58483-95-7Relevant articles and documents
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR
Yu, Tao,Li, Ning,Wu, Chengde,Guan, Amy,Li, Yi,Peng, Zhengang,He, Miao,Li, Jie,Gong, Zhen,Huang, Lei,Gao, Bo,Hao, Dongling,Sun, Jikui,Pan, Yan,Shen, Liang,Chan, Chichung,Lu, Xiulian,Yuan, Hongyu,Li, Yongguo,Li, Jian,Chen, Shuhui
, p. 256 - 261 (2018/03/21)
The identification and lead optimization of a series of pyridopyrimidinone derivatives are described as a novel class of efficacious dual PI3K/mTOR inhibitors, resulting in the discovery of 31. Compound 31 exhibited high enzyme activity against PI3K and mTOR, potent suppression of Akt and p70s6k phosphorylation in cell assays, and good pharmacokinetic profile. Furthermore, compound 31 demonstrated in vivo efficacy in a PC-3M tumor xenograft model.
QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
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Page/Page column 75, (2008/06/13)
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and c-erbB-2
Cockerill, Stuart,Stubberfield, Colin,Stables, Jeremy,Carter, Malcolm,Guntrip, Stephen,Smith, Kathryn,McKeown, Steve,Shaw, Robert,Topley, Peter,Thomsen, Lindy,Affleck, Karen,Jowett, Amanda,Hayes, David,Willson, Malcolm,Woollard, Patrick,Spalding, David
, p. 1401 - 1405 (2007/10/03)
Described herein is the design and synthesis of indazolylaminopyridopyrimidines and quinazolines as inhibitors of the class 1 tyrosine kinase receptor family. Data is presented for N4-(1-benzyl-1H-indazol-5-yl)-N6,N6- dime