847802-85-1Relevant academic research and scientific papers
Aniline pyrimidines, its preparation method and medical use (by machine translation)
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Paragraph 0705; 0706; 0707, (2018/03/01)
The invention relates to: an aniline pyrimidine compound represented as the formula (I), a medicinal salt thereof, a prodrug thereof, and a hydrate or solvate thereof and also relates to: the preparation method of the compound, a medicine composition comp
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: Design, synthesis, and evaluation
Harmange, Jean-Christophe,Weiss, Matthew M.,Germain, Julie,Polverino, Anthony J.,Borg, George,Bready, James,Chen, Danlin,Choquette, Deborah,Coxon, Angela,DeMelfi, Tom,DiPietro, Lucian,Doerr, Nicholas,Estrada, Juan,Flynn, Julie,Graceffa, Russell F.,Harriman, Shawn P.,Kaufman, Stephen,La, Daniel S.,Long, Alexander,Martin, Matthew W.,Neervannan, Sesha,Patel, Vinod F.,Potashman, Michele,Regal, Kelly,Roveto, Phillip M.,Schrag, Michael L.,Starnes, Charlie,Tasker, Andrew,Teffera, Yohannes,Wang, Ling,White, Ryan D.,Whittington, Douglas A.,Zanon, Roger
, p. 1649 - 1667 (2008/09/20)
A series of naphthyl-based compounds were synthesized as potential inhibitors of vascular endothelial growth factor (VEGF) receptors. Investigations of structure-activity relationships led to the identification of a series of naphthamides that are potent inhibitors of the VEGF receptor tyrosine kinase family. Numerous analogues demonstrated low nanomolar inhibition of VEGF-dependent human umbilical vein endothelial cell (HUVEC) proliferation, and of these several compounds possessed favorable pharmacokinetic (PK) profiles. In particular, compound 48 demonstrated significant antitumor efficacy against established HT29 human colon adenocarcinoma xenografts implanted in athymic mice. A full account of the preparation, structure-activity relationships, pharmacokinetic properties, and pharmacology of analogues within this series is presented.
NAPHTHALENE CARBOXAMIDES AND THEIR DERIVATIVES USEFUL AS NEW ANTI-ANGIOGENIC AGENTS
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Page/Page column 45, (2010/02/11)
The invention relates to compounds represented by Formula (I) and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of R1a-d , R2a-b , R3, and X1 are defined herein, The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula(l).
