Cell-specific glycopeptide ligands
US4386026A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Apr 20, 1981 |
| Grant date | May 31, 1983 |
| Priority date | — |
| Expiry date | Apr 20, 2001 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07J41/005
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release. Other examples include the macrophage ligand N.sup.2 -N.sup.2, N.sup.6 -Bis-[3-(.alpha.-D-mannopyranosylthio)propionyl]-6-lysyl-N.sup.6 -[3-(.alpha.-D-mannopyranosylthio)propionyl]-L-lysine, 5, which when coupled to .beta.-glucocerebrosidase, can deliver the enzyme selectively to kupffer cells. This is useful in the enzyme replacement therapy of Gaucher's disease.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.