- NEW ANTIBACTERIAL COMPOUNDS
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The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.
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Page/Page column 84; 85
(2018/01/19)
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- New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors
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A series of 5,7-disubstituted quinazolines, bearing 4-heteroaryl substituents such as 2-pyridinylamine or 2-pyrazinylamine, has been synthetised and evaluated as c-Src kinase inhibitors. Highly potent inhibition, high selectivity and physical properties suitable for oral dosing were achieved within this series: 23d and 42 were identified as sub-0.1 μM inhibitors in a c-Src-driven cell proliferation assay and displayed adequate rat pharmacokinetics after oral administration.
- Barlaam, Bernard,Fennell, Mike,Germain, Herve,Green, Tim,Hennequin, Laurent,Morgentin, Remy,Olivier, Annie,Ple, Patrick,Vautier, Michel,Costello, Gerard
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p. 5446 - 5449
(2007/10/03)
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- PYRAZINYL 3-CYANOQUINOLINE DERIVATIVES FOR USE IN THE TREATMENT OF TUMOURS
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The invention concerns quinoline derivatives of Formula I Formula (I) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)(R3) group wherein each R2 or R3 group is hydrogen or (1-8C)alkyl, m is 1, 2 or 3, each R1 group has any of the meanings defined in the description, Ra is hydrogen or halogeno, Rc is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy, and Rd is (1-6C)alkoxy, or Rc and Rd together form a (1-3C)alkylenedioxy group, or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
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- PYRAZINIL QUINAZOLINE DERIVATIVES FOR USE IN THE TREATMENT OF TUMOURS
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The invention concerns quinazoline derivatives of Formula (I) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)(R3) group wherein each R2 or R3group is hydrogen or (1-8C)alkyl, m is 1, 2 or 3,
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