944342-88-5Relevant academic research and scientific papers
SUBSTITUTED PYRIMIDINE-5-CARBOXAMIDE AND 5-CARBOXYLIC ESTER KINASE INHIBITORS
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Page/Page column 16, (2009/05/29)
The present invention is directed to substituted pyrimidine-5-carboxamide and 5-carboxylic ester compounds of Formula (I): and forms thereof wherein R1, R2, R3, R4, R5, R6, R7 and L are as defined herein and their synthesis and use as kinase inhibitors for treating a chronic or acute protein kinase mediated disease.
A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: Design, synthesis, and biological activity
Hughes, Terry V.,Xu, Guozhang,Wetter, Steven K.,Connolly, Peter J.,Emanuel, Stuart L.,Karnachi, Prabha,Pollack, Scott R.,Pandey, Niranjan,Adams, Mary,Moreno-Mazza, Sandra,Middleton, Steven A.,Greenberger, Lee M.
scheme or table, p. 4896 - 4899 (2009/05/07)
A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine was synthesized and found to have potent dual EGFR/HER2 kinase inhibitory activity. The structure-based drug design of this molecule as well as the kinase and cellular inhibition of HER2 kinase dependent cell lines will be discussed.
Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases
Xu, Guozhang,Searle, Lily Lee,Hughes, Terry V.,Beck, Amanda K.,Connolly, Peter J.,Abad, Marta C.,Neeper, Michael P.,Struble, Geoffrey T.,Springer, Barry A.,Emanuel, Stuart L.,Gruninger, Robert H.,Pandey, Niranjan,Adams, Mary,Moreno-Mazza, Sandra,Fuentes-Pesquera, Angel R.,Middleton, Steven A.,Greenberger, Lee M.
scheme or table, p. 3495 - 3499 (2009/04/11)
We herein disclose a novel series of 4-aminopyrimidine-5-carbaldehyde oximes that are potent and selective inhibitors of both EGFR and ErbB-2 tyrosine kinases, with IC50 values in the nanomolar range. Structure-activity relationship (SAR) studies elucidated a critical role for the 4-amino and C-6 arylamino moieties. The X-ray co-crystal structure of EGFR with 37 was determined and validated our design rationale.
A chemoselective aniline-chloropyrimidine coupling in a competing electrophilic environment
Choudhury, Anusuya,Chen, Hongfeng,Nilsen, Christopher N.,Sorgi, Kirk L.
, p. 102 - 105 (2008/09/18)
A highly chemoselective substitution on 4-amino-6-chloropyrimidine ring system having a competing aldehyde functionality has been realized with anilines which produces 4, 6-diaminopyrimidine-5-carbaldehyde in high yield. The reaction may involve the inter
SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS
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Page/Page column 97, (2008/06/13)
The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.
