913003-15-3Relevant academic research and scientific papers
Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity
Diallo, Hawa,Angell, Davina C.,Barnett, Heather A.,Biggadike, Keith,Coe, Diane M.,Cooper, Tony W.J.,Craven, Andy,Gray, James R.,House, David,Jack, Torquil I.,Keeling, Steve P.,MacDonald, Simon J.F.,McLay, Iain M.,Oliver, Samuel,Taylor, Simon J.,Uings, Iain J.,Wellaway, Natalie
scheme or table, p. 1126 - 1133 (2011/04/16)
A novel series of indazole non-steroidal glucocorticoid receptor agonist has been discovered. This series features a sulfonamide central core and meta amides which interact with the extended ligand binding domain. This series has produced some of the most potent and least lipophilic agonists of which we are aware such as 20a (NFκB pIC50 8.3 (100%), c log P 1.9). Certain analogues in this series also display evidence for modulated pharmacology.
INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 51-52, (2009/05/28)
The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture o
INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 49, (2009/05/28)
The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture o
INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 53, (2009/05/28)
The present invention provides compounds of formula (I), a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture o
INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 51-52, (2009/05/28)
The present invention provides compounds of formula (I), a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture o
N- (2 { [1-PHENYL-1H-INDAZ0L-4-YL] AMINO} PROPYL) -SULFONAMIDE DERIVATIVES AS NON-STEROIDAL GLUCOCORTICOID RECEPTOR LIGANDS FOR THE TREATMENT OF INFLAMMATIONS
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Page/Page column 56, (2009/07/17)
The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture o
NOVEL COMPOUNDS
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Page/Page column 48-49, (2008/06/13)
The present invention provides compounds 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 manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation, allergy and/or skin disease.
NOVEL COMPOUNDS
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Page/Page column 49, (2008/06/13)
The present invention provides compounds of formula (I): pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament, particularly for the treatment of inflammation and/or allergic conditions.
INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 49-50, (2008/06/13)
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.
