| abstract |
The present invention relates to peptidomimetic compounds of formula (I) and intermediates for their preparation as protease inhibitors, particularly as serine protease inhibitors, more particularly as hepatitis C NS3 protease inhibitors. The present invention further relates to the use of pharmaceutical compositions as well as HCV protease inhibition or HCV infection or physiological healing or prophylactic treatment of such infection. In formula (1): R0 is a bond or a difluoromethylene group; R1 is hydrogen, optionally substituted aliphatic or aromatic; R2 and R9 are independently an optionally substituted aliphatic cyclic or aromatic group; R3, R5 and R7 are each independently selected from optionally substituted 1,1- or 1,2-cycloalkylene; or optionally substituted 1,1- or 1,2-heterocyclylene; or a further optionally substituted aliphatic ring or aromatic group, and optionally an additional aliphatic substituted methylene or ethylene group; R4, R6, R8 and R10 are independently hydrogen or optionally substituted aliphatic; (NO) is substituted by a more cyclic aza-heterocyclyl group, or optionally substituted multiple ring aza-heterocyclenyl, wherein the unsaturated bond is R9-L- (N (R8) -R7-C (O) -) nN (R6) -R5-C (O) N is in a fraction of the half-chain (or in a ring farther away from said ring-bearing ring) which is attached to the -C (O) -N (R4) -R3-C (O) C (O) NR2R1 group ; L is -C (O) -, -OC (O) -, -NR 10 C (O) -, -S (O) 2 - or -NR 10 S (O) 2; and n is 0 or 1. Oh |