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Featured researches published by Dirk Kosemund.


ChemMedChem | 2017

Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer

Ulrich Lücking; Arne Scholz; Philip Lienau; Gerhard Siemeister; Dirk Kosemund; Rolf Bohlmann; Hans Briem; Ildiko Terebesi; Kirstin Meyer; Katja Prelle; Karsten Dr Denner; Ulf Bömer; Martina Schäfer; Knut Eis; Ray Valencia; Stuart Ince; Franz von Nussbaum; Dominik Mumberg; Karl Ziegelbauer; Bert Klebl; Axel Choidas; Peter Nussbaumer; Matthias Baumann; Carsten Schultz-Fademrecht; Gerd Rühter; Jan Eickhoff; Michael Brands

Selective inhibition of exclusively transcription‐regulating PTEFb/CDK9 is a promising new approach in cancer therapy. Starting from lead compound BAY‐958, lead optimization efforts strictly focusing on kinase selectivity, physicochemical and DMPK properties finally led to the identification of the orally available clinical candidate atuveciclib (BAYu20051143572). Structurally characterized by an unusual benzyl sulfoximine group, BAYu20051143572 exhibited the best overall profile inu2005vitro and inu2005vivo, including high efficacy and good tolerability in xenograft models in mice and rats. BAYu20051143572 is the first potent and highly selective PTEFb/CDK9 inhibitor to enter clinical trials for the treatment of cancer.


Archive | 2011

6-SUBSTITUTED IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS

Marcus Koppitz; Ulrich Klar; Rolf Jautelat; Dirk Kosemund; Rolf Bohlmann; Benjamin Bader; Philip Lienau; Gerhard Siemeister


Archive | 2015

Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group

Ulrich Lücking; Dirk Kosemund; Arne Scholz; Philip Lienau; Gerhard Siemeister; Ulf Bömer; Rolf Bohlmann


Archive | 2012

DISUBSTITUTED 5-FLUORO-PYRIMIDINES

Ulrich Lücking; Dirk Kosemund; Arne Scholz; Philip Lienau; Gerhard Siemeister; Ulf Bömer; Rolf Bohlmann


Archive | 2012

4-ARYL-N-PHENYL-1,3,5-TRIAZIN-2-AMINES CONTAINING A SULFOXIMINE GROUP

Ulrich Lücking; Rolf Bohlmann; Arne Scholz; Gerhard Siemeister; Mark Jean Gnoth; Ulf Bömer; Dirk Kosemund; Philip Lienau; Gerd Rühter; Carsten Schultz-Fademrecht


Archive | 2011

6,7-dihydro-5h-benzo[7]annulene derivatives, process for preparation thereof, pharmaceutical preparations comprising them, and the use thereof for production of medicaments

Tim Wintermantel; Carsten Möller; Ulrich Bothe; Reinhard Nubbemeyer; Ludwig Zorn; Dirk Kosemund; Laak Antonius Ter; Rolf Bohlmann; Lars Wortmann; Donald Bierer


Archive | 2011

IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT HYPERPROLIFERATIVE DISORDERS

Marcus Koppitz; Ulrich Klar; Rolf Jautelat; Dirk Kosemund; Rolf Bohlmann; Benjamin Bader; Philip Lienau; Gerhard Siemeister


Archive | 2016

2,4-disubstituted 5-fluoro-pyrimidines as selective cdk9 inhibtors

Ulrich Lücking; Dirk Kosemund; Arne Scholz; Philip Lienau; Gerhard Siemeister; Ulf Bömer; Rolf Bohlmann


Archive | 2015

6-thio-substituted imidazo[1,2-a]pyrazines as Mps-1 inhibitors

Marcus Koppitz; Ulrich Klar; Rolf Jautelat; Dirk Kosemund; Rolf Bohlmann; Benjamin Bader; Philip Lienau; Gerhard Siemeister


Archive | 2012

SUBSTITUTED BENZIMIDAZOLES AS MPS-1 KINASE INHIBITORS

Ulrich Klar; Marcus Koppitz; Duy Nguyen; Dirk Kosemund; Roland Neuhaus; Gerhard Siemeister

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