- Organocatalytic Stereoconvergent Synthesis of α-CF3 Amides: Triketopiperazines and Their Heterocyclic Metamorphosis
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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.
- Foster, Robert W.,Lenz, Eva N.,Simpkins, Nigel S.,Stead, Darren
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p. 8810 - 8813
(2017/07/11)
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- Use of NK-1 receptor antagonists in pruritus
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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.
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- Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists
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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
- 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.
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experimental part
p. 3039 - 3046
(2010/03/03)
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- POLYMORPHS OF A HYDROISOINDOLINE TACHYKININ RECEPTOR ANTAGONIST
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This application is directed to a novel polymorph of a hydroisoindoline tachykinin receptor antagonist having the following structural formula A.
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Page/Page column 15-16
(2008/12/05)
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- Process for making hydroisoindoline tachykinin receptor antagonists
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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.
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Page/Page column 8; 9
(2008/06/13)
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- HYDROISOINDOLINE TACHYKININ RECEPTOR ANTAGONISTS
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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
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Page/Page column 16
(2008/06/13)
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- Hydroisoindoline tachykinin receptor antagonists
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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
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Page/Page column 8
(2008/06/13)
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