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US 5,238,922 AGranted
Inhibitors of farnesyl protein transferase
AssigneeMerck & Co., Inc.
InventorsSamuel L. Graham, S. Jane deSolms, Victor M. Garsky
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Abstract
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Claims21
A compound which inhibits farnesylprotein transferase of the formula:
- ##STR7## wherein:
- X, Y and Z are independently H.sub.2 or O, provided that at least one of these is H.sub.2 ;
- R.sup.1 is H, an alkyl group, an acyl group, an alkylsulfonyl group or arylsulfonyl group, wherein alkyl and acyl groups comprise straight chain or branched chain hydrocarbons of 1 to 6 carbon atoms, or in the alternative, R.sup.1 NH may be absent;
- R.sup.2, R.sup.3 and R.sup.4 are the side chains of naturally occurring amino acids, or in the alternative may be substituted or unsubstituted aliphatic, aromatic or heteroaromatic groups, wherein the aliphatic substitutents may be substituted with an aromatic or heteroaromatic ring;
- R.sup.5 is H or a straight or branched chain aliphatic group, which may be substituted with an aromatic or heteroaromatic group;
- or the pharmaceutically acceptable salts thereof.
3 more elements
Dependencies are inferred from the claim text.