Inhibitors of farnesyl-protein transferase
US5756528A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 23, 1996 |
| Grant date | May 26, 1998 |
| Priority date | — |
| Expiry date | May 23, 2016 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D401/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.