Heterocyclic inhibitors of farnesyl protein transferase

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/04 (2006.01) A61K 31/47 (2006.01) A61K 38/04 (2006.01) C07D 217/26 (2006.01) C07D 401/02 (2006.01) C07D 403/06 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 417/12 (2006.01) C07K 5/06 (2006.01) C07K 5/078 (2006.01) C07K 5/083 (2006.01) C07K 5/087 (2006.01) C07K 5/097 (2006.01) C07K 5/103 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2118985

Abstract HETEROCYCLIC INHIBITORS OF FARNESYL PROTEIN TRANSFERASE Inhibition of farnesyl protein transferase is effected by compounds of the formula Image 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.

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