Heterocyclic inhibitors of farnesyl protein transferase.

摘要

Inhibition of farnesyl protein transferase is effected by compounds of the formula <CHEM> its enantiomers, diastereomers, pharmaceutically acceptable salts, prodrugs or solvates thereof, wherein: A1 and A2 are each independently H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, phenyl or substituted phenyl; G1 is S or O; G2 is H, -C(O)OH, -C(O)NH2, 5-tetrazolyl, -C(O)N(R7)OH or -CH2OH; X is O or R8N; Y and Z are each independently -CH2- or -C(O)-; R1, R2, R3, R4, R5, R6 and R7 are each independently H or alkyl; R1 may also be alkanoyl, R1 and A1 taken together may be -(CH2)m; R8 is H, alkyl, phenyl, phenylalkyl, substituted phenyl, (substituted phenyl)alkyl or -C(O)R9; R9 is H, alkyl, phenyl, phenylalkyl, substituted phenyl or (substituted phenyl)alkyl; m is 3 or 4; n is 0, 1 or 2; p is 0, 1 or 2; and q is 0 or 1, with the proviso that when p is 0, then q is also 0.