Indolin-2-one p38α inhibitors II: Lead optimisation
Optimisation of a series of indolin-2-one p38α inhibitors was achieved via both blocking of a potential metabolic 'hot spot' and by increasing overall polarity of the lead series leading to non-cytotoxic compounds which showed improved oral bioavailabilities in the rat.
Eastwood, Paul,González, Jacob,Gómez, Elena,Caturla, Francisco,Balagué, Cristina,Orellana, Adelina,Domínguez, María
p. 5270 - 5273
(2011/10/09)
New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
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Page/Page column 90
(2009/10/21)
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