95901-05-6Relevant articles and documents
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064
Akwabi-Ameyaw, Adwoa,Bass, Jonathan Y.,Caldwell, Richard D.,Caravella, Justin A.,Chen, Lihong,Creech, Katrina L.,Deaton, David N.,Jones, Stacey A.,Kaldor, Istvan,Liu, Yaping,Madauss, Kevin P.,Marr, Harry B.,McFadyen, Robert B.,Miller, Aaron B.,III, Frank Navas,Parks, Derek J.,Spearing, Paul K.,Todd, Dan,Williams, Shawn P.,Wisely, G. Bruce
experimental part, p. 4339 - 4343 (2009/04/06)
Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a. Analog 1b also reduced the severit
NAPTHTHALENE DERIVATIVES WHICH INHIBIT THE CYTOKINE OR BIOLOGICAL ACTIVITY OF MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)
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Page 83-84, (2010/02/04)
Where Y, R1-R8 and R101-R108 are as defined in the specification. Compounds of formula (II) and methods of inhibiting the cytokine or biological activity of Macrophage Migrating Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as part of a combination therapy.
Piperidine-renin inhibitors compounds with improved physicochemical properties
Gueller, Rolf,Binggeli, Alfred,Breu, Volker,Bur, Daniel,Fischli, Walter,Hirth, Georges,Jenny, Christian,Kansy, Manfred,Montavon, Francois,Mueller, Marcel,Oefner, Christian,Stadler, Heinz,Vieira, Eric,Wilhelm, Maurice,Wostl, Wolfgang,Maerki, Hans Peter
, p. 1403 - 1408 (2007/10/03)
Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D((pH 7.4)) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets.