Abstract: The invention relates to a process for producing pharmaceutical dosage forms containing potent and selective TASK-1 and/or TASK-3 channel inhibitors, and to the use of the dosage forms obtained by the said production process to treat and/or prevent breathing disorders, including sleep-related breathing disorders such as obstructive and central sleep apnea and snoring.
Abstract: The present invention relates to: • combinations of: * a component A: which is a PI3K kinase inhibitor, such as copanlisib, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, in particular a physiologically acceptable salt, or a mixture of same, for example; * a component B: which is an androgen receptor antagonist, such as darolutamide or enzalutamide for example; and, optionally, * one or more pharmaceutical agents C; in which optionally either or both of said components A and B are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially; • use of such combinations: * in the treatment or prophylaxis of a cancer, particularly prostate cancer, or * for the preparation of a medicament for the treatment or prophylaxis of a cancer, particularly prostate cancer; • methods of treatment or prophylaxis of a cancer, particularly prostate cancer, in a subject, comprising administering to said subject
Type:
Grant
Filed:
June 21, 2018
Date of Patent:
November 30, 2021
Assignees:
BAYER CONSUMER CARE AG, BAYER PHARMA AKTIENGESELLSCHAFT
Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
Type:
Grant
Filed:
August 8, 2019
Date of Patent:
November 23, 2021
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Eloisa Jimenez Nunez, Jens Ackerstaff, Susanne Roehrig, Alexander Hillisch, Katharina Meier, Stefan Heitmeier, Adrian Tersteegen, Jan Stampfuss, Pascal Ellerbrock, Daniel Meibom, Dieter Lang
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.
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:
Grant
Filed:
July 15, 2016
Date of Patent:
November 9, 2021
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Tobias Marquardt, Markus Follmann, Johannes-Peter Stasch
Abstract: The present invention covers 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7-carboxamide compounds of general formula (I): in which R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5 and X 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, as a sole agent or in combination with other active ingredients.
Inventors:
Jörg Weiske, Carlo Stresemann, Stefan Nikolaus Gradl, Ulrike Röhn, Clara Christ, Holger Steuber, Manfred Husemann, Norbert Schmees, Kai Thede, Stephan Siegel, Antonius Ter Laak
Abstract: The present application relates to novel substituted N-arylethyl-2-aminoquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.
Inventors:
Hartmut Beck, Raimund Kast, Mark Meininghaus, Chantal Fuerstner, Timo Stellfeld, Clemens-Jeremias Von Buehler, Lisa Dietz, Michaela Bairlein, Johanna Anlahr, Hannah Joerissen, Peter Hauff, Joerg Mueller, Karoline Droebner, Jens Nagel
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:
October 19, 2021
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Marie-Pierre Collin-Kroepelin, Peter Kolkhof, Thomas Neubauer, Chantal Fuerstner, Elisabeth Pook, Matthias Beat Wittwer, Heiko Schirmer, Hanna Tinel
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.
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
Abstract: The present invention relates to combinations of at least two components, component A and component B, component A being an immune checkpoint inhibitor, and component B being a pharmaceutically acceptable salt of the alkaline-earth radio-nuclide radium-223, the combination being useful for the treatment or prophylaxis of cancer.
Abstract: The present invention features improved compounds, especially the compound having the structure (1). Compositions and methods of identifying patients having cancer using biomarkers (e.g., PDE3A, PDE3B, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention.
Type:
Grant
Filed:
February 1, 2018
Date of Patent:
October 12, 2021
Assignees:
The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
Inventors:
Timothy A. Lewis, Xiaoyun Wu, Heidi Greulich, Matthew Meyerson, Manuel Ellermann, Philip Lienau, Knut Eis, Antje Margret Wengner, Charlotte Christine Kopitz, Martin Lange
Abstract: The present application relates to novel substituted N-arylethyl-2-arylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.
Abstract: The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.
Abstract: The present invention relates to orally administrable modified-release pharmaceutical dosage forms comprising (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid and to processes for producing the dosage forms and to the use thereof for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiac, renal, pulmonary and ophthalmological disorders, disorders of the central nervous system, fibrotic and inflammatory disorders and metabolic disorders.
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.
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
Abstract: The present invention relates to novel diazabicyclically substituted imidazo[1,2-a]pyrimidine derivatives, to methods for producing the same, to the use thereof either alone or in combinations for the treatment and/or prevention of diseases, as well as to their use for preparing medicaments for the treatment and/or prevention of diseases, especially for treatment and/or prevention of breathing disorders, including sleep-related breathing disorders such as obstructive and central sleep apnoea and snoring.
Inventors:
Martina Delbeck, Michael Hahn, Thomas Müller, Klemens Lustig, Karl Collins, Niels Lindner, Janine Nicolai, Moritz Beck-Broichsitter, Udo Albus, Doris Gehring, Björn Rosenstein
Abstract: The present invention includes methods of treating patients with acute myeloid leukemia across a range of genetic subtypes with DHODH inhibitors, such as 6-fluoro-2-(2?-fluoro-[1,1?-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid).
Type:
Grant
Filed:
August 29, 2016
Date of Patent:
August 24, 2021
Assignees:
THE BROAD INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATION, PRESIDENT AND FELLOWS OF HARVARD COLLEGE, BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
David B. Sykes, David Scadden, Timothy A. Lewis, Andreas Janzer, Hanna Meyer, Detlef Stöckigt
Abstract: The present invention covers a method for preparing 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine (“the compound of formula (I)” in the following) as well as intermediate compounds useful in the preparation of the compound of formula (I). The present invention also covers polymorphic form B of the compound of formula (I) with very high purity.
Inventors:
Johannes PLATZEK, Philipp RUBENBAUER, Hendricus Nicolaas Sebastiaan VAN DER HAAS, Sonja Elisabeth HOOGEVEEN, Matthijs Cornelis Maria VAN OERS, Reinerus Gerardus GIELING, Jeroen Alexander DEKKER
Abstract: The present invention relates to novel 5-(carboxamide)-1-pyridinyl-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:
September 23, 2019
Date of Patent:
August 17, 2021
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Marie-Pierre Collin, Peter Kolkhof, Thomas Neubauer, Chantal Fuerstner, Elisabeth Pook, Matthias Beat Wittwer, Klemens Lustig, Anja Buchmueller, Hanna Tinel, Karoline Droebner, Thomas Mondritzki, Heiko Schirmer, Axel Kretschmer, Carsten Schmeck, Pierre Wasnaire, Hana Cernecka
Abstract: The present invention relates to novel Mannose-binding lectin (MBL)-associated serine protease (MASP) inhibitory compounds, as well as analogues and derivatives thereof, to processes for the preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of renal and cardiovascular disorders and of ischemia reperfusion injuries.
Inventors:
Donald BIERER, Ingo FLAMME, Dmitry ZUBOV, Thomas NEUBAUER, Adrian TERSTEEGEN, Cathleen JUHL, Marie GLATZ, Jan DREHER, Simon HOLTON, Carsten TERJUNG, Lars BAUMANN, Thorsten POETHKO, Jiancheng XIONG, Yibo QIU