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US 5,352,705 AGranted
Inhibitors of farnesyl protein transferase
AssigneeMerck & Co., Inc.
InventorsAlbert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
Life of this patent
Estimating the term…
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.
Claims12
A compound of the formula:
- ##STR8## wherein:
- ##STR9## ##STR10## R.sup.1 is an alkyl group, hydrogen, 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 which alternatively may be substituted with an aryl group;
- R.sup.2 is the side chains of naturally occurring amino acids, or in the alternative may be substituted or unsubstituted aliphatic, or aromatic groups, selected from the group consisting of allyl, cyclohexyl, phenyl, or saturated chains of 2 to 8 carbon atoms which may be branched or unbranched, wherein the aliphatic substitutents may be substituted with an aromatic ring;
- R.sup.3 is an aromatic ring or in the alternative, an alkyl group or an aryl substituted alkane, wherein the aromatic ring is unsubstituted or in the alternative, substituted with one or more groups selected from the group consisting of alkyl, halo, alkoxy, trifluoromethyl or sulfamoyl groups, and which may be polycyclic;
- or the pharmaceutically acceptable salts thereof.
2 more elements
Dependencies are inferred from the claim text.