1222368-75-3Relevant articles and documents
INHIBITORS OF ENL/AF9 YEATS
-
Paragraph 00172-00173, (2021/06/26)
Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.
3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINES
-
Page/Page column 33-34, (2011/04/14)
The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. T
2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics
Zeng, Qingping,Bourbeau, Matthew P.,Wohlhieter, G. Erich,Yao, Guomin,Monenschein, Holger,Rider, James T.,Lee, Matthew R.,Zhang, Shiwen,Lofgren, Julie,Freeman, Daniel,Li, Chun,Tominey, Elizabeth,Huang, Xin,Hoffman, Douglas,Yamane, Harvey,Tasker, Andrew S.,Dominguez, Celia,Viswanadhan, Vellarkad N.,Hungate, Randall,Zhang, Xiaoling
scheme or table, p. 1652 - 1656 (2010/07/15)
A series of 2-aminothiadiazole of inhibitors of AKT1 is described. SAR relationships are discussed, along with selectivity for protein kinase A (PKA) and cyclin-dependent kinase 2 (CDK2). Moderate selectivity observed in several compounds for AKT1 versus PKA is rationalized by X-ray crystallographic analysis. Key compounds showed activity in cellular assays measuring phosphorylation of two AKT substrates, PRAS40 and FKHRL1. Compound 30 was advanced to a mouse liver PD assay, where it showed dose-dependent inhibition of AKT activity, as measured by the inhibition of phospho-PRAS40.