发明名称 CHELATORS FOR RADIOACTIVELY LABELED CONJUGATES COMPRISING A STABILIZING SIDECHAIN
摘要 <p>The invention relates to a conjugate PT comprising (a) a peptide P and (b) a targeting moiety T; wherein the peptide P contains from 4 to 20 amino acid residues with optionally a single thiol moiety at the C- or N-terminus replacing one of these amino acid residues, and including a complexing amino acid sequence comprising (i) a tridentate or tetradentate planar chelator containing a ligand backbone defined by a perimeter containing - a single sulfur donor atom, - two or three non-sulfur donor atoms, and - intervening atoms between the donor atoms; and (ii) a stabilizing sidechain comprising a further donor atom, the further donor atom being covalently linked to the ligand backbone of the planar chelator through two or three intervening atoms, provided that - said further donor atom is neither the nitrogen nor the oxgen atom of a peptide bond and - if said further donor atom is part of a heterocyclic ring, no more than one of the intervening atoms can be part of that ring; and a radioactive metal complexed to the donor atoms of the planar chelator.</p>
申请公布号 WO2006094725(A1) 申请公布日期 2006.09.14
申请号 WO2006EP01986 申请日期 2006.03.03
申请人 SCHERING AG;CYR, JOHN E. 发明人 CYR, JOHN E.
分类号 A61K51/08;A61K51/04 主分类号 A61K51/08
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