10325. Telaprevir

Nomenclature

CAS number: 402957-28-2
(1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-l-valyl-N-[(1S)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide; (1S,3aR,6aS)-2-[(2S)-2-[[(2S)-cyclohexyl[(pyrazinylcarbonyl)amino]acetyl]amino]-3,3-dimethylbutanoyl]-N-[(1S)-1-[2-(cyclopropylamino)oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide; LY-570310; VX-950.
C36H53N7O6; mol wt 679.85.
C 63.60%, H 7.86%, N 14.42%, O 14.12%.

Description and references

Peptidomimetic inhibitor of the NS3-4A serine protease of hepatitis C virus (HCV). Prepn: R. E. Babine et al., WO 0218369; eidem, US 050197299 (2002, 2005 both to Lilly); and SAR: S.-H. Chen et al., Lett. Drug Des. Discovery 2, 118 (2005) DOI. Pharmacology and antiviral activity: R. B. Perni et al., Antimicrob. Agents Chemother. 50, 899 (2006) DOI PubMed. Clinical evaluation in hepatitis C patients: N. Forestier et al., Hepatology 46, 640 (2007) DOI PubMed; E. Lawtiz et al., J. Hepatol. 49, 163 (2008) DOI PubMed.

Chemical structure

Therapeutic Category

Antiviral.

Keywords

Antiviral