Andreas Janzer

TL;DR: The discovery and characterization of BAY 2402234 is described - a novel, potent, selective and orally bioavailable DHODH inhibitor that shows monotherapy efficacy and differentiation induction across multiple AML subtypes.

TL;DR: In this article, the triazolone compounds compounds of general formula (I): in which R 1, R 2, R 3, R 4 and R 5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compound, 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 disorders, as a sole agent or in combination with other active ingredients.

TL;DR: The discovery of 4-triazolosalicylamides as inhibitors of DHODH and their structure activity relationship (SAR) is disclosed, which leads to compounds with sub-nanomolar potency in cellular assays and increased metabolic stability enabling the proof of concept in vivo xenograft experiments.

TL;DR: In this article, the authors described 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'- biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid.