EP0618221A3

Heterocyclic inhibitors of farnesyl protein transferase.

Abstract

Inhibition of farnesyl protein transferase is effected by compounds of the formula 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.

EP0618221A3, drawing sheet 1
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Term

Term ended

Projected expiry passed 29 March 2014, 12.5 years ago.

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