The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. The
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Page/Page column 14
(2008/06/13)
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRα and β
A series of branched and unbranched anilinohexafluoroisopropanols related to the known sulfonamide T0901317 were prepared and evaluated as activators/modulators of both LXRα and LXRβ. A structure-activity relationship was established and compounds with high potency on both the receptors were identified. Many compounds showed a tendency toward selectivity for LXRβ versus LXRα. Several analogues were evaluated for effects on plasma lipoprotein levels in mice. A few of these significantly raised HDL-cholesterol levels in plasma but showed markedly different effects on liver triglyceride content, suggesting that this series may yield candidates with improved efficacy/safety profiles compared to existing molecules.
Panday, Narendra,Benz, Joerg,Blum-Kaelin, Denise,Bourgeaux, Vanessa,Dehmlow, Henrietta,Hartman, Peter,Kuhn, Bernd,Ratni, Hassen,Warot, Xavier,Wright, Matthew B.
p. 5231 - 5237
(2007/10/03)
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