960249-71-2Relevant academic research and scientific papers
Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists
Barnett, Heather A.,Coe, Diane M.,Cooper, Tony W.J.,Jack, Torquil I.,Jones, Haydn T.,Macdonald, Simon J.F.,McLay, Iain M.,Rayner, Natalie,Sasse, Rosemary Z.,Shipley, Tracy J.,Skone, Phil A.,Somers, Graham I.,Taylor, Simon,Uings, Iain J.,Woolven, James M.,Weingarten, Gordon G.
scheme or table, p. 158 - 162 (2009/05/30)
Aryl aminopyrazole amides capped with N-alkylbenzamides 13-16 are selective glucocorticoid receptor agonists. 2,6-Disubstituted benzamides have prednisolone-like potency or better in vitro. Good oral exposure was demonstrated in the rat, with compounds wi
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.
PYRAZOLE DERIVATIVES AS NON-STEROIDAL GLUCOCORTICOID RECEPTOR LIGANDS
-
Page/Page column 54-55, (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
-
Page/Page column 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
NOVEL COMPOUNDS
-
Page/Page column 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.
