschungszentrum
    Inventors: Jeffrey Stuart Mowat, Bernd Buchmann, Nuria Aiguabella Font, Gabriele Leder, Rafael Carretero, Olaf Panknin, Roland Neuhaus, Robin Michael Meier, Sandra Berndt, Kirstin Petersen, Rienk Offringa
  • Dihydrooxadiazinones
    Patent number: 11427553
    Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: August 2, 2018
    Date of Patent: August 30, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Manuel Ellermann, Stefan Nikolaus Gradl, Charlotte Christine Kopitz, Martin Lange, Adrian Tersteegen, Philip Lienau, Christa Hegele-Hartung, Detlev Sülzle, Timothy A. Lewis, Heidi Greulich, Xiaoyun Wu, Matthew Meyerson, Alex Burgin