1143535-08-3Relevant academic research and scientific papers
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H- pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases
Addie, Matt,Ballard, Peter,Buttar, David,Crafter, Claire,Currie, Gordon,Davies, Barry R.,Debreczeni, Judit,Dry, Hannah,Dudley, Philippa,Greenwood, Ryan,Johnson, Paul D.,Kettle, Jason G.,Lane, Clare,Lamont, Gillian,Leach, Andrew,Luke, Richard W. A.,Morris, Jeff,Ogilvie, Donald,Page, Ken,Pass, Martin,Pearson, Stuart,Ruston, Linette
, p. 2059 - 2073 (2013/05/08)
Wide-ranging exploration of analogues of an ATP-competitive pyrrolopyrimidine inhibitor of Akt led to the discovery of clinical candidate AZD5363, which showed increased potency, reduced hERG affinity, and higher selectivity against the closely related AGC kinase ROCK. This compound demonstrated good preclinical drug metabolism and pharmacokinetics (DMPK) properties and, after oral dosing, showed pharmacodynamic knockdown of phosphorylation of Akt and downstream biomarkers in vivo, and inhibition of tumor growth in a breast cancer xenograft model.
PYRROLO [2,3-D] PYRIMIDIN DERIVATIVES AS PROTEIN KINASE B INHIBITORS
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Page/Page column 137, (2009/05/30)
The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I)
