890129-80-3Relevant articles and documents
A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis
Bold, Guido,Schnell, Christian,Furet, Pascal,McSheehy, Paul,Brüggen, Josef,Mestan, Jürgen,Manley, Paul W.,Drückes, Peter,Burglin, Marion,Dürler, Ursula,Loretan, Jacqueline,Reuter, Robert,Wartmann, Markus,Theuer, Andreas,Bauer-Probst, Beatrice,Martiny-Baron, Georg,Allegrini, Peter,Goepfert, Arnaud,Wood, Jeanette,Littlewood-Evans, Amanda
, p. 132 - 146 (2016)
This paper describes the identification of 6-(pyrimidin-4-yloxy)-naphthalene-1-carboxamides as a new class of potent and selective human vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase inhibitors. In biochemical and cellular assays, the compounds exhibit single-digit nanomolar potency toward VEGFR2. Compounds of this series show good exposure in rodents when dosed orally. They potently inhibit VEGF-driven angiogenesis in a chamber model and rodent tumor models at daily doses of less than 3 mg/kg by targeting the tumor vasculature as demonstrated by ELISA for TIE-2 in lysates or by immunohistochemical analysis. This novel series of compounds shows a potential for the treatment of solid tumors and other diseases where angiogenesis plays an important role.
BICYCLIC AMIDES AS KINASE INHIBITORS
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Page/Page column 47, (2010/11/08)
The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
