501693-17-0Relevant academic research and scientific papers
4-AMINO-6-ARYL[2,3-D]PYRIMIDINES FOR THE INHIBITION OF EGFR TYROSINE KINASE
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Page/Page column 73, (2015/01/16)
This invention relates to certain new pyrrolo-, thieno-, and furo-[2,3- d]pyrimidine compounds, such as of general formula (I) These compounds are epidermal growth factor receptor tyrosine kinase inhibitors and therefore offer potential in the treatment of cancer.
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors
Miyazaki, Yasushi,Matsunaga, Shinichiro,Tang, Jun,Maeda, Yutaka,Nakano, Masato,Philippe, Rocher J.,Shibahara, Megumi,Liu, Wei,Sato, Hideyuki,Wang, Liping,Nolte, Robert T.
, p. 2203 - 2207 (2007/10/03)
A novel class of furo[2,3-d]pyrimidines has been discovered as potent dual inhibitors of Tie-2 and VEGFR2 receptor tyrosine kinases (TK) and a diarylurea moiety at 5-position shows remarkably enhanced activity against both enzymes. One of the most active compounds, 4-amino-3-(4-((2-fluoro-5-(trifluoromethyl) phenyl)amino-carbonylamino)phenyl)-2-(4-methoxyphenyl)furo[2,3-d]pyrimidine (7k) is 3 nM on both TK receptors and the activity is rationalized based on the X-ray crystal structure.
