405512-86-9Relevant articles and documents
PROCESS FOR MAKING LACTAM TACHYKININ RECEPTOR ANTAGONISTS
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Page/Page column 32-33; 44; 50, (2008/06/13)
The present invention is directed to a process for preparing certain α,α disubstituted γ-lactam derivatives that are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful i
COMBINATION THERAPY FOR THE TREATMENT OF URINARY FREQUENCY, URINARY URGENCY AND URINARY INCONTINENCE
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, (2010/11/29)
This invention concerns compositions for the treatment of urinary frequency, urinary urgency and urinary incontinence comprising a selected antagonist of the NK-1 receptor or a pharmaceutically acceptable salt thereof and an anti-muscarinic agent or a pha
Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives
Meurer, Laura C.,Finke, Paul E.,Owens, Karen A.,Tsou, Nancy N.,Ball, Richard G.,Mills, Sander G.,MacCoss, Malcolm,Sadowski, Sharon,Cascieri, Margaret A.,Tsao, Kwei-Lan,Chicchi, Gary G.,Egger, Linda A.,Luell, Silvi,Metzger, Joseph M.,MacIntyre, D. Euan,Rupniak, Nadia M.J.,Williams, Angela R.,Hargreaves, Richard J.
, p. 4504 - 4511 (2007/10/03)
The synthesis and optimization of a cyclopentane-based hNK1 antagonist scaffold 3, having four chiral centers, will be discussed in the context of its enhanced water solubility properties relative to the marketed anti-emetic hNK1 antagonist EMEND (Aprepitant). Sub-nanomolar hNK1 binding was achieved and oral activity comparable to Aprepitant in two in vivo models will be described.
Lactam tachykinin receptor antagonists
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Page/Page column 8; 9, (2010/02/15)
The present invention is directed to certain lactam 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 compri