918643-33-1Relevant academic research and scientific papers
PROCESSES AND INTERMEDIATES FOR PREPARING FUSED HETEROCYCLIC KINASE INHIBITORS
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Page/Page column 88; 102, (2009/04/25)
The invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, particularly at an industrial level The processes are aimed at ultimately forming compounds of the formula (A) where M is thieno[3,2,b]pyridinyl as shown, the group D is a ring or ring system, preferably pyridine, and the group Z, Ar, and G are as defined herein Such compounds can act to inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signalling, for example, the inhibition of VEGF receptor signalling and HGF receptor signalling.
Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases
Claridge, Stephen,Raeppel, Franck,Granger, Marie-Claude,Bernstein, Naomy,Saavedra, Oscar,Zhan, Lijie,Llewellyn, David,Wahhab, Amal,Deziel, Robert,Rahil, Jubrail,Beaulieu, Normand,Nguyen, Hannah,Dupont, Isabelle,Barsalou, Annie,Beaulieu, Carole,Chute, Ian,Gravel, Serge,Robert, Marie-France,Lefebvre, Sylvain,Dubay, Marja,Pascal, Roussen,Gillespie, Jeff,Jin, Zhiyun,Wang, James,Besterman, Jeffrey M.,MacLeod, A. Robert,Vaisburg, Arkadii
, p. 2793 - 2798 (2008/12/21)
A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC50 values in the low nanomolar range in vitro while the lead compound also showed in vivo activity against various human tumor xenograft models in mice. Further exploration of this class of compounds is underway.
