Novel Liver-targeting Agents and their Synthesis

This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilo triacetic 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 Ne-benzyloxycarbonyl-Na-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- AH A- Asp was used to conjugate 2 moles 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.

Attached files:


Patents:
WO 2,011,038,356

Inventor(s): LEE REIKO TAKASAKA [US]; LEE YUAN-CHUAN [US]; WANG MEI-HUI; LIN WUU-JYH

Type of Offer: Licensing



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