Farnesyl:protein transferase inhibitors as anticancer agents
AssigneeMerrell Pharmaceuticals Inc.
InventorDavid M. Stemerick
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Abstract
The present invention relates to certain inhibitors of farnesyl:protein transferase which are useful as antineoplastic agents.
Claims2
A method of treating a patient afflicted with a neoplastic disease state selected from the group consisting of leukemia, lung carcinoma, colon carcinoma, and pancreas carcinoma comprising the administration thereto of a therapeutically effective antineoplastic amount of a compound of the formula ##STR23## wherein X is CCl.sub.2 or CF.sub.2, R.sub.1 and R.sub.2 are each independently H;
- C.sub.1 -C.sub.4 alkyl;
- (CH.sub.2).sub.n -Z, wherein n is the integer 0,1,2,3 or 4 and Z is phenyl or naphthyl, unsubstituted or substituted with from 1 to 3 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, CF.sub.3, OCF.sub.3, OH, CN, NO.sub.2 and NH.sub.2 ;
- or a pharmaceutically acceptable cation, and
- A is a radical selected from the group consisting of ##STR24##
A method of controlling the growth of a neoplasm in a patient afflicted with a neoplastic disease state selected from the group consisting of leukemia, lung carcinoma, colon carcinoma, and pancreas carcinoma comprising administration thereto of a therapeutically effective antineoplastic amount of a compound of the formula ##STR25## wherein X is CCl.sub.2 or CF.sub.2, R.sub.1 and R.sub.2 are each independently H;
- C.sub.1 -C.sub.4 alkyl;
- (CH.sub.2).sub.n -Z, wherein n is the integer 0,1,2,3 or 4 and Z is phenyl or naphthyl, unsubstituted or substituted with from 1 to 3 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, CF.sub.3, OCF.sub.3, OH, CN, NO.sub.2 and NH.sub.2 ;
- or a pharmaceutically acceptable cation, and
- A is a radical selected from the group consisting of ##STR26##
Dependencies are inferred from the claim text.