Liver-targeting agents and their synthesis
US8552163B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Sep 27, 2010 |
| Grant date | Oct 8, 2013 |
| Priority date | — |
| Expiry date | Apr 11, 2031 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H15/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilotriacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in Nε-benzyloxycarbonyl-Nα-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 molecules of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.