the new farnesyle transferase inhibitors, their preparation, pharmaceutical compositions which contain them.

摘要

The invention concerns novel products of general formula (I), the preparation, the pharmaceutical compositions containing them and their use for preparing medicines. In said formula, Ar represents a substituted or condensed phenyl radical, or polycyclic or heterocyclic aromatic radical; R represents a radical of general formula -(CH2)m-X1-(CH2)n-Z in which X1 represents a single bond, O, S; m = 0, 1; n = 0, 1, 2; the CH2 radicals can be substituted; Z represents carboxy, COOR6, (R6 = alkyl), CON(R7)(R8) (R7 = hydrogen or alkyl) and R8 = hydrogen hydroxy, arylsulphonyl, heterocyclyl, amino optionally substituted, alkyloxy optionally substituted, alkyl optionally substituted, amino, PO(OR9)2 (R9 = hydrogen or alkyl), a -NH-CO-T (T = hydrogen or alkyl optionally substituted), or else (II); R1 and R2 = hydrogen or halogen or alkyl, alkyloxy optionally substituted, alkylthio, alkyloxycarbonyl or else R1 and R2 in the ortho position relative to each other, form a heterocyclic compound containing 1 or 2 heteroatoms optionally substituted; R3 and R4 = hydrogen or halogen or alkyl, alkylene, alkyloxy, alkylthio, carboxy or alkyloxycarbonyl; R5 = hydrogen, alkyl, alkylthio; X = O or S or -NH-, -CO- methylene, vinyldiyl, alkene-1,1-diyl or cycloalkan-1,1-diyl; and Y = O or S in racemic form and the optical isomers and salts of the product of general formula (I). The products of formula (I) are inhibitors of farnesyl transferase which remarkable tumoricidal and anti-leukemic properties.