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
Abstract: The present invention features improved compounds, especially methods of identifying patients having cancer using biomarkers (e.g., PDE3A, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., Compounds 1-6 disclosed herein).
Type:
Application
Filed:
January 28, 2021
Publication date:
August 5, 2021
Applicants:
BAYER PHARMA AKTIENGESELLSCHAFT, THE BROAD INSTITUTE, INC., DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
TIMOTHY A. LEWIS, ALEX BURGIN, MONICA SCHENONE, XIAOYUN WU, HEIDI GREULICH, MATTHEW MEYERSON, LUC DE WAAL, ANTJE MARGRET WENGNER, KNUT EIS, PHILIP LIENAU, ULRIKE SACK, MARTIN LANGE
Abstract: The invention relates to specific Antibody-Drug-Conjugates (ADCs) with KSP inhibitors and anti-CD123-antibodies, to the use of these conjugates for the treatment and/or prophylaxis 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. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
Type:
Application
Filed:
April 8, 2021
Publication date:
July 29, 2021
Applicant:
Bayer Pharma Aktiengesellschaft
Inventors:
Hans-Georg LERCHEN, Anne-Sophie REBSTOCK, Yolanda CANCHO GRANDE, Sven WITTROCK, Beatrix STELTE-LUDWIG, Dennis KIRCHHOFF, Christoph MAHLERT, Simone GREVEN, Stephan MÄRSCH
Abstract: The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.
Type:
Grant
Filed:
June 20, 2016
Date of Patent:
July 27, 2021
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Hans-Georg Lerchen, Anne-Sophie Rebstock, Yolanda Cancho Grande, Sven Wittrock, Sandra Berndt, Uwe Gritzan, Jenny Fitting, Beatrix Stelte-Ludwig, Patrick Jones, Christoph Mahlert, Christian Votsmeier, Dorian Schönfeld, Mark Trautwein, Ernst Weber, Nikolaus Pawlowski, Simone Greven, Julian Marius Glück, Stefanie Hammer, Lisa Dietz, Stephan Märsch
Abstract: The present invention relates to use 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds for the treatment or prophylaxis of diseases which are associated with nerve fibre sensitization, in particular for treatment and prophylaxis of Chronic Cough (CC), Idiopathic Pulmonary Fibrosis (IPF), Chronic Obstructive Pulmonary Disorder (COPD), and asthma.
Abstract: The present invention relates to use 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds for the treatment or prophylaxis of diseases which are associated with nerve fiber sensitization, and/or other pathological conditions associated with autonomic imbalance caused by increased chemoreceptor sensitivity, in particular for the treatment of breathing disorders, Cheyne Stokes respiration, central and obstructive sleep apnea, cardiovascular disease, hypertension, resistant hypertension, and heart failure, which are related to increased activity of P2X3 receptors.
Abstract: The present invention relates to antibodies capable of binding to the coagulation Factor XI and/or its activated form factor XIa and methods of use thereof, particularly methods of use as agents inhibiting platelet aggregation and by this inhibits thrombus formation.
Type:
Grant
Filed:
March 4, 2019
Date of Patent:
June 29, 2021
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Andreas Wilmen, Julia Straßburger, Frank Dittmer, Michael Strerath, Anja Buchmüller, Joanna Grudzinska-Goebel, Ricarda Finnern, Martina Schäfer, Christoph Gerdes, Hannah Jörißen, Asako Itakura, Philberta Y. Leung, Erik Tucker
Abstract: The present invention covers 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I): in which R1, R2, R3, 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.
Inventors:
Norbert Schmees, Ilona Gutcher, Horst Irlbacher, Benjamin Bader, Na Zhao, Michael Platten, Ulrike Röhn, Ludwig Zorn, Lars Röse, Detlef Stöckigt
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:
Application
Filed:
November 26, 2018
Publication date:
June 17, 2021
Applicant:
Bayer Pharma Aktiengesellschaft
Inventors:
Peter FEY, Philipp RUBENBAUER, Kai LOVIS, Britta OLENIK, Julia KUSEL, Felix SPINDLER
Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also to the preparation of the enantiomer (Ia) by racemate resolution using chiral substituted tartaric acid esters of the general formulae (IIIa) and (IIIb) where Ar represents a substituted or unsubstituted aromatic or heteroaromatic radical.
Abstract: The invention relates to specific Antibody-Drug-Conjugates (ADCs) with KSP inhibitors and anti-CD 123-antibodies, to the use of these conjugates for the treatment and/or prophylaxis 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. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
Type:
Grant
Filed:
June 8, 2017
Date of Patent:
May 11, 2021
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Hans-Georg Lerchen, Anne-Sophie Rebstock, Yolanda Cancho Grande, Sven Wittrock, Beatrix Stelte-Ludwig, Dennis Kirchhoff, Christoph Mahlert, Simone Greven, Stephan Märsch