Peptide dimers as agonists of the erythropoietin (EPO)...

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues

Reexamination Certificate

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C530S334000, C530S345000, C530S317000, C514S002600, C514S012200

Reexamination Certificate

active

07459522

ABSTRACT:
Novel peptide dimers are provided that bind and activate the erythropoietin receptor (EPO-R) or otherwise act as an EPO agonist. The novel compounds have a first peptide chain R1and a second peptide chain R2, wherein R1and R2may be the same or different, and are linked through a linking moiety. R1is approximately 10 to 40 amino acid residues in length and comprises the sequence X3X4X5GPX6TX7X8X9(SEQ ID NO: 1) wherein X3is C or Hoc, X4is R, H, L or W, X5is M, F, I or nor-leucine (J), X6is any one of the 20 genetically coded L-amino acids or J, X7is W, 1-naphthylalanine (B) or 2-naphthylalanine (U), X8is D, E, I, L or V, and X9is C or Hoc. Similarly, R2comprises the sequence X′3X′4X′5GPX′6TX′7X′8X′9(SEQ IN NO: 2) wherein X′3is C or Hoc, X′4is R, H, L or W, X′5is M, F, I or J, X′6is any one of the 20 genetically coded L-amino acids or J, X′7is W, B or U, X8′ is D, E, I, L or V, and X′9is C or Hoc. Methods for synthesizing the compounds are provided as well, as are pharmaceutical compositions and methods of use.

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