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.
申请公布号
WO2011038356(A3)
申请公布日期
2011.08.04
申请号
WO2010US50424
申请日期
2010.09.27
申请人
JOHNS HOPKINS UNIVERSITY;INSTITUTE OF NUCLEAR ENERGY RESEARCH ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN;LEE, REIKO, TAKASAKA;LEE, YUAN-CHUAN;WANG, MEI-HUI;LIN, WUU-JYH