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 …

…, J Jiang, J Bunda, D Wilson, J Bao, H Lu…

文献索引：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. Journal of Medicinal Chemistry, 2013 , vol. 56, # 14 p. 5940 - 5948

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被引用次数: 4

摘要

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 predicted, based on data in preclinical species, to have a human half-life longer than 40 h and likely to have drug–drug- interactions (DDI), as 2 is a victim of CYP3A4 inhibition caused by its exclusive clearance ...