65784-33-0Relevant articles and documents
DIHYDROPYRIMIDIN-2-ONE COMPOUNDS AND MEDICAL USE THEREOF
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Paragraph 0679-0681, (2016/08/07)
A compound of Formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is defined as in the specification.
Discovery of diarylhydantoins as new selective androgen receptor modulators
Nique, Francois,Hebbe, Severine,Peixoto, Christophe,Annoot, Denis,Lefrancois, Jean-Michel,Duval, Eric,Michoux, Laurence,Triballeau, Nicolas,Lemoullec, Jean-Michel,Mollat, Patrick,Minet, Dominique,Clement-Lacroix, Philippe,Robin-Jagerschmidt, Catherine,Fleury, Damien,Guedin, Denis,Deprez, Pierre,Thauvin, Maxime,Prange, Thierry
, p. 8225 - 8235,11 (2020/09/15)
A novel selective androgen receptor modulator scaffold has been discovered through structural modifications of hydantoin antiandrogens. Several 4-(4-hydroxyphenyl)-N-arylhydantoins displayed partial agonism with nanomolar in vitro potency in transactivation experiments using androgen receptor (AR) transfected cells. In a standard castrated male rat model, several compounds showed good anabolic activity on levator ani muscle, dissociated from the androgenic activity on ventral prostate, after oral dosing at 30 mg/kg. (+)-4-[3,4-Dimethyl-2,5-dioxo-4-(4-hydroxyphenyl)imidazolidin-1-yl] -2-(trifluoromethyl)benzonitrile ((+)-11b) displayed anabolic potency with a strong dissociation between levator ani muscle and ventral prostate (A 50 = 0.5 mg/kg vs 70 mg/kg). The binding modes of two compounds, including (+)-11b, within the AR ligand-binding domain have been studied by cocrystallization experiments using a coactivator-like peptide. Both compounds bound to the same site, and the overall structures of the AR were very similar.
2-aryl-propionamide derivatives useful as bradykinin receptor antagonists and pharmaceutical compositions containing them
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Page/Page column 7, (2011/05/08)
(R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.