- Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases
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A new series of quinoline ether inhibitors, which potently and selectively inhibit PDGFR tyrosine kinases, is described in this Letter. Compounds 23 and 33 are selective, low nanomolar inhibitors of PDGFRα and β, display good pharmacokinetics in rat and dog and are active in vivo at low doses when given orally twice daily. Further evaluation of these compounds is warranted.
- Plé, Patrick A.,Jung, Frédéric,Ashton, Sue,Hennequin, Laurent,Laine, Romuald,Lambert-Van Der Brempt, Christine,Morgentin, Rémy,Pasquet, Georges,Taylor, Sian
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p. 3050 - 3055
(2012/06/04)
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- QUINOLINE DERIVATIVES
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The invention concerns quinoline derivatives of Formula (I): or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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Page/Page column 105; 107; 121
(2008/06/13)
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