- Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists
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Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NFκB agonist activity was optimised in an iterative process from pIC50 7.5 (for 7), to pIC50 10.1 (for 38E1). An explanation for the SAR observed base
- Biggadike, Keith,Caivano, Matilde,Clackers, Margaret,Coe, Diane M.,Hardy, George W.,Humphreys, Davina,Jones, Haydn T.,House, David,Miles-Williams, Annette,Skone, Philip A.,Uings, Iain,Weller, Vicki,McLay, Iain M.,Macdonald, Simon J.F.
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scheme or table
p. 4846 - 4850
(2010/05/18)
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- NOVEL COMPOUNDS
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The present invention provides glucocorticoid receptor agonists of formula (I), a process for their preparation, pharmaceutical compositions comprising the compounds and the preparation of said compositions, intermediates and use of the compounds for the
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Page/Page column 61-62
(2008/06/13)
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- Cyclic phenyl-substituted indazols, a process for their production and their use as anti-inflammatory agents
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The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.
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Page/Page column 9-10
(2008/12/04)
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- Indazole and indole derivatives as anti-inflammatory agents
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The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.
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Page/Page column 14
(2008/12/05)
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- INDAZOLE AND INDOLE DERIVATIVES AS ANTI -INFLAMMATORY AGENTS
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The present invention relates to the compounds of formula (I), processes for their production and their use as anti-inflammatory agents.
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Page/Page column 25-26
(2008/12/05)
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- NOVEL BICYCLIC SULFONAMIDES FOR USE AS GLUCOCORTICOID RECEPTOR MODULATORS IN THE TREATMENT OF INFLAMMATORY DISEASES
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Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
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- INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS
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The present invention is directed to compounds of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents -C(R3)- or nitrogen; when X represents -C(R3)-, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents -C(R3)- and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents -C(R3)- and R2 represents hydroxy, methoxy, -CO2CH3 or -CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; and physiologically functional derivatives thereof, pharmaceutical compositions and formulations comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions and/or skin diseases, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.
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Page/Page column 37-38
(2008/06/13)
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