960249-70-1Relevant academic research and scientific papers
Novel selective glucocorticoid receptor agonists (SEGRAs) with a covalent warhead for long-lasting inhibition
Ryabtsova, Oksana,Joossens, Jurgen,Van Der Veken, Pieter,Vanden Berghe, Wim,Augustyns, Koen,De Winter, Hans
, p. 5032 - 5038 (2016/10/05)
The synthesis and in vitro properties of six analogues of the selective glucocorticoid receptor (GR) agonist GSK866, bearing a warhead for covalent linkage to the glucocorticoid receptor, is described.
INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 50-51, (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 48-49, (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 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 50-51, (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
Efficient synthesis of an α-trifluoromethyl-α-tosyloxymethyl epoxide enabling stepwise double functionalisation to afford CF3-substituted tertiary alcohols
Keeling, Steven P.,Campbell, Ian B.,Coe, Diane M.,Cooper, Tony W.J.,Hardy, George W.,Jack, Torquil I.,Jones, Haydn T.,Needham, Deborah,Shipley, Tracy J.,Skone, Philip A.,Sutton, Peter W.,Weingarten, Gordon A.,Macdonald, Simon J.F.
, p. 5101 - 5104 (2008/12/22)
The efficient synthesis of an α-trifluoromethyl-α-tosyloxymethyl epoxide is reported. This highly versatile building block may be reacted sequentially with two different nucleophiles to furnish α-trifluoromethyl tertiary alcohols. Furthermore, the two enantiomers of this key intermediate have been separated using chiral HPLC and the stereochemistry shown to be conserved during subsequent chemical manipulations. Finally, an enzyme-driven desymmetrisation approach has been successfully employed to confer chirality on an intermediate in the sequence.
NOVEL COMPOUNDS
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Page/Page column 59-60, (2008/06/13)
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
NOVEL COMPOUNDS
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Page/Page column 56-57, (2010/11/29)
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 of
PYRAZOLE DERIVATIVES AS NON-STEROIDAL GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 53-54, (2008/12/06)
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 of a medicament for therapeutic treatment, particularly for the treatment of inflammation.
NOVEL COMPOUNDS
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Page/Page column 68-69, (2008/06/13)
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 of a medicament for therapeutic treatment, particularly for the treatment of inflammation, allergy and/or auto-immune conditions.
