916143-41-4Relevant academic research and scientific papers
Proline bis-amides as potent dual orexin receptor antagonists
Bergman, Jeffrey M.,Roecker, Anthony J.,Mercer, Swati P.,Bednar, Rodney A.,Reiss, Duane R.,Ransom, Richard W.,Meacham Harrell,Pettibone, Douglas J.,Lemaire, Wei,Murphy, Kathy L.,Li, Chunze,Prueksaritanont, Thomayant,Winrow, Christopher J.,Renger, John J.,Koblan, Kenneth S.,Hartman, George D.,Coleman, Paul J.
, p. 1425 - 1430 (2008/12/21)
A series of OX2R/OX1R dual orexin antagonists was prepared based on a proline bis-amide identified as a screening lead. Through a combination of classical and library synthesis, potency enhancing replacements for both amide portions
PROLINE BIS-AMIDE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 33-34, (2008/06/13)
The present invention is directed to proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
