Bayer Pharma Aktiengesellschaft

Bayer Aktiengesellschaft

Lisa Dietz

Frank Wunder

Alexandros Vakalopoulos

Johannes-Peter Stasch

Hans-Georg Lerchen

Anne-Sophie Rebstock

Beatrix Stelte-Ludwig

Tobias Marquardt

Simone Greven

Christoph Mahlert

Sandra Berndt

Volkhart Min-Jian Li

Damian Brockschnieder

Anette Sommer

Stephan Märsch

Stefanie Hammer

Timo Stellfeld

Dennis Kirchhoff

Hannah Joerissen

Markus Follmann

Gorden Redlich

Niels Lindner

Raimund Kast

Hartmut Beck

Philipp Buchgraber

Chantal Fuerstner

Jens Nagel

Sarah Anna Liesa Johannes

Carsten Terjung

Mark Meininghaus

Peter Hauff

Joerg Mueller

Karoline Droebner

Leo Marx

Michaela Bairlein

Johanna Anlahr

Min Jian Volkhart Li

Clemens-Jeremias Von Buehler

Peter Fey

Dieter Lang

Carsten Schmeck

Michael Hahn

Hanna Tinel

Yolanda Cancho Grande

Britta Olenik

Heiko Schirmer

Ingo Hartung

Sonja Anlauf

Sven Wittrock

Birgit Keil

Uwe Gritzan

Eva Maria Becker-Pelster

Ernst Weber

Thomas Mondritzki

Peter Sandner

Mark Trautwein

Christian Votsmeier

Ildiko Terebesi

Alexey Gromov

Dorian Schönfeld

Nikolaus Pawlowski

Julian Egger

Julian Marius Glück

Guido Becker

Uwe Muenster

Clemens Bothe

Ilka Mathar

Annett Richter

Lucas Hudson Hofmeister

Helene Faber

Bernd Rösler

Robert Alan Webster

Andre Philippe Dieskau

Patrick Jones

Lisa Candish

Melissa Boultadakis-arapinis

Nuria Ortega Hernandez

Marie-Pierre Collin-kröpelin

Johannes Nagelschmitz

Soundos Saleh

Tobias Mundry

Gerrit Weimann

David Jung

Mark Parry

David Ward

Cecile Vitre

Jenny Fitting

Jan Dreher

Léo Marx

Andre Dieskau

Hahn Michael G

Michael G Hahn

The invention relates to substituted pyrazolo piperidine carboxylic acids, their salts 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 and cardiac diseases, preferably heart failure with reduced and preserved ejection fraction (HFrEF, HFmrEF and HFpEF), hypertension (HTN), peripheral arterial diseases (PAD, PAOD), cardio-renal and kidney diseases, preferably chronic and diabetic kidney disease (CKD and DKD), cardiopulmonary and lung diseases, preferable pulmonary hypertension (PH), and other diseases, preferably neurodegenerative diseases and different forms of dementias, fibrotic diseases, systemic sclerosis (SSc), sickle cell disease (SCD), wound healing disorders such as diabetic foot ulcer (DFU).

Substituted pyrazolo piperidine carboxylic acids

The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), prefer-ably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid inform of mono hydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (P AH), chronic tromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 μg, preferably 480 to 2000 μg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid in form of mono hydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of treatment for the whole course of the disease, wherein the inhalative dosage form preferably comprises the combination of the active ingredient and a pharmaceutically suitable excipient or carrier, while preferably the active ingredient and a pharmaceutically suitable excipient are filled in a hard capsule.

Treatment of cardiopulmonary disorders

The invention relates to novel prodrugs or conjugates of the general formula (Ia) in which La, n, R and D have the definitions given in the description and which have a structural motif reduced to an asparagine derivative as cleavage site for tumour-associated proteases such as legumain, in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are released by legumain cleavage, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers. Reduction of the legumain-cleavable substrate peptide sequence to an asparagine derivative as structural motif, as a result of slowed legumain cleavage, achieves an increase in stability in the lysosomes of healthy organs while simultaneously maintaining the high anti-tumour effect.

Prodrugs of cytotoxic active agents having enzymatically cleavable groups

The invention relates to novel prodrugs or conjugates of the general formula (Ia) in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are masked with legumain-cleavable groups and hence release the drug, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers.

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.

Antibody drug conjugates (ADCs) having enzymatically cleavable groups

Antibody drug conjugates (ADCS) having enzymatically cleavable groups

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.

Specific antibody drug conjugates (ADCs) having KSP inhibitors

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.

Substituted N-arylethyl-2-aminoquinoline-4-carboxamides and use thereof

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.

Substituted-arylethyl-2-arylquinoline-4-carboxamides and use thereof

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.

Antibody drug conjugates of kinesin spindel protein (KSP) inhibitors with antiB7H3-antibodies

The present application relates to novel heteroaryl-substituted imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.

Heteroaryl-substituted imidazo[1,2-A]pyridines and their use

The present application relates to novel substituted pyrazolo[1,5-a]pyridine-3-carboxamides, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

Substituted pyrazolo[1,5-a]-pyridine-3-carboxamides and use thereof

The present application relates to novel substituted pyrazolo[1,5-a]pyridines of the formula (I-A) 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 cardiovascular disorders.

Substituted pyrazolo[1,5-A]pyridines and their use

The present application relates to novel substituted imidazo[1,2-a]pyrazine carboxamides of general formula (I) to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

N-substituted 8-[(2,6-difluorobenzyl)oxy]-2,6- dimethylimidazo[1,2-a]pyrazin-3-carboxamide derivatives as stimulators of soluble guanylate cyclase (SGC) for the treatment of cardiovascular diseases

The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.

Cyano-substituted imidazo[1,2-A]pyridinecarboxamides and their use

Growing community of inventors

Wuppertal, Germany

Lisa Dietz