1013099-51-8Relevant articles and documents
Protein Kinase Inhibitors
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Paragraph 0180; 0181; 0182, (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.
Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series
Cheng, Hengmiao,Hoffman, Jacqui E.,Le, Phuong T.,Pairish, Mason,Kania, Robert,Farrell, William,Bagrodia, Shubha,Yuan, Jing,Sun, Shaoxian,Zhang, Eric,Xiang, Cathy,Dalvie, Deepak,Rahavendran, Sadayappan V.
supporting information, p. 2787 - 2792 (2013/07/04)
PI3K, AKT and mTOR, key kinases from a frequently dysregulated PI3K signaling pathway, have been extensively pursued to treat a variety of cancers in oncology. Clinical trials of PF-04691502, a highly potent and selective ATP competitive kinase inhibitor of class 1 PI3Ks and mTOR, from 4-methylpyridopyrimidinone series, led to the discovery of a metabolite with a terminal carboxylic acid, PF-06465603. This paper discusses structure-based drug design, SAR and antitumor activity of the MPP derivatives with a terminal alcohol, a carboxylic acid or a carboxyl amide.