Beta-hairpin peptidomimetics as selective elastase inhibitors

A backbone cyclized peptidic compound, built up from 13 amino acid residues, of the general formula

• cyclo(-Xaa1-Xaa2-Thr3-Xaa4-Ser5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-) (I),
• and pharmaceutically acceptable salts thereof,
• wherein
• Xaa1 is OctGly;
• Arg;
• hArg;
• Cha;
• Glu(Phenethyl);
• or Dab(Butanoyl);
• Xaa2 is Glu;
• Val;
• Leu;
• Nle;
• Phe;
• hPhe;
• DiHPhe;
• Tyr;
• hTyr;
• or Trp;
• Xaa4 is Ala;
• AllylGly;
• Abu;
• or Val;
• Xaa6 is Ile;
• or OctGly;
• Xaa7 is Pro;
• Xaa8 is Pro;
• Xaa9 is Gln;
• or Tyr;
• Xaa10 is Lys;
• or Asn;
• Xaa11 is hLeu;
• Ser;
• hSer;
• hSer(Me);
• Thr;
• alloThr;
• Asn;
• Gln;
• hGln;
• Dap;
• Tyr;
• or His;
• Xaa12 is DPro;
• and
• Xaa13 is Pro;
• Tic;
• Glu;
• Asp;
• Ala;
• Val;
• or Lys;
• with the proviso that
• if Xaa1 is OctGly, then
• Xaa2 is Glu;
• or Nle;
• Xaa4 is Ala;
• or Abu;
• Xaa6 is Ile;
• or OctGly;
• Xaa10 is Lys;
• Xaa11 is Ser;
• Thr;
• Asn;
• or Gln;
• Xaa13 is Pro;
• Tic;
• Ala;
• Val;
• or Lys;
• and/or if Xaa6 is OctGly, then
• Xaa1 is OctGly;
• Arg;
• or Cha;
• Xaa2 is Glu;
• or Nle;
• Xaa4 is Ala;
• or Abu;
• Xaa10 is Lys;
• Xaa11 is Ser;
• Thr;
• Asn;
• Gln;
• Xaa13 is Pro;
• Tic;
• Ala;
• Val;
• or Lys;
• and with the further proviso that
• if Xaa11 is Tyr;
• or His, then
• Xaa1 is Arg;
• hArg;
• or Glu(Phenethyl).