Novartis Ag

Schering Aktiengesellschaft

Bayer Intellectual Property Gmbh

Bayer Pharma Aktiengesellschaft

Bayer Schering Pharma Ag

Piramal Imaging Sa

Martin Krüger

Pascal Furet

Andreas Huth

Guido Bold

Dieter Seidelmann

Andreas Menrad

Jeanette Marjorie Wood

Ulrich Lücking

Gerhard Siemeister

Rolf Bohlmann

Paul William Manley

Martin Haberey

Karl-Heinz Altmann

Francesco Hofmann

Hans Briem

Eckhard Ottow

Markus Berger

Karl-Heinz Thierauch

Jürgen Mestan

Stefano Ferrari

Rolf Jautelat

Joachim Kuhnke

Duy Nguyen

Norbert Schmees

Anne Mengel

Roland Neuhaus

Ulrich Bothe

Ingo Hartung

Georg Kettschau

Amaury Ernesto Fernandez-Montalvan

Stuart Ince

Olaf Prien

Holger Siebeneicher

Holger Hess-Stumpp

Stephan Siegel

Bernard Jacques Haendler

Jessica Lohrke

Arne Von Bonin

Michael Schirner

Ulf Boemer

Daniel Gallenkamp

Oliver Von Ahsen

Michael Reinhardt

Pascale Lejeune

Hermann Künzer

Jose Brüggen

Krolikiewicz Konrad

Hermann KÜNZER

The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R, R, Rand Rhave the meanings given for the general formula (I),to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.

BET protein-inhibiting 5-aryltriazoleazepines

This invention relates to pyrimidine derivatives of general formula I in which Q, R, R, R, R, R, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.

Sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents

The invention relates to sulfoximine-substituted pyrimidines of the general formula I processes for the preparation thereof and their use as drugs.

Sulfoximine-substituted pyrimidines, processes for production thereof and use thereof as drugs

The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.

Anthranilic acid amides and the use thereof as medicaments

Described are compunds of formula (I), wherein W is O or S; X is NR; Y is CRR&#x2014;(CH)n wherein Rand Rare independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO; Ris aryl; Ris a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that Rcannot represent 2-phthalimidyl, and in case of Y=SOcannot represent 2,1,3-benzothiadiazol-4-yl; any of R, R, Rand R, independently of the other, is H or a substituent other than hydrogen; and Rand R, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

N-Aryl (thio) anthranilic acid amide derivatives, their preparation and their use as VEGF

Described are compunds of formula (I), wherein W is O or S; X is NR; Y is CRR&#x2014;(CH)n wherein Rand Rare independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO; Ris aryl; Ris a bicyclic heteroaryl group comprising one ring nitrogen atom with the exception that Rcannot represent 2-phthalimidyl; any of R, R, Rand R, independently of the other, is H or a substituent other than hydrogen; and Rand R, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

VEGF receptor tyrosine kinase inhibitors

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Berlin, Germany

Martin Krüger