1127327-80-3Relevant articles and documents
Identification of a novel series of potent RON receptor tyrosine kinase inhibitors
Raeppel, Stéphane,Gaudette, Frédéric,Mannion, Michael,Claridge, Stephen,Saavedra, Oscar,Isakovic, Ljubomir,Déziel, Robert,Beaulieu, Normand,Beaulieu, Carole,Dupont, Isabelle,Nguyen, Hannah,Wang, James,Macleod, A. Robert,Maroun, Christiane,Besterman, Jeffrey M.,Vaisburg, Arkadii
scheme or table, p. 2745 - 2749 (2010/07/15)
A novel series of N-(3-fluoro-4-(2-substituted-thieno[3,2-b]pyridin-7-yloxy)phenyl)-1-phenyl-5-(trifluoromethyl)-1H-pyrazole-4-carboxamides targeting RON receptor tyrosine kinase was designed and synthesized. SAR study of the series allowed us to identify compounds possessing either inhibitory activity of RON kinase enzyme in the low nanomolar range with low residual activity against the closely related c-Met or potent dual inhibitory activity against RON and c-Met, - with no significant activity against VEGFR2 in both cases.
INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY
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Page/Page column 134, (2009/04/25)
The invention relates to compounds of Formula (I) and their use for inhibiting protein tyrosine kinase activity In Formula (I), the group M is thieno[3,2,b]pyridinyl as shown, and the group D is a ring or ring system, and the groups Z, Ar, and G are as defined herein The invention relates particularly to compounds that 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 The invention also provides compositions and methods for treating cell proliferative diseases and conditions, such as cancer, and for treating ophthalmic diseases, including age-related macular degeneration (AMD) and diabetic retinopathy (DR)