444731-17-3Relevant academic research and scientific papers
Pyrimidineamines as angiogenesis modulators
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Paragraph 0275; 0276, (2015/11/16)
Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2- pyrimidinyl]amino]-2-methyl-benzenesulfonamide (pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor
Harris, Philip A.,Boloor, Amogh,Cheung, Mui,Kumar, Rakesh,Crosby, Renae M.,Davis-Ward, Ronda G.,Epperly, Andrea H.,Hinkle, Kevin W.,Hunter III, Robert N.,Johnson, Jennifer H.,Knick, Victoria B.,Laudeman, Christopher P.,Luttrell, Deirdre K.,Mook, Robert A.,Nolte, Robert T.,Rudolph, Sharon K.,Szewczyk, Jerzy R.,Truesdale, Anne T.,Veal, James M.,Wang, Liping,Stafford, Jeffrey A.
experimental part, p. 4632 - 4640 (2009/06/18)
Inhibition of the vascular endothelial growth factor (VEGF) signaling pathway has emerged as one of the most promising new approaches for cancer therapy. We describe herein the key steps starting from an initial screening hit leading to the discovery of pazopanib, N4-(2,3-dimethyl-2H-indazol- 6-yl)-N4-methyl-N2-(4-methyl-3-sulfonamidophenyl)-2,4- pyrimidinediamine, a potent pan-VEGF receptor (VEGFR) inhibitor under clinical development for renal-cell cancer and other solid tumors.
