1070764-29-2Relevant academic research and scientific papers
2-[(3a R,4 R,5 S,7a S)-5-{(1 S)-1-[3,5-bis(trifluoromethyl)phenyl]-2- hydroxyethoxy}-4-(2-methylphenyl)octahydro-2 H -isoindol-2-yl]-1,3-oxazol-4(5 H)-one: A potent human NK1 receptor antagonist with multiple clearance pathways
Kassick, Andrew J.,Jiang, Jinlong,Bunda, Jaime,Wilson, David,Bao, Jianming,Lu, Huagang,Lin, Peter,Ball, Richard G.,Doss, George A.,Tong, Xinchun,Tsao, Kwei-Lan C.,Wang, Hong,Chicchi, Gary,Karanam, Bindhu,Tschirret-Guth, Richard,Samuel, Koppara,Hora, Donald F.,Kumar, Sanjeev,Madeira, Maria,Eng, Waisi,Hargreaves, Richard,Purcell, Mona,Gantert, Liza,Cook, Jacquelyn,Devita, Robert J.,Mills, Sander G.
, p. 5940 - 5948 (2013/08/23)
Hydroisoindoline 2 has been previously identified as a potent, brain-penetrant NK1 receptor antagonist with a long duration of action and improved profile of CYP3A4 inhibition and induction compared to aprepitant. However, compound 2 is predict
HYDROXYMETHYL ETHER HYDROISOINDOLINE TACHYKININ RECEPTOR ANTAGONISTS
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, (2008/12/04)
The present invention is directed to certain hydroxymethyl ether 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 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, LUTS, depression, and anxiety.
