Patents Assigned to Bayer Pharma
  • 4H-pyrrolo[3,2-c]pyridin-4-one derivatives
    Patent number: 11339157
    Abstract: Compounds of formula (I) processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: May 24, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, Dana-Farber Cancer Institute, Inc., The Broad Institute, Inc.
    Inventors: Stephan Siegel, Franziska Siegel, Volker Schulze, Markus Berger, Keith Graham, Ulrich Klar, Knut Eis, Detlev Sülzle, Ulf Bömer, Daniel Korr, Kirstin Petersen, Ursula Mönning, Uwe Eberspächer, Dieter Moosmayer, Matthew Meyerson, Heidi Greulich, Bethany Kaplan, Hassan Youssef Harb, Phi Manh Dinh
  • Method for producing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4- chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclo-propylpropanoic acid and the crystalline form thereof for use as a pharmaceutical ingredient
    Patent number: 11332435
    Abstract: The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders.
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: May 17, 2022
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Peter Fey, Philipp Rubenbauer, Kai Lovis, Britta Olenik, Julia Kusel, Felix Spindler
  • Combination containing sGC activators and mineralocorticoid receptor antagonists
    Patent number: 11331308
    Abstract: The present invention relates to the combination of activators of soluble guanylate cyclase (sGC activators) with mineralocorticoid receptor antagonists (MR antagonists) and to the use of the combination for the treatment and/or prophylaxis of cardiac and cardiovascular disorders, of renal and cardiorenal disorders, of pulmonary and cardiopulmonary disorders and also for the treatment and/or prophylaxis of fibrotic disorders.
    Type: Grant
    Filed: October 5, 2017
    Date of Patent: May 17, 2022
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Peter Kolkhof, Peter Sandner
  • Amine substituted triazole derivatives and uses thereof
    Patent number: 11331314
    Abstract: The present invention relates to novel amine substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: May 17, 2022
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Marie-Pierre Collin-Kroepelin, Peter Kolkhof, Thomas Neubauer, Chantal Fuerstner, Elisabeth Pook, Hanna Tinel, Carsten Schmeck, Pierre Wasnaire, Heiko Schirmer, Klemens Lustig
  • RADIO-PHARMACEUTICAL COMPLEXES
    Publication number: 20220143229
    Abstract: The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a coupling moiety terminating in a carboxylic acid group; b) coupling said octadentate chelator to at least one tissue-targeting moiety targeting HER2; and c) contacting said tissue-targeting chelator with an aqueous solution comprising an ion of at least one alpha-emitting thorium isotope.
    Type: Application
    Filed: January 21, 2022
    Publication date: May 12, 2022
    Applicants: Bayer Pharma Aktiengesellschaft, Bayer AS
    Inventors: Lars LINDEN, Alan CUTHBERTSON
  • 2,4,5-TRISUBSTITUTED 1,2,4-TRIAZOLONES USEFUL AS INHIBITORS OF DHODH
    Publication number: 20220135536
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4, and R5 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 and prophylaxis of diseases, in particular hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: August 20, 2021
    Publication date: May 5, 2022
    Applicants: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus GRADL, Duy NGUYEN, Knut EIS, Judith GÜNTHER, Timo STELLFELD, Andreas JANZER, Sven CHRISTIAN, Thomas MÜLLER, Sherif El SHEIKH, David B. SYKES, Steven James FERRARA, Michael KRÖBER, Claudia MERZ, Michael NIEHUES, Martina SCHÄFER, Katja ZIMMERMANN, Carl Friedrich NISING
  • Pyrazolo-pyrrolo-pyrimidine-dione derivatives as P2X3 inhibitors
    Patent number: 11319324
    Abstract: The present invention covers substituted. Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R1, R2 and R3 are as defined herein, methods of 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 diseases, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: May 3, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Marcus Koppitz, Holger Siebeneicher, Nico Bräuer, Elisabeth Pook, Andrea Rotgeri, Roland Neuhaus, Oliver Martin Fischer, Jens Nagel, Adam James Davenport, James Lindsay Carr, Robert James Townsend, Nina Connelly Ursinyova, Shelley Anne Parrott
  • Substituted dihydroimidazopyridinediones as MKNK1 and MKNK2 inhibitors
    Patent number: 11311520
    Abstract: The present invention relates to substituted dihydroimidazopyridinedione compounds of general formula (I) as described and 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 a hyperproliferative, angiogenesis disorders, inflammatory diseases or diseases associated with inflammatory pain, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: August 3, 2020
    Date of Patent: April 26, 2022
    Assignees: Bayer Pharma Aktiengesellschaft, Bayer Aktiengesellschaft
    Inventors: Ulrich Klar, Rolf Bohlmann, Heike Schäcke, Detlev Sülzle, Stephan Menz, Olaf Panknin
  • 2-hetarylpyrimidine-4-carboxamides as aryl hydrocarbon receptor antagonists
    Patent number: 11304946
    Abstract: The present invention covers 2-hetarylpyrimidine-4-carboxamide compounds of general formula (I): in which X, Y, Z, R1, R2 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 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: April 19, 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
  • THE MONOHYDRATE OF ROGARATINIB HYDROCHLORIDE AND SOLID STATES THEREOF
    Publication number: 20220098201
    Abstract: Compound (III) which is the crystalline form of [4-{[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrrolo[2, -f] [1,2,4]triazin-7-yl]methyl}piperazin-2-one hydrochloride] which is the monohydrate, processes for its preparation, pharmaceutical compositions comprising it and its use in the control of disorders, including cancer.
    Type: Application
    Filed: January 27, 2020
    Publication date: March 31, 2022
    Applicants: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Jörg GRIES, Johannes PLATZEK, Claus-Christian HÄSELHOFF, Kai LOVIS
  • Macrocyclic fluorine substituted indole derivatives
    Patent number: 11286263
    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: March 29, 2022
    Assignees: The Broad Institute, Inc., Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Steven James Ferrara, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Laura Furst, Guo Wei, Patrick Ryan McCarren, Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Sack, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning
  • 7-SUBSTITUTED 1-ARYL-NAPHTHYRIDINE-3-CARBOXYLIC ACID AMIDES AND USE THEREOF
    Publication number: 20220089591
    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: Application
    Filed: January 28, 2021
    Publication date: March 24, 2022
    Applicants: 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
  • Process for preparing benzothiophen-2yl boronate
    Patent number: 11274110
    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: Grant
    Filed: October 18, 2018
    Date of Patent: March 15, 2022
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Jörg Gries, Johannes Platzek
  • COMPOSITIONS AND METHODS FOR CANCER EXPRESSING PDE3A OR SLFN12
    Publication number: 20220071995
    Abstract: The present invention features improved methods of identifying patients having cancer (e.g., melanoma, adenocarcinoma, lung, cervical, liver or breast cancer) using biomarkers (e.g., PDE3A, SLFN12) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., DNMDP, zardaverine, and anagrelide).
    Type: Application
    Filed: November 18, 2021
    Publication date: March 10, 2022
    Applicants: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., Bayer Pharma Aktiengesellschaft
    Inventors: Luc De Waal, Matthew Meyerson, Heidi Greulich, Monica Schenone, Alex Burgin, Xiaoyun Wu, Ulrike Sack
  • Use of chymase inhibitors for the treatment of endometriosis, post operative fibrosis and diseases which are characterized by fibrosis formation
    Patent number: 11266646
    Abstract: The present application relates to the use of bicyclic-substituted uracil derivatives, alone or in combinations with other active ingredients for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of inflammatory and fibrotic disorders, for the treatment of endometriosis, of endometriosis-associated fibrosis, of adenomyosis and of pain associated with an endometriosis disorder and also of postoperative peritoneal fibrosis and adhesion formation.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: March 8, 2022
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Michaele Peters, Markus Koch, Thomas Zollner
  • Radio-pharmaceutical complexes
    Patent number: 11260136
    Abstract: The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a coupling moiety terminating in a carboxylic acid group; b) coupling said octadentate chelator to at least one tissue-targeting moiety targeting HER2; and c) contacting said tissue-targeting chelator with an aqueous solution comprising an ion of at least one alpha-emitting thorium isotope. A method of treatment of a neoplastic or hyperplastic disease comprising admistration of such a tissue-targeting thorium complex, as well as the complex and corresponding pharmaceutical formulations are also provided.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: March 1, 2022
    Assignees: BAYER PHARMA AKTIENGESELLSCHAFT, Bayer AS
    Inventors: Lars Linden, Alan Cuthbertson
  • PTEFb inhibiting macrocyclic compounds
    Patent number: 11254690
    Abstract: The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: February 22, 2022
    Assignees: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER AKTIENGESELLSCHAFT
    Inventors: Ulrich Lücking, Daniel Hog, Clara Christ, Ulrike Sack, Franziska Siegel, Philip Lienau, Nicolas Werbeck
  • PTEFb inhibiting macrocyclic compounds
    Patent number: 11242356
    Abstract: The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: February 8, 2022
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Lücking, Daniel Hog, Clara Christ, Ulrike Sack, Franziska Siegel, Philip Lienau, Nicolas Werbeck
  • STIMULATORS AND/OR ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE (SGC) IN COMBINATION WITH AN INHIBITOR OF NEUTRAL ENDOPEPTIDASE (NEP INHIBITOR) AND/OR AN ANGIOTENSIN AII ANTAGONIST AND THE USE THEREOF
    Publication number: 20220023246
    Abstract: The present invention relates to stimulators and activators of soluble guanylate cyclase in combination with an inhibitor of neutral endopeptidase and/or angiotensin AII antagonists and the use thereof for the treatment and/or prophylaxis of cardiovascular disorders, for example heart failure with preserved ejection fraction or heart failure with reduced ejection fraction, renal disorders, for example chronic kidney failure, urological disorders, lung disorders, disorders of the central nervous system, for regulation of cerebral perfusion, for example in the event of vascular cerebral states of dementia, for the treatment and/or prophylaxis of fibrotic disorders and other disease symptoms (e.g. end organ damage affecting the brain, kidney or heart).
    Type: Application
    Filed: October 5, 2021
    Publication date: January 27, 2022
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Tobias MARQUARDT, Markus FOLLMANN, Johannes-Peter STASCH
  • Substituted triazole derivatives and uses thereof
    Patent number: 11230540
    Abstract: The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: January 25, 2022
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Marie-Pierre Collin-Kroepelin, Peter Kolkhof, Thomas Neubauer, Chantal Fuerstner, Elisabeth Pook, Hanna Tinel, Carsten Schmeck, Pierre Wasnaire, Heiko Schirmer, Klemens Lustig