Farnesyl protein transferase inhibitors e.g. of formula (I) and (II) and their enantiomers, diastereomers, salts, prodrugs and solvates are new: G = a group of formula (i): m, n, r, s, t = 0 or 1; p = 0-2; V, W, X = O, H, R1, R2 or R3; Z, Y = CHR9, SO2, SO3, CO, CO2, O, NR10, SO2NR11, CONR12, C(=NCN), C(=NCN)NR13, NR14C(=O), NR15SO2, C(=O)N(R16)N(R17), SO2N(R18)N(R19), S(=O)(=NR20), S(=NR21)(=NR22) or Z may be absent; R6, R7, R9-R22, R24-R38 = H, lower alkyl, substituted alkyl or optionally substituted aryl; R4, R5 = H, halo, NO2, CN or UR23; U = S, O, NR24, CO, SO, SO2, CO2, NR25CO2, NR26CONR27, NR28SO2, NR29SO2NR30, SO2NR31, NR32CO, CONR33, PO2R34, PO3R35 or is absent; R1-R3 = H, alkoxycarbonyl, aralkyl, cycloalkyl, CN, COOH, CONQ1Q2 or optionally substituted alkyl, alkenyl, alkynyl, aryl or heterocyclyl; Q1, Q2 = H, alkyl aryl or aralkyl; R8, R23 = H, aralkyl, cycloalkyl or optionally substituted alkyl, alkenyl, alkynyl, aryl or heterocyclyl; or two of R1-R3 = cycloalkyl; R, S', T = CH2, CO or CH(CH2)pQ; Q = NR36R37, OR38 or CN; A, B, C, D = C, O, S or N; provided that (i) when m = 0 then V and W are not both O, or W + X = O only if Z = absent, O, NR10, CHR9, NR14C(=O) or NR15SO2 in (I) or (II) and V+X = O only if Y = O, NR10, CHR9, NR14C(=O) or NR15SO2 in (III) or (IV); (ii) R23 is not H when U = SO, SO2, NR25CO2 or NR28SO2; or R8 is not H when Z = SO2, CO2 NR15SO2, S(=O)(=NR20) or S(=NR21)(=NR22). About 560 compounds are specifically claimed e.g. 2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1- naphthalenylcarbonyl)-1H-1,4-benzodiazepine.HCl.
Inhibitors of farnesyl protein transferase