# US 5,705,686 A · Inhibition of farnesyl transferase

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- Number: US 5,705,686 A
- Document ID: US5705686A
- Status: Granted
- Kind: A
- Application number: 08/371,682
- Filed: 1995-01-12
- Granted: 1998-01-06
- Earliest claimed: 1993-05-18
- Assignees: University of Pittsburgh
- Inventors: Said Sebti; Andrew Hamilton
- Web page: https://patentgrep.com/patent/US5705686A

## CPC

- C07C 323/25: the carbon skeleton being acyclic and saturated
- C07C 323/59: with acylated amino groups bound to the carbon skeleton
- C07C 323/60: with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
- C07C 329/06: having sulfur atoms of thiocarbonic groups bound to acyclic carbon atoms
- C07D 207/34: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D 215/38: Nitrogen atoms (nitro radicals C07D215/18)
- C07D 217/22: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D 263/48: Nitrogen atoms not forming part of a nitro radical
- C07D 277/38: Nitrogen atoms
- C07D 307/66: Nitrogen atoms
- C07K 5/1013: {the side chain containing O or S as heteroatoms, e.g. Cys, Ser}
- C07K 5/1016: {and aromatic or cycloaliphatic}
- C07K 14/5437: {IL-13}
- C07K 14/61: Growth hormone [GH], i.e. somatotropin
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A compound of the formula C.sup.1 R where C.sup.1 is 3-mercapto-2-amino-propylamino and R is an aryl group. The compounds are useful for inhibiting p21ras farnesyltransferase.

## Claims

### Claim 1

A compound of the formula
C.sup.1 R
where C.sup.1 is 3-mercapto-2-amino-propylamino and R is biphenyl, optionally substituted with a carboxyl and/or alkyl moiety; or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A compound according to claim 1 wherein R is a biphenyl group substituted with --COOH.

### Claim 3 (depends on 1)

A compound according to claim 1 wherein R is a biphenyl group substituted with lower alkyl.

### Claim 4 (depends on 3)

A compound according to claim 3 wherein the lower alkyl is methyl.

### Claim 5 (depends on 1)

A compound according to claim 1 of the formula: ##STR1## where R.sup.1 is hydrogen, COOH or CH.sub.3 ; and R.sup.2 is hydrogen or COOH, R.sup.1 being COOH or CH.sub.3 when R.sup.2 is hydrogen.

### Claim 6 (depends on 5)

A compound according to claim 5 wherein R.sup.1 is COOH and R.sup.2 is hydrogen.

### Claim 7 (depends on 1)

A method of inhibiting p21ras farnesyltransferase in a host in need of such inhibition which comprises administering to said host an effective amount of a compound according to claim 1.

### Claim 8 (depends on 1)

A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier therefor.