Hepatitis C inhibitor peptide analogues

Details Hepatitis C inhibitor peptide analogues Hepatitis C inhibitor peptide analogues

1998-08-10

2000-11-07

Celsa, Bennett

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 17, 514 18, 530329, 530330, 4241891, A61K 3804, C07K 500

Patent

active

061437158

ABSTRACT:
Compound of formula (I) active against the Hepatitis C virus: ##STR1## wherein B is an acyl derivative; a is 0 or 1; R.sub.6, when present, is carboxy(lower)alkyl; b is 0 or 1; R.sub.5, when present, is C.sub.1-6 alkyl, or carboxy (lower)alkyl; Y is H or C.sub.1-6 alkyl; R.sub.4 is C.sub.1-10 alkyl; R.sub.3 is C.sub.1-10 alkyl; W is --NH--CH(R.sub.2)--C(O)--, wherein R.sub.2 is C.sub.1-6 alkyl; C.sub.6 or C.sub.10 aryl; C.sub.7-16 aralkyl; or carboxy (lower)alkyl; or W is a proline derivative; Q is a group of the formula --Z(R.sub.1)--C(O)--R.sub.13, wherein Z is CH or N; R.sub.1 is C.sub.1-6 alkyl or C.sub.1-6 alkenyl both optionally substituted with thio or halo,; and R.sub.13 is an activated carbonyl substituent, or Q is a phosphonate group of the formula --CH(R.sub.1)--P(O)R.sub.15 R.sub.16 wherein R.sub.15 and R.sub.16 are independently C.sub.6-20 aryloxy; and R.sub.1 is as defined above.

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Steinkuhler et al., Product inhibition of the Hepatitis C Virus NS3 protease, Biochemistry, vol. 37, pp. 8899-8905, 1968.
Ingallinella et al., Potent peptide inhibitors of human Hepatitis C Virus NS3 protease are obtained by optimizing the cleavage products, Biochemisty, vol. 37, pp. 8906-8914, 1998.
Mori, E.A., "The N-terminal region of NS3 serine protease of HCV is important to maintain its enzymatic integrity", Biochem. Biophys. Res. Comm., vol. 231, No. 3, Feb. 24, 1997, pp. 738-742.
Landro, E.A., "Mechanistic role of NS4A peptide cofactor with the truncated NS3 protease of HCV: elucidation of the NS4A stimulatory effect via kinetic mapping and inhibitor mapping", Biochemistry, vol. 36, No. 31, Aug. 5, 1997, pp. 9340-9348.

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