Bayer Pharma Aktiengesellschaft

Deutsches Krebsforschungszentrum

Bayer Aktiengesellschaft

Bayer Intellectual Property Gmbh

Harvard College

The General Hospital Corporation

The Broad Institute, Inc.

Deutsches Krebsforschungszentrum Heidelberg

Detlef Stöckigt

Benjamin Bader

Michael Platten

Lars Röse

Ilona Gutcher

Ludwig Zorn

Antje Margret Wengner

Philip Lienau

Gerhard Siemeister

Norbert Schmees

Volker Schulze

Dirk Kosemund

Hans Briem

Marcus Koppitz

Judith Günther

Clara Christ

Ulf Bömer

Hans-Georg Lerchen

Knut Eis

Bernd Buchmann

Stefan Prechtl

Tobias Heinrich

David T Scadden

Ulrich Lücking

Lars Bärfacker

Anne Mengel

Jens Ackerstaff

Hartmut Schirok

Ursula Mönning

Timothy A Lewis

Thomas Brumby

Wilhelm Bone

Simon Holton

Ursula Krenz

Donald Bierer

Olaf Prien

Timo Stellfeld

Antonius Ter Laak

Bernard Jacques Haendler

Ulrike Röhn

Julien Lefranc

Horst Irlbacher

Christina Kober

Rafael Carretero

Roman Hillig

Michael Brüning

David B Sykes

Jens Schröder

Katrin Nowak-Reppel

Andreas Janzer

Daniel Gallenkamp

Naomi Barak

Rienk Offringa

Manfred Husemann

Jörg Weiske

Carlo Stresemann

Volker Badock

Jeffrey Stuart Mowat

Silke Köhr

Na Zhao

Florian Prinz

Joszef Bálint

Rosemary Helen Crampton

Ian Stefanuti

Ildikó Terebesi

Hanna Meyer

Gabriele Leder

Katrin Nowak-reppel

Anders Roland Friberg

Richard Alexander Bouglas

Hassan Y Harb

Ashley Eheim

Naomi Barack

Lars BÄRFACKER

Richard Alexander Bissell

Michael Bruening

The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compounds of general formula (1): in which X, R, R, R, Rand Rare 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.

2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer

The present invention covers 3-oxo-6-heteroaryl-2-phenyl-2,3-dihydropyri-dazine-4-carboxamide compounds of general formula (I): in which R, R, R, R, R, X, Y and Z 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. 

3-oxo-6-heteroaryl-2-phenyl-2,3-dihydropyridazine-4-carboxamides

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. 

2-phenylpyrimidine-4-carboxamides as AHR inhibitors

Disclosed are compounds of general formula (I): wherein R, R, 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.

Sulphur substituted 3-oxo-2,3-dihydropyridazine-4-carboxamides

The present invention covers 2-hetarylpyrimidine-4-carboxamide compounds of general formula (I): in which X, Y, Z, R, Rand Rare 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. 

2-hetarylpyrimidine-4-carboxamides as aryl hydrocarbon receptor antagonists

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&#x2032;-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid).

Compounds and methods useful for treating or preventing hematological cancers

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. 

3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides

The present invention covers heteroarylbenzimidazole compounds of general formula (I) in which R, R, R, Rand Rare 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 and/or inflammatory disorders, as a sole agent or in combination with other active ingredients. 

Heteroarylbenzimidazole compounds

The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I) wherein R, R, R, R, R, X and r have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyper-proliferative disorders, in particular for cancer, respectively tumor disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility. 

Aryl-cyanoguanidine compounds

The present invention relates to isothiazoles of general formula (I) which inhibit the mitotic checkpoint: in which A, R1 and R2 are as defined in the claims, 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 neoplasms, as a sole agent or in combination with other active ingredients. 

Amino-substituted isothiazoles

The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R, R, R, R, and Rare as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

Substituted triazolopyridines and their use as TTK inhibitors

The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.

Prodrug derivatives of substituted triazolopyridines

The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R, R, R, R, and Rare as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds. 

Substituted triazolopyridines

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Potsdam, Germany

Detlef Stöckigt