1357159-12-6Relevant academic research and scientific papers
IMIDAZO[1,2-A]PYRAZINE MODULATORS OF THE ADENOSINE A2A RECEPTOR
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Page/Page column 78; 79; 80, (2019/01/17)
The present invention relates to the compound of formula (I) and salts, stereoisomers, tautomers, isotopologues,or N-oxides thereof. The present invention is further concerned with the use of such a compound or salt, stereoisomer, tautomer, isotopologues,or N-oxide thereof as medicament and a pharmaceutical composition comprising said compound.
Diverse heterocyclic scaffolds as allosteric inhibitors of AKT
Kettle, Jason G.,Brown, Simon,Crafter, Claire,Davies, Barry R.,Dudley, Phillippa,Fairley, Gary,Faulder, Paul,Fillery, Shaun,Greenwood, Hannah,Hawkins, Janet,James, Michael,Johnson, Keith,Lane, Clare D.,Pass, Martin,Pink, Jennifer H.,Plant, Helen,Cosulich, Sabina C.
supporting information; experimental part, p. 1261 - 1273 (2012/04/10)
Wide-ranging exploration of potential replacements for a quinoline-based inhibitor of activation of AKT kinase led to number of alternative, novel scaffolds with potentially improved potency and physicochemical properties. Examples showed predictable DMPK properties, and one such compound demonstrated pharmacodynamic knockdown of phosphorylation of AKT and downstream biomarkers in vivo and inhibition of tumor growth in a breast cancer xenograft model.
