359018-66-9Relevant academic research and scientific papers
Thiazole derivatives
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Page/Page column 8-9, (2008/06/13)
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents have the significance given in the specification, and the compounds are neuropeptide Y(NPY) antagonists which are useful in the treatment of o
Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza- benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists
Rueeger, Heinrich,Gerspacher, Marc,Buehlmayer, Peter,Rigollier, Pascal,Yamaguchi, Yasuchika,Schmidlin, Tibur,Whitebread, Steven,Nuesslein-Hildesheim, Barbara,Nick, Hanspeter,Cricione, Leoluca
, p. 2451 - 2457 (2007/10/03)
Combination of structural elements from a potent Y5 antagonist (2) with thiazole fragments that exhibit weak Y5 affinities followed by lead optimisation led to the discovery of (5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen-2-yl)- piperidin-4-ylmethyl-amino and (4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen-2- yl)-piperidin-4-ylmethyl-amino derivatives. Both classes of compounds are capable of delivering potent and selective orally and centrally bioavailable NPY Y5 receptor antagonists.
