875340-08-2Relevant academic research and scientific papers
BIOMARKER-BASED THERAPEUTIC COMPOSITION
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, (2021/05/13)
The present invention provides an anticancer agent for treating a patient who is resistant to a protein kinase inhibitor, the anticancer agent comprising, as an active ingredient, a thienopyridine derivative compound or a pharmaceutically acceptable salt thereof. Here, the patient may be a patient carrying active RON. In addition, the patient may be a patient carrying normal KRAS. In addition, the anticancer agent may be applied to a patient who is resistant to an EGFR inhibitor. In particular, the anticancer agent may be usefully used to treat a patient who is resistant to the therapeutic agent cetuximab.
Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups
Gaudette, Frederic,Raeppel, Stephane,Nguyen, Hannah,Beaulieu, Normand,Beaulieu, Carole,Dupont, Isabelle,Macleod, A. Robert,Besterman, Jeffrey M.,Vaisburg, Arkadii
scheme or table, p. 848 - 852 (2010/09/08)
A novel series of malonamide-type dual VEGFR2/c-Met inhibitors in which one of the amide bonds was replaced by an amide isostere-a trifluoroethylamine unit, was designed, synthesized, and evaluated for their enzymatic and cellular inhibition of VEGFR2 and c-Met enzymes. Optimization of these molecular entities resulted in identification of potent and selective inhibitors of VEGFR2 enzyme.
N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: A novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors
Raeppel, Stephane,Claridge, Stephen,Saavedra, Oscar,Gaudette, Frederic,Zhan, Lijie,Mannion, Michael,Zhou, Nancy,Raeppel, Franck,Granger, Marie-Claude,Isakovic, Ljubomir,Deziel, Robert,Nguyen, Hannah,Beaulieu, Normand,Beaulieu, Carole,Dupont, Isabelle,Robert, Marie-France,Lefebvre, Sylvain,Dubay, Marja,Rahil, Jubrail,Wang, James,Ste-Croix, Helene,Robert Macleod,Besterman, Jeffrey,Vaisburg, Arkadii
scheme or table, p. 1323 - 1328 (2009/10/02)
A series of N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting c-Met and VEGFR2 tyrosine kinases was designed and synthesized. The compounds were potent against these two enzymes with IC50/
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.
