1448869-67-7Relevant articles and documents
IMIDAXOPYROLONE COMPOUND AND APPLICATION THEREOF
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, (2021/01/28)
Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof. (I-1), (I-2)
In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor
Vaupel, Andrea,Holzer, Philipp,Ferretti, Stephane,Guagnano, Vito,Kallen, Joerg,Mah, Robert,Masuya, Keiichi,Ruetz, Stephan,Rynn, Caroline,Schlapbach, Achim,Stachyra, Thérèse,Stutz, Stefan,Todorov, Milen,Jeay, Sébastien,Furet, Pascal
, p. 3404 - 3408 (2018/09/17)
Small molecule inhibitors of the p53-MDM2 protein complex are under intense investigation in clinical trials as anti-cancer agents, including our first generation inhibitor NVP-CGM097. We recently described the rational design of a novel pyrazolopyrrolidinone core as a new lead structure and now we report on the synthesis and optimization of this to provide a highly potent lead compound. This new compound displayed excellent oral efficacy in our preclinical mechanistic in vivo model and marked a significant milestone towards the identification of our second generation clinical candidate NVP-HDM201.
SUBSTITUTED PURINONE COMPOUNDS
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, (2014/08/07)
The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.