# US 5,350,867 A · Inhibitors of farnesyl protein transferase

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 5,350,867 A
- Document ID: US5350867A
- Status: Granted
- Kind: A
- Application number: 08/074,257
- Filed: 1993-06-09
- Granted: 1994-09-27
- Earliest claimed: 1991-12-16
- Assignees: Merck & Co., Inc.
- Inventors: Sheo B. Singh
- Web page: https://patentgrep.com/patent/US5350867A

## CPC

- C07C 57/13: Dicarboxylic acids
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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.

## Claims

### Claim 1

A compound, which inhibits farnesyl-protein transferase, of the formula: ##STR7## wherein: X--X is
CH.dbd.CH(cis);
CH.dbd.CH(trans); or
CH.sub.2 CH.sub.2 ;
R.sup.1 and R.sup.2 are each independently selected from:
a) H;
b) C.sub.1-5 alkyl;
c) C.sub.1-5 alkyl substituted with a member of the group consisting of:
i) phenyl;
ii) phenyl substituted with methyl, methoxy, halogen, (Cl, Br, F, I) or hydroxy;
or a pharmaceutically acceptable salt of a compound of formula (II) in which at least one of R.sup.1 and R.sup.2 is hydrogen.

### Claim 2 (depends on 1)

A compound according to claim 1 which is ##STR8##

### Claim 3 (depends on 1)

A chemotherapeutic composition comprising a pharmaceutical carrier, and dispersed therein, a therapeutically effective amount of compound of claim 1.