1252464-84-8Relevant articles and documents
Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17 β-hydroxysteroid dehydrogenase type 2 inhibitors
Gargano, Emanuele M.,Perspicace, Enrico,Hanke, Nina,Carotti, Angelo,Marchais-Oberwinkler, Sandrine,Hartmann, Rolf W.
, p. 203 - 219 (2015/01/09)
17β-HSD2 is a promising new target for the treatment of osteoporosis. In this paper, a rational strategy to overcome the metabolic liability in the 2,5-thiophene amide class of 17β-HSD2 inhibitors is described, and the biological activity of the new inhibitors. Applying different strategies, as lowering the cLogP or modifying the structures of the molecules, compounds 27, 31 and 35 with strongly improved metabolic stability were obtained. For understanding biotransformation in the 2,5-thiophene amide class the main metabolic pathways of three properly selected compounds were elucidated.
BIARYL DERIVATIVES AS SELECTIVE 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 2 INHIBITORS
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Page/Page column 59, (2012/09/21)
The invention relates to selective, non-steroidal 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) inhibitors of formula (I), their production and use, notably for the treatment and prophylaxis of sex steroid deficient diseases like osteoporosis in men and women.