860642-35-9Relevant academic research and scientific papers
Organocatalytic Stereoconvergent Synthesis of α-CF3 Amides: Triketopiperazines and Their Heterocyclic Metamorphosis
Foster, Robert W.,Lenz, Eva N.,Simpkins, Nigel S.,Stead, Darren
, p. 8810 - 8813 (2017/07/11)
The highly enantioselective alkylation of α-CF3 enolates, generated from triketopiperazines, has been accomplished through use of a bifunctional thiourea organocatalyst to facilitate 1,4-addition to varied enone acceptors. On treatment with appropriate nitrogen nucleophiles, the chiral triketopiperazine products undergo a metamorphosis, to provide novel fused heterocyclic lactams such as extended pyrazolopyrimidines.
Use of NK-1 receptor antagonists in pruritus
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, (2014/12/12)
The invention relates to methods for treating pruritus with an NK-1 receptor antagonist. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonist.
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists
Jiang, Jinlong,Bunda, Jaime L.,Doss, Geoge A.,Chicchi, Gary G.,Kurtz, Marc M.,Tsao, Kwei-Lan C.,Tong, Xinchun,Zheng, Song,Upthagrove, Alana,Samuel, Koppara,Tschirret-Guth, Richard,Kumar, Sanjeev,Wheeldon, Alan,Carlson, Emma J.,Hargreaves, Richard,Burns, Donald,Hamill, Terence,Ryan, Christine,Krause, Stephen M.,Eng, WaiSi,DeVita, Robert J.,Mills, Sander G.
experimental part, p. 3039 - 3046 (2010/03/03)
3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy} -4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]-cyclopent-2-en-1-one (17) is a high affinity, brain-penetrant, hydroisoindoline-based neurokinin-1 (NK1) receptor antagonist with a long ce
POLYMORPHS OF A HYDROISOINDOLINE TACHYKININ RECEPTOR ANTAGONIST
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Page/Page column 15-16, (2008/12/05)
This application is directed to a novel polymorph of a hydroisoindoline tachykinin receptor antagonist having the following structural formula A.
Process for making hydroisoindoline tachykinin receptor antagonists
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Page/Page column 8; 9, (2008/06/13)
The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
HYDROISOINDOLINE TACHYKININ RECEPTOR ANTAGONISTS
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Page/Page column 16, (2008/06/13)
The present invention is directed to certain hydroisoindoline 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 formulati
Hydroisoindoline tachykinin receptor antagonists
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Page/Page column 8, (2008/06/13)
The present invention is directed to certain hydroisoindoline 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 formulati
