Inhibitors of farnesyl protein transferase

Details Inhibitors of farnesyl protein transferase Inhibitors of farnesyl protein transferase

C - Chemistry, Metallurgy

07

K

C07K 5/04 (2006.01) A61K 38/04 (2006.01)

Patent

CA 2143588

Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula Image their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein: A1 and A2 are each independently H, alkyl, substituted alkyl, phenyl or substituted phenyl Y and Z are each independently -CH2- or -C(O)-; R1 and R2 are each independently H or alkyl; R1 and A1 taken together may be -(CH2)m- R3 is H, alkyl or phenyl; J, K and L are each independently, N, NR4, O, S or CR5 with the provisos that only one of the groups J, K and L can be O or S, one or two of the groups J, K and L may be N or NR4, and at least one of the groups J or L must be N, NR4, O or S to form a fused five-membered heteroring; the bond between J and K or K and L may also form one side of a phenyl ring fused to the fused five-membered heteroring; x is O or NR6; R4 is H, alkyl or phenylalkyl; R5 is H or alkyl; R6 is H, alkyl, phenyl, phenylalkyl, substituted phenyl, (substituted phenyl)alkyl or C(O)R7; R7 is H, alkyl, phenyl or substituted phenyl; m is 3 or 4; p is 0, 1 or 2; and q is 0 or 1, with the proviso that when p is 0, q is also 0.

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