680588-95-8Relevant academic research and scientific papers
N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists
Aissaoui, Hamed,Koberstein, Ralf,Zumbrunn, Cornelia,Gatfield, John,Brisbare-Roch, Catherine,Jenck, Francois,Treiber, Alexander,Boss, Christoph
scheme or table, p. 5729 - 5733 (2009/06/30)
A series of dual OX1R/OX2R orexin antagonists was prepared based on a N-glycine-sulfonamide core. SAR studies of a screening hit led to compounds with low nanomolar affinity for both receptors and good oral bioavailability. One of these compounds, 47, has demonstrated in vivo activity in rats following oral administration.
SULFONYLAMINO-ACETIC ACID DERIVATIVES
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Page 42, (2010/02/06)
The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
