189816-05-5Relevant articles and documents
Hepatitis C Virus Inhibitors
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Page/Page column 27-28, (2009/12/02)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors
Vendeville, Sandrine,Nilsson, Magnus,Kock, Herman de,Lin, Tse-I,Antonov, Dmitry,Classon, Bjoern,Ayesa, Susana,Ivanov, Vladimir,Johansson, Per-Ola,Kahnberg, Pia,Eneroth, Anders,Wikstrom, Kristina,Vrang, Lotta,Edlund, Michael,Lindstroem, Stefan,Vreken, Wim Van de,McGowan, David,Tahri, Abdellah,Hu, Lili,Lenz, Oliver,Delouvroy, Frederic,Dooren, Marleen Van,Kindermans, Natalie,Surleraux, Dominique,Wigerinck, Piet,Rosenquist, Asa,Samuelsson, Bertil,Simmen, Kenneth,Raboisson, Pierre
scheme or table, p. 6189 - 6193 (2009/08/07)
A novel series of P3-truncated macrocyclic HCV NS3/4A protease inhibitors containing a P2 proline-urea or carbamate scaffold was synthesized. Very potent inhibitors were obtained through the optimization of the macrocycle size, urea and proline substitution, and bioisosteric replacement of the P1 carboxylic acid moiety. Variation of the lipophilicity by introduction of small lipophilic substituents resulted in improved PK profiles, ultimately leading to compound 13Bh, an extremely potent (Ki = 0.1 nM, EC50 = 4.5 nM) and selective (CC50 (Huh-7 cells) > 50 μM) inhibitor, displaying an excellent PK profile in rats characterized by an oral bioavailability of 54% and a high liver exposure after oral administration.
Substituted cycloalkyl P1' hepatitis C virus inhibitors
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Page/Page column 20, (2010/02/06)
The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.