1013099-50-7Relevant articles and documents
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors
Lin, Songwen,Wang, Chunyang,Ji, Ming,Wu, Deyu,Lv, Yuanhao,Sheng, Li,Han, Fangbin,Dong, Yi,Zhang, Kehui,Yang, Yakun,Li, Yan,Chen, Xiaoguang,Xu, Heng
, p. 637 - 646 (2018)
A series of new thienopyrimidine derivatives has been discovered as potent PI3K inhibitors. The systematic SAR studies for these analogues are described. Among them, 8a and 9a exhibit nanomolar enzymatic potencies and sub-micromolar cellular anti-prolifer
Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR
Le, Phuong T.,Cheng, Hengmiao,Ninkovic, Sacha,Plewe, Michael,Huang, Xiaojun,Wang, Hai,Bagrodia, Shubha,Sun, Shaoxian,Knighton, Daniel R.,Lafleur Rogers, Caroline M.,Pannifer, Andrew,Greasley, Samantha,Dalvie, Deepak,Zhang, Eric
, p. 5098 - 5103 (2012)
Lead optimization efforts that employed structure base drug design and physicochemical property based optimization leading to the discovery of a novel series of 4-methylpyrido pyrimidinone (MPP) are discussed. Synthesis and profile of 1, a PI3Kα/mTOR dual inhibitor, is highlighted.
Protein Kinase Inhibitors
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, (2014/02/16)
The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
PYRIDO (2, 3-D) PYRIMIDIN0NE COMPOUNDS AND THEIR USE AS PI3 INHIBITORS
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Page/Page column 63, (2008/06/13)
The present invention is directed to novel 4-methylpyridopyhmidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3- Ka).