NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS
First Claim
1. A liver targeting agent comprising a lysine-based nitrilo triacetic acid structure which acquires multivalency with one or more saccharide groups to bind with a galactosamine chain or lactose chain.
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Abstract
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 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 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.
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Citations
17 Claims
- 1. A liver targeting agent comprising a lysine-based nitrilo triacetic acid structure which acquires multivalency with one or more saccharide groups to bind with a galactosamine chain or lactose chain.
- 5. A method of synthesizing a trivalent ligand in one step, the method comprising conjugating lysine based NTA with three glycosides of GalNAc or Lac.
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11. A method of synthesizing hexa-lactoside, comprising:
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conjugating NTA-(ahLac)3 with TFA-ah modified Asp [CF3CONH(CH2)5CONHCH(CH2COOH)COOH] in DMSO in the presence of DCC/1-OH-Bt; and performing de-N-trifluoroacetylation in aqueous solution containing 10% ethanol and 10% triethylamine (TEA) overnight at room temperature. - View Dependent Claims (12, 13)
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- 14. A method of adding a spacer between NTA and a possible chelator.
Specification