Patent · US Expired

Synthesis of template-fixed β-hairpin loop mimetics

US6878804B1 · kind B1 · utility

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4Claims
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Key dates

Filing dateAug 30, 1999
Grant dateApr 12, 2005
Priority date
Expiry dateAug 30, 2019

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07K7/64
  • WIPO fieldBiotechnology
  • WIPO sectorChemistry

Abstract

Template-fixed β-hairpin loop mimetics comprising a template corresponding to one of the structures (a), (b), (c), (d), (e), (f), (g), (h) and a template-fixed chain of 4 to 20 α-amino acid residues which, if their α-C atom is asymmetric, have L-configuration can be manufactured by a novel process which is based on a mixed solid- and solution phase synthetic strategy. If desired, this process can be modified to give the enantiomers of these template-fixed β-hairpin loop mimetics. These enantiomers are novel compounds, and many of said template-fixed β-hairpin loop mimetics themselves are also novel compounds. The template-fixed β-hairpin loop mimetics and their enantiomers can mimick flat surfaces of proteins and thus be used to probe large surface protein-protein interactions. Accordingly they can serve as lead finding tools for protein targets where it is difficult to find small-molecular-weight lead compounds.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.