Bayer Pharma Aktiengesellschaft

Bayer Aktiengesellschaft

Deutsches Krebsforschungszentrum

Deutsches Krebsforschungszentrum Stiftung Des Offentlichen Rechts

Olaf Panknin

Katja Zimmermann

Roland Neuhaus

Thomas Frenzel

Markus Berger

Christoph-Stephan Hilger

Gregor Jost

Hubertus Pietsch

Jessica Lohrke

Hartmut Rehwinkel

Duy Nguyen

Sven Ring

Johannes Platzek

Marcus Bauser

Sonja Anlauf

Stefan Kaulfuss

Detlev Suelzle

Wolfgang Schwede

Holger Siebeneicher

Paul Matthew Blaney

Ulrich Klar

Rolf Bohlmann

Bernd Buchmann

Lars Bärfacker

Ludwig Zorn

Detlev Sülzle

Judith Günther

Ingo Hartung

Kirstin Petersen

Sandra Berndt

Antonius Ter Laak

Antje Rottmann

Hana Cernecka

Heike Schäcke

Rienk Offringa

Rafael Carretero

Gernot Langer

Jeffrey Stuart Mowat

Petra Helfrich

Robin Michael Meier

Gabriele Leder

Nuria Aiguabella Font

Stephan Menz

Gianna Toschi

Katrin Nowak-reppel

Frank Sacher

Nicole Schmidt

Sabine Pilari

Andreas Von Deimling

Stefan Pusch

Reinhard Nubbemeyer

Ondozabal Hideki Miyatake

Thomas Fenzel

An aqueous pharmaceutical composition including compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[({2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl}amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclododecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.

Gadolinium chelate compounds for use in magnetic resonance imaging

The present invention relates to a new class of high relaxivity extracellular gadolinium chelate complexes, to methods of preparing said compounds, and to the use of said compounds as MRI contrast agents.

High relaxivity gadolinium chelate compounds for use in magnetic resonance imaging

A compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[({2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl}amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclo dodecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.

The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I), in which A, X, R, R, R, R, R, Rand Rare as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control. 

Substituted pyrrolopyridine-derivatives

The present invention relates to substituted dihydroimidazopyridinedione compounds of general formula (I) as described and defined herein, 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 a hyperproliferative, angiogenesis disorders, inflammatory diseases or diseases associated with inflammatory pain, as a sole agent or in combination with other active ingredients.

Substituted dihydroimidazopyridinediones as MKNK1 and MKNK2 inhibitors

The present invention relates to a new class of high relaxivity extracellular gadolinium chelate complexes, to methods of preparing said compounds, and to the use of said compounds as MRI contrast agents. 

The present invention relates to compounds of general formula (I): in which R, R, R, R, R, R, R, R, R, R, R, Rand X are as defined herein, 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. 

Fused imidazoles as mIDH1 inhibitors

A compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[{2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl} amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclo dodecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.

The present invention relates to benzimidazol-2-amines of general formula (I), in which R, R, R, R, R, R, R, R, R, R, Rand Rare as defined herein, 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.

Benzimidazol-2-amines as mIDH1 inhibitors

The present invention relates to benzimidazol-2-amines of general formula (I) in which R, R, R, R, R, Rand Rare as defined herein, 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. 

5-hydroxyalkylbenzimidazoles as mIDH1 inhibitors

The present invention relates to benzimidazol-2-amines of general formula (I), in which R, R, R, R, R, R, Rand Rare as defined herein, 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. 

N-Methylbenzimidazoles as mIDH1 inhibitors

The present invention relates to 2-Aryl- and 2-Arylalkyl-benzimidazoles of general formula (I): in which A, R, R, R, R, R, R, R, Rand Rare as defined herein, 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. 

2-aryl- and 2-arylalkyl-benzimidazoles as mIDH1 inhibitors

The present invention relates to benzimidazol-2-amines of general formula (I) in which R, R, R, R, R, R, R, R, R, R, Rand Rare as defined herein, 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. 

1-cyclohexyl-2-phenylaminobenzimidazoles as mIDH1 inhibitors for the treatment of tumors

The present invention relates to benzimidazol-2-amines of general formula (I), in which R, R, R, R, R, R, R, R, R, R, Rand Rare as defined herein, 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. 

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Berlin, Germany

Olaf Panknin