US 7,582,604 B2
Template-fixed peptidomimetics with antibacterial activity
Jan Wim Vrijbloed, Zurich (Switzerland); Daniel Obrecht, Battwil (Switzerland); John Anthony Robinson, Wermatswil (Switzerland); Odile Sellier, Sausheim (France); and Marc Kessler, Bischheim (France)
Assigned to Polyphor Ltd., Allschwil (Switzerland); and Universität Zürich, Zürich (Switzerland)
Filed on Feb. 18, 2005, as Appl. No. 11/62,021.
Application 11/062021 is a continuation of application No. PCT/EP02/09278, filed on Aug. 20, 2002.
Prior Publication US 2005/0239693 A1, Oct. 27, 2005
Int. Cl. A61K 38/12 (2006.01); C07K 7/64 (2006.01)
U.S. Cl. 514—9  [530/317] 13 Claims
 
1. A compound of the general formula

OG Complex Work Unit Drawing
wherein the template is DPro-LPro
Z is a chain of 12 α-amino acid residues, the positions of said amino acid residues in said chain being counted starting from the N-terminal amino acid, wherein the amino acids in positions 1-12 are:
P1: Arg;
P2: Trp;
P3: Leu;
P4: Lys or Val;
P5: Lys;
P6: Arg;
P7: Arg;
P8: Trp;
P9: Leu, Val or Lys;
P10: Tyr or Gln;
P11: Val, Leu, Tyr or Gln; and
P12: Arg;
with the proviso that
the amino acid residue in position P4 is Val; and/or
the amino acid residue in position P9 is Leu or Val; and/or
the amino acid residue in position P10 is Gln; and/or
the amino acid residue in position P11 is Val or Leu or Gln;
and the enantiomer thereof and pharmaceutically acceptable salts thereof.