1206687-12-8Relevant articles and documents
Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome
Maletic, Milana,Leeman, Aaron,Szymonifka, Michael,Mundt, Steven S.,Zokian, Hratch J.,Shah, Kashmira,Dragovic, Jasminka,Lyons, Kathy,Thieringer, Rolf,Vosatka, Anne H.,Balkovec, James,Waddell, Sherman T.
, p. 2568 - 2572 (2011)
Following the discovery of a metabolic 'soft-spot' on a bicyclo[2.2.2]octyltriazole lead, an extensive effort was undertaken to block the oxidative metabolism and improve PK of this potent HSD1 lead. In this communication, SAR survey focusing on various alkyl chain replacements will be detailed. This effort culminated in the discovery of a potent ethyl sulfone inhibitor with an improved PK profile across species and improved physical properties.
SEH AND 11β-HSD1 DUAL INHIBITORS
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Page/Page column 22; 23, (2010/04/03)
The invention is directed to bicycle[2.2.2]oct-1-yl compounds, pharmaceutical compositions containing them and their use in the treatment of a variety of conditions mediated by the sEH enzyme and/or the 11β-HSD1 enzyme.