945467-31-2Relevant academic research and scientific papers
Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists
Morriello, Gregori J.,DeVita, Robert J.,Mills, Sander G.,Young, Jonathan R.,Lin, Peter,Doss, George,Chicchi, Gary G.,DeMartino, Julie,Kurtz, Marc M.,Tsao, Kwei-Lan C.,Carlson, Emma,Townson, Karen,Wheeldon, Alan,Boyce, Susan,Collinson, Neil,Rupniak, Nadia,Moore, Stephen
, p. 2156 - 2170 (2008/12/21)
Previous work on human NK1 antagonists in which the core of the structure is a substituted pyrrolidine has been disclosed. These compounds showed good binding affinity and functional IP activity, however, many did not exhibit the necessary brai
HEXAHYDRO-3H-PYRROLIZIN-3-ONES USEFUL AS TACHYKININ RECEPTOR ANTAGONISTS
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Page/Page column 28-29, (2008/06/13)
The present invention is directed to certain hexahydroyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
