Bayer Pharma Aktiengesellschaft

Bayer Intellectual Property Gmbh

Bayer Pharma Aktiengessellschaft

Matthias Busemann

Andrea Rotgeri

Ulrich Bothe

Tobias Marquardt

Oliver Martin Fischer

Naomi Barak

Joachim Kuhnke

Norbert Schmees

Arwed Cleve

Ursula Mönning

Ingo Hartung

Simon Holton

Amaury Ernesto Fernandez-Montalvan

Christian Stegmann

Stephan Siegel

Bernard Jacques Haendler

Stefan Bäurle

Pascale Lejeune

Sabine Krause

Isabella Gashaw

What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R, R, R, R, R, R, R, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumor disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.

2,3-benzodiazepines

The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis. 

Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (AKR1C3)

The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.

3-substituted estra-1,3,5(10),16-tetraene derivatives, methods for the production thereof, pharmaceutical preparations containing same, and use thereof for the production of medicaments

Estra-1,3,5(10),16-tetraene-3-carboxamide derivatives, processes for their preparation, pharmaceutical preparations comprising them and their use for preparing medicaments

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Berlin, Germany

Matthias Busemann