J
Joerg Berghausen
Researcher at Novartis
Publications - 15
Citations - 768
Joerg Berghausen is an academic researcher from Novartis. The author has contributed to research in topics: Solubility & Receptor tyrosine kinase. The author has an hindex of 8, co-authored 15 publications receiving 637 citations.
Papers
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Journal ArticleDOI
Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase
Vito Guagnano,Pascal Furet,Carsten Spanka,Vincent Bordas,Mickaël Le Douget,Christelle Stamm,Josef Brueggen,Michael Rugaard Jensen,Christian Schnell,Herbert A. Schmid,Markus Wartmann,Joerg Berghausen,Peter Drueckes,Alfred Zimmerlin,Dirksen E. Bussiere,Jeremy Murray,Diana Graus Porta +16 more
TL;DR: In vivo evaluation of compound 1h showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3 and support the potential therapeutic use of 1h as a new anticancer agent.
Journal ArticleDOI
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Philipp Holzer,Keiichi Masuya,Pascal Furet,Joerg Kallen,Therese Valat-Stachyra,Stephane Ferretti,Joerg Berghausen,Michele Bouisset-Leonard,Nicole Buschmann,Carole Pissot-Soldermann,Caroline Rynn,Stephan Ruetz,Stefan Stutz,Patrick Chène,Sébastien Jeay,François Gessier +15 more
TL;DR: An overview of the discovery of the potent and selective p53:MDM2 inhibitor NVP-CGM097 with an excellent in vivo profile is provided, which is currently in phase 1 clinical development.
Patent
Substituted isoquinolinones and quinazolinones
Joerg Berghausen,Nicole Buschmann,Pascal Furet,François Gessier,Joanna Lisztwan,Philipp Holzer,Edgar Jacoby,Joerg Kallen,Keiichi Masuya,Carole Pissot Soldermann,Ren Haixia,Stefan Stutz +11 more
TL;DR: In this article, substituted nitrogen containing bicyclic heterocycles of the formula (I): wherein Z is CH2 or N-R4 and X, R1, R2, R4, R6, R7 and n are as defined in the description.
Journal ArticleDOI
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Robin Alec Fairhurst,Thomas Knoepfel,Nicole Buschmann,Catherine Leblanc,Robert Mah,Milen Todorov,Pierre Nimsgern,Sebastien Ripoche,Michel Niklaus,Nicolas Warin,Van Huy Luu,Mario Madoerin,Jasmin Wirth,Diana Graus-Porta,Andreas Weiss,Michael Kiffe,Markus Wartmann,Jacqueline Kinyamu-Akunda,Dario Sterker,Christelle Stamm,Flavia Adler,Alexandra Buhles,Heiko Schadt,Philippe Couttet,Jutta Blank,Inga Galuba,Joerg Trappe,Johannes Voshol,Nils Ostermann,Chao Zou,Joerg Berghausen,Alberto Del Rio Espinola,Wolfgang Jahnke,Pascal Furet +33 more
TL;DR: Key challenges addressed during the optimisation are improving the FGFR4 potency, metabolic stability and solubility leading ultimately to the highly-selective first-in-class clinical candidate roblitinib.
Patent
Crystalline form of an inhibitor of mdm2/4 and p53 interaction
Joerg Berghausen,Ren Haixia +1 more
TL;DR: A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4]-methyl-[4- methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-p53, or variants thereof, respectively, is useful in the treatment of a disease or disorder associated with the interaction between p53 and MDM2 and/or MDM4.