Template-fixed peptidomimetics as inhibitors of serine proteases
AssigneesPolyphor AG, UniversitäT ZüRich
InventorsDaniel Obrecht, John Anthony Robinson, Anne Descours
Life of this patent
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Abstract
Template-fixed β-hairpin peptidomimetics of the general formulae (I), wherein Z is a template-fixed chain of 7 to 11 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
Claims4
Compounds of the general formula
- is the group DPro-LPro;
- Z is a chain of n α-amino acid residues, n being the integer 7 or 11, the positions of said amino acid residues in said chain being counted starting from the N-terminal amino acid;
- and either —n is 7;
- and the amino acid residues in positions 1-7 are:
- —P1:
- Thr;
- P2:
- Lys;
- P3:
- Ser;
- P4:
- Ile;
- P5:
- Pro;
- P6:
- Pro;
- P7:
- Ile;
- or
- —P1:
- Thr;
- P2:
- Lys;
- P3:
- Ala;
- P4:
- Ile;
- P5:
- Pro;
- P6:
- Pro;
- P7:
- Ile;
- or
- —P1:
- Thr;
- P2:
- Lys;
- P3:
- Ser;
- P4:
- Ile;
- P5:
- Pro;
- P6:
- Ala;
- P7:
- Ile;
- or
- —P1:
- Thr;
- P2:
- Lys;
- P3:
- Ser;
- P4:
- Ile;
- P5:
- Pro;
- P6:
- Pro;
- P7:
- Ala;
- or
- —n is 11:
- and the amino acid residues in positions 1-11 are:
- —P1:
- Arg;
- P2:
- Cys;
- P3:
- Thr;
- P4:
- Lys;
- P5:
- Ser;
- P6:
- Ile;
- P7:
- Pro;
- P8:
- Pro;
- P9:
- Ile;
- P10:
- Cys;
- P11:
- Phe;
- the two Cys residues forming a disulfide bridge;
- and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.