abstract |
A pharmaceutical composition for treatment of diseases caused by ras farnesylation, which comprises an inhibitor for ras farnesylation of the formula I (I) in which R1 is selected from H, -CO-C1-4-alkyl, -CO-O-C2-4-alkenyl, -CO-O-(CH2)nPh and -C1-C4-alkylene-CONH2, in which the phenyl ring is optionally substituted by a nitro; R2 is H, -COC1-4-alkyl and -COOC1-4-alkyl; R3 is hydroxy, nitro, -(CH2)nCOOR8 (in which R8 represents H, C1-C4-alkyl, C2-C4-alkenyl and n is 0), -CONR9R10 (in which R9 and R10 independently are selected from H, C1-C4-alkyl, -O-C1-C4-alkyl, -O-C2-C4-alkenyl, and -C1-C3-alkylenePh, in which the phenyl ring is optionally substituted by halogen or nitro); -CON(R11)OR12 (in which R11 and R12 independently represent H, C1-C4-alkyl and C2-C4-alkenyl); a group of the formula II, -CONHCHR14-COOR17 (in which R14 is 2-(methylthio)ethyl or 2-(carbonyl)ethyl and R17 is H or C1-C6-alkyl), X-R15 (in which X is O or CH2 and R15 is phenyl), phenyl, a radical of the formula II having L or D configuration on the chiral α carbon contained the corresponding free amino acid; p is 0-3, in which R3 values can be the same or different. |