The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, Y, n and m are as defined herein. The compounds are useful for the treatment and prevention of hepatitis C viral infection in mammals by inhibiting HCV NS3 protease. The invention further relates to azalactone compounds of the formula (III) which can be reacted with an amide anion to produce the compounds of formula (I).

Hepatitis C inhibitor peptide analogs

Compound of formula (I) active against the Hepatitis C virus, wherein when Q is CH2, a is 0, b is 0 and B is an amide derivative; or when Q is N-Y wherein Y is H or C1-6 alkyl, then B is an acyl derivative; R6, when present, is C1-6 alkyl substituted with carboxyl; R5, when present, is C1-6 alkyl optionally substituted with carboxyl; when Q is either CH2 or N-Y, then Z is oxo or thioxo; R4 is C1-10alkyl, C3-7 cycloalkyl or C4-10 (alkylcycloalkyl); R3 is C1-10 alkyl optionally substituted with carboxyl, C3-7 cycloalkyl or C4-10 (alkylcycloalkyl); W is a proline derivative; R1' is hydrogen, and R1 is C1-6 alkyl optionnaly substituted with thiol; or R1 is C2-6 alkenyl; or R1' and R1 together form a 3- to 6-membered ring; and A is hydroxy or a pharmaceutically acceptable salt or ester thereof.

Hepatitis c inhibitor peptides

Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.

Hepatitis c inhibitor compounds

The biosynthesis of steroids and triterpenoids

The present invention relates to compounds of formula (I): wherein R1, R2, R4, n and m are as defined herein and R3 is selected from: (i) -C(O)OR31 wherein R31 is (C1-6)alkyl or aryl, wherein the (C1-6)alkyl is optionally substituted with one to three halogen substituents; (ii) -C(O)NR32R33, wherein R32 and R33 are each independently selected form H, (C1-6)alkyl, and Het; (iii) -SOvR34, wherein v is 1 or 2 and R34 is selected from: (C1-6)alkyl, aryl, Het, and NR32R33 wherein R32 and R33 are as defined above; and (iv) -CO(O)-R35, wherein R35 is selected from (C1-8)alkyl, (C3-7)cycloalkyl-(C1-4)alkyl, aryl, aryl-(C1-6)alkyl, Het and Het-(C1-6)alkyl, each of which are optionally substituted with one or more substituents each independently selected from halo, (C1-6)alkyl, (C3-7)cycloalkyl, aryl, Het, hydroxyl, -O-(C1-6)alkyl, -S-(C1-6)alkyl, -SO-(C1-6)alkyl, -SO2-(C1-6)alkyl, -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl, wherein the aryl portion of the -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl are each optionally substituted with one to five halo substituents. The present invention further relates to pharmaceutical compositions containing the compounds of formula (I) and methods for using these analogs in the treatment of HCV infection.

Hepatitis c inhibitor dipeptide analogs

This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P2 moiety is substituted with various nitrogen-containing heterocyclic groups. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.

Novel elastase inhibitors

Inhibition of oxidosqualene cyclase by substituted quinolizidines

L'invention concerne des composes inhibiteurs d'elastase, en particulier de l'elastase des neutrophiles chez l'homme. Ces inhibiteurs sont de peptides courts synthetiques dans lesquels la fraction P2 est substituee par differents groupes heterocycliques contenant de l'azote. En tant qu'inhibiteurs de l'elastase des neutrophiles chez l'homme, ces composes sont efficaces dans le traitement d'un malade atteint d'une maladie inflammatoire associee aux neutrophiles.

Steven L. Gallion

Papers

Novel elastase inhibitors

Inhibition of oxidosqualene cyclase by substituted quinolizidines

Nouveaux inhibitieurs d'elastase