Extended lifetimes in vivo renin inhibitors
US6107489A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 12, 1999 |
| Grant date | Aug 22, 2000 |
| Priority date | — |
| Expiry date | Mar 12, 2019 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D233/64
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have renin inhibition activity are provided. Specifically, the renin inhibitor compounds of the present invention are tripeptide derivatives of a known renin inhibitor which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated renin inhibitors thereby have extended lifetimes in the bloodstream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining renin inhibitory activity for extended periods of time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting renin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.