136117-69-6Relevant articles and documents
Discovery of (S)-1-(1-(Imidazo[1,2- a ]pyridin-6-yl)ethyl)-6-(1-methyl-1 H -pyrazol-4-yl)-1 H -[1,2,3]triazolo[4,5- b ]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal-Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer
Jia, Hong,Dai, Guangxiu,Weng, Jianyang,Zhang, Zhulin,Wang, Qing,Zhou, Feng,Jiao, Longxian,Cui, Yumin,Ren, Yongxin,Fan, Shiming,Zhou, Jinghong,Qing, Weiguo,Gu, Yi,Wang, Jian,Sai, Yang,Su, Weiguo
supporting information, p. 7577 - 7589 (2014/12/11)
HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
Fragment based discovery of a novel and selective PI3 kinase inhibitor
Hughes, Samantha J.,Millan, David S.,Kilty, Iain C.,Lewthwaite, Russell A.,Mathias, John P.,Reilly, Mark A.O.,Pannifer, Andrew,Phelan, Anne,Stühmeier, Frank,Baldock, Darren A.,Brown, David G.
scheme or table, p. 6586 - 6590 (2011/12/04)
We report the use of fragment screening and fragment based drug design to develop a PI3c kinase fragment hit into a lead. Initial fragment hits were discovered by high concentration biochemical screening, followed by a round of virtual screening to identify additional ligand efficient fragments. These were developed into potent and ligand efficient lead compounds using structure guided fragment growing and merging strategies. This led to a potent, selective, and cell permeable PI3c kinase inhibitor with good metabolic stability that was useful as a preclinical tool compound.
SYNTHESIS OF PYRAZOLES
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Page/Page column 39; 43, (2009/08/16)
The present invention provides methods of making HCl salts, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other
