1246034-80-9Relevant academic research and scientific papers
Identification of a novel and selective series of Itk inhibitors via a template-hopping strategy
Alder, Catherine M.,Ambler, Martin,Campbell, Amanda J.,Champigny, Aurelie C.,Deakin, Angela M.,Harling, John D.,Harris, Carol A.,Longstaff, Tim,Lynn, Sean,Maxwell, Aoife C.,Mooney, Chris J.,Scullion, Callum,Singh, Onkar M. P.,Smith, Ian E. D.,Somers, Donald O.,Tame, Christopher J.,Wayne, Gareth,Wilson, Caroline,Woolven, James M.
, p. 948 - 952 (2013)
Inhibition of Itk potentially constitutes a novel, nonsteroidal treatment for asthma and other T-cell mediated diseases. In-house kinase cross-screening resulted in the identification of an aminopyrazole-based series of Itk inhibitors. Initial work on this series highlighted selectivity issues with several other kinases, particularly AurA and AurB. A template-hopping strategy was used to identify a series of aminobenzothiazole Itk inhibitors, which utilized an inherently more selective hinge binding motif. Crystallography and modeling were used to rationalize the observed selectivity. Initial exploration of the SAR around this series identified potent Itk inhibitors in both enzyme and cellular assays.
PYRIMIDINE DERIVATIVES USED AS ITK INHIBITORS
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Page/Page column 110, (2010/10/03)
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular ltk activity.
