In vitro and in vivo isotope effects with hepatitis C protease inhibitors: Enhanced plasma exposure of deuterated telaprevir versus telaprevir in rats
Telaprevir 2 (VX-950), an inhibitor of the hepatitis C virus (HCV a) NS3-4A protease, is in phase 3 clinical trials. One of the major metabolites of 2 is its P1-(R)-diastereoisomer, 3 (VRT-394), containing an inversion at the chiral center next
Maltais, Fran?ois,Jung, Young Chun,Chen, Minzhang,Tanoury, Jerry,Perni, Robert B.,Mani, Nagraj,Laitinen, Leena,Huang, Hui,Liao, Shengkai,Gao, Hongying,Tsao, Hong,Block, Eric,Ma, Chien,Shawgo, Rebecca S.,Town, Christopher,Brummel, Christopher L.,Howe, David,Pazhanisamy,Raybuck, Scott,Namchuk, Mark,Bennani, Youssef L.
experimental part
p. 7993 - 8001
(2010/08/19)
Deuterated hepatitis C protease inhibitors
A deuterated α-ketoamido steric specific compound of the formula wherein D denotes a deuterium atom on a steric specific carbon atom.
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Page/Page column 19; 21
(2010/11/28)
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