Lim, Jongwon; Kelley, Elizabeth Helen; Methot, Joey L.; Zhou, Hua; Petrocchi, Alessia; Mansoor, Umar Faruk; Fischer, Christian; O'Boyle, Brendan M.; Guerin, David Joseph; Bienstock, Corey E.; Boyce, Christopher W.; Daniels, Matthew H.; Falcone, Danielle; Ferguson, Ronald D., II; Fevrier, Salem; Huang, Xianhai; Lipford, Kathryn Ann; Sloman, David L.; Wilson, Kevin; Zhou, Wei; Witter, David; Maletic, Milana M.; Siliphaivanh, Phieng
Disclosed are the ERK inhibitors of formula I (wherein X is S or O; R1 is H, halo, CN, (un)substituted heteroaryl, etc.; R2 is H, (C1-6)alkyl, (un)substituted aryl, etc.; R3 is H, (C1-6)alkyl, (un)substituted aryl, etc.; R4 is H, halo, (C1-C6)alkyl, OH and NH2) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compds. of formula I an of synthesizing compds. of formula I. Example compd. II was prepd. from intermediate III and 1-(tert-butoxycarbonyl)piperidine-3-carboxylic acid in the presence of diphenylphosphoryl azide and TEA. In an active mouse ERK2 activity assay, II had an IC50 of 3.13 nM.
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