Compounds for enzyme inhibition
US8129346B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 14, 2005 |
| Grant date | Mar 6, 2012 |
| Priority date | — |
| Expiry date | Dec 25, 2026 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/0827
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.