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Molecular constructs with targeting and effector moieties

  • US 10,010,626 B2
  • Filed: 01/18/2016
  • Issued: 07/03/2018
  • Est. Priority Date: 01/16/2015
  • Status: Active Grant
First Claim
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1. A molecular construct comprising a first linker unit and a second linker unit, wherein,the first linker unit comprises a first center core comprising a plurality of amine groups, and a first linking arm and optionally a first coupling arm that are respectively linked to the amine groups of the first center core;

  • andthe second linker unit comprises a second center core comprising a plurality of amine groups, and a second linking arm and optionally a second coupling arm that are respectively linked to the amine groups of the second center core;

    whereinthe first and second center cores are independently a polypeptide comprising a plurality of lysine (K) residues or a compound selected from the group consisting of, benzene-1,3,5-triamine, 2-(aminomethyl)-2-methylpropane-1,3-diamine, tris(2-aminoethyl)amine, benzene-1,2,4, 5-tetraamine, 3,3′

    ,5,5′

    -tetraamine-1,1′

    -biphenyl, tetrakis(2-aminoethyl)methane, tetrakis(ethylamine)hydrazine, N,N,N′

    ,N′

    ,-tetrakis(aminoethyl)ethylenediamine, benzene-1,2,3,4, 5,6-hexaamine, 1-N,1-N,3-N,3-N,5-N,5-N-hexakis-(methylamine)-benzene-1,3,5-triamine, 1-N,1-N,2-N,2-N,4-N,4-N,5-N,5-N,-octakis(methylamine)-benzene-1,2,4,5-triamine, and N,N-bis[(1-amino-3,3-diaminoethyl)pentyl] methanediamine; and

    the first and second linker units are coupled to each other via copper catalyzed azide-alkyne cycloaddition (CuAAC) reaction, strained-promoted azide-alkyne click chemistry (SPAAC) reaction or inverse electron demand Diels-Alder (iEDDA) reaction occurred between any of the followings;

    the first and second center cores, the first coupling arm and the second center core, the first and second coupling arms, or the first center core and the second coupling arm.

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