# US 11,753,446 B2 · Beta-hairpin peptidomimetics

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- Number: US 11,753,446 B2
- Document ID: US11753446B2
- Status: Granted
- Kind: B2
- Application number: 16/843,527
- Filed: 2020-04-08
- Published: 2020-07-23
- Granted: 2023-09-12
- Earliest claimed: 2014-09-30
- Assignees: Polyphor AG
- Applicants: Polyphor AG
- Inventors: Daniel Obrecht; Anatol Luther; Francesca Bernardini; Peter Zbinden; Sophie Barthelemy; Alexander Lederer
- Web page: https://patentgrep.com/patent/US11753446B2

## CPC

- C07K 7/64: Cyclic peptides containing only normal peptide links
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/12: Antidiarrhoeals
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 13/08: of the prostate
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 19/00: Drugs for skeletal disorders
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 27/02: Ophthalmic agents
- A61P 27/16: Otologicals
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Beta-hairpin peptidomimetics of the general formula (I), cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2], and pharmaceutically acceptable salts thereof, with P1 to P12, T1 and T2 being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

## Claims

### Claim 1

A method of treating infections by Gram-negative bacteria, the method comprising
administering to a subject in need thereof a pharmaceutically acceptable amount of a compound or pharmaceutical composition,
wherein the Gram-negative infections are respiratory infections, skin or soft tissue infections, gastrointestinal infections, eye infections, ear infections, CNS infections, bone infections, cardiovascular infections, or genitourinary infections; and
wherein the compound is a compound of the general formula (I) or a pharmaceutically acceptable salt thereof,
cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2] (I)
wherein the single elements T or P are connected in either direction from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element; and
wherein the compound is selected from
the group consisting of β-hairpin peptidomimetics of general formula (I) having a disulfide linkage; a lactam linkage; or a 1,2,3-triazole linkage between P2 and P11:
cyclo(-Leu-Cys-Tyr-Ala-Dab-Dab-Dab-Trp-Ala-Val-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Ala-Dab-DDab-Dab-Trp-Ala-Val-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Ala-Orn-DDab-Dab-Trp-Ala-Val-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Leu-Ser-
tBuGly-Cys-Val-DDab-Arg-);
cyclo(-Ile-Cys-Tyr-Asn-Orn-DDab-Dab-Leu-Ser-Val-
Cys-Tyr-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-
tBuGly-Cys-Thr-DDab-Dab-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Thr-DDab-Dab-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Ser-DDab-Dab-);
cyclo(-Val-Cys-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-NMeAla-Pro-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Tyr-DDab-Arg-);
cyclo(-Ile-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-DDab-Arg-);
cyclo(-Ile-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-DDab-Ala-);
cyclo(-Ile-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-DDab-Pro-);
cyclo(-Val-Cys-Tyr-Dab-Dap-Dab-Dab-Trp-Dab-
tBuGly-Cys-Thr-DTyr-Pro-);
cyclo(-Ile-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-DAla-Tyr-);
cyclo(-Leu-Cys-Tyr-Ala-Orn-DDab-Dab-Trp-Ala-Tyr-
Cys-Tyr-DDab-Arg-);
cyclo(-Leu-Cys-Val-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Ala-Orn-DDab-Dab-Phe-Ala-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Val-Val-Orn-DDab-Dab-Trp-Tyr-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Val-Orn-DDab-Dab-Trp-Tyr-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Val-Orn-DDab-Dab-Trp-Tyr-Tyr-
Cys-Tyr-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Ala-Orn-DDab-Dab-Trp-Ala-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Phe-Cys-Val-Thr-Orn-DDab-Dab-Trp-Thr-Tyr-
Cys-Dab-DDab-Arg-);
cyclo(-Leu-Cys-Val-Thr-Orn-DDab-Dab-Trp-Thr-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Dab-);
cyclo(-Leu-Cys-Tyr-Ser-Orn-DDab-Dab-Trp-Asn-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Asn-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Asn-Tyr-
Cys-Val-DDab-Dab-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-Dab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Dab-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Val-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Cpa-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Cpg-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Nva-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Abu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Gln-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Leu-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-tBuGly-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DLys-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DArg-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Lys-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Dap-);
cyclo(-Val-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Leu-DDab-Arg-);
cyclo(-Ile-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Ala-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Dap-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Asn-Tyr-
Cys-Val-DAla-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Thr-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Dab-Tyr-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Dab-Tyr-
Cys-Val-DAla-Arg-);
cyclo(-Leu-Pen-tBuGly-Dab-Orn-DDab-Dab-Trp-Dab-
Chg-Pen-Ser-DPro-Pro-);
cyclo(-Leu-Dab-Tyr-Dab-Dab-Dab-Dab-Trp-Dab-
tBuGly-Asp-Ser-DAla-Pro-);
cyclo(-Val-Dab-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Asp-Ser-DAla-Pro-);
cyclo(-Val-Dab-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-Val-
Asp-Thr-DAla-Pro-);
cyclo(-Val-Dab-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Asp-Thr-DThr-Pro-);
cyclo(-Val-Dab-Tyr-Dab-Dab-DDab-Dab-Trp-Dab-
tBuGly-Asp-Ser-DAla-Ala-);
cyclo(-Val-Dab-Tyr-Dab-Dap-DDab-Dab-Trp-Dap-
tBuGly-Asp-Ser-DAla-Tyr-);
cyclo(-Val-Dab-Tyr-Dab-Dab-Dab-Dab-Trp-Dab-
tBuGly-Asp-Ser-Sar-Pro-);
cyclo(-Leu-Asp-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-
tBuGly-Dab-Thr-DDab-Arg-);
cyclo(-Leu-Asp-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-
tBuGly-Dab-Thr-DDab-Dab-);
cyclo(-Leu-Asp-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-Tyr-
Dab-Ser-DAla-Pro-);
cyclo(-Val-Pra-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Abu(4N3)-Ser-DPro-Pro-);
or a pharmaceutically acceptable salt thereof;
and/or
the group consisting of β-hairpin peptidomimetics of general formula (I) having a disulfide linkage; or a lactam linkage between P4 and P9; or disulfide linkages between P2 and P11, and P4 and P9:
cyclo(-Leu-Thr-Tyr-Cys-Dab-Dab-Dab-Trp-Cys-Val-
Thr-Val-DPro-Arg-);
cyclo(-Leu-Thr-Tyr-Cys-Dab-DDab-Dab-Trp-Cys-Val-
Thr-Val-DPro-Arg-);
cyclo(-Leu-Thr-Tyr-Cys-Dab-DDab-Dab-Trp-Cys-Val-
Thr-Val-DPro-Dab-);
cyclo(-Leu-Ser-Tyr-Cys-Orn-DDab-Dab-Trp-Cys-Tyr-
Ala-Ser-DDab-Dab-);
cyclo(-Leu-Ser-Tyr-Cys-Orn-DDab-Dab-Phe-Cys-Val-
Ser-Val-DDab-Arg-);
cyclo(-Leu-Ser-Tyr-Cys-Orn-Gly-Dab-Trp-Cys-Val-
Ala-Val-DDab-Arg-);
cyclo(-Leu-Tyr-Tyr-Dab-Orn-DDab-Dab-Trp-Asp-
tBuGly-Val-Ser-DDab-Pro-);
cyclo(-Leu-Cys-Tyr-Cys-Dab-Dab-Dab-Trp-Cys-Tyr-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Cys-Dab-DDab-Dab-Trp-Cys-Tyr-
Cys-Val-DPro-Arg-);
or a pharmaceutically acceptable salt thereof;
and/or
the group consisting of β-hairpin peptidomimetics of general formula (I)
cyclo(-Val-Ser-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DPro-NMeAla-);
cyclo(-Val-Dap-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Ser-Thr-DAla-Pro-);
cyclo(-Val-Dap-Tyr-Dab-Dab-DDab-Dab-Trp-Dab-
tBuGly-Ser-Thr-DAla-Pro-);
cyclo(-Ile-Thr-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DPro-Tyr-);
cyclo(-Ile-Thr-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DDab-Pro-);
cyclo(-Ile-Thr-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DAla-Tyr-);
cyclo(-Phe-Dap-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DDab-Pro-);
or a pharmaceutically acceptable salt thereof;
wherein said pharmaceutical composition contains said compound of the general formula (I) or a mixture of compounds of general formula (I) and at least one pharmaceutically inert carrier.

### Claim 2

A method of treating an infection by Gram-negative bacteria, the method comprising
administering to a subject in need thereof a pharmaceutically acceptable amount of a compound or pharmaceutical composition,
wherein the infection is a nosocomial infection, a catheter-related infection, a non-catheter-related infection, a urinary tract infection, or a bloodstream infection,
wherein the compound is a compound of the general formula (I) or a pharmaceutically acceptable salt thereof,
cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2] (I)
wherein the single elements T or P are connected in either direction from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element, and
wherein the compound is selected from
the group consisting of β-hairpin peptidomimetics of general formula (I) having a disulfide linkage; a lactam linkage; or a 1,2,3-triazole linkage between P2 and P11:
cyclo(-Leu-Cys-Tyr-Ala-Dab-Dab-Dab-Trp-Ala-Val-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Ala-Dab-DDab-Dab-Trp-Ala-Val-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Ala-Orn-DDab-Dab-Trp-Ala-Val-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Leu-Ser-
tBuGly-Cys-Val-DDab-Arg-);
cyclo(-Ile-Cys-Tyr-Asn-Orn-DDab-Dab-Leu-Ser-Val-
Cys-Tyr-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-
tBuGly-Cys-Thr-DDab-Dab-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Thr-DDab-Dab-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Ser-DDab-Dab-);
cyclo(-Val-Cys-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-NMeAla-Pro-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Tyr-DDab-Arg-);
cyclo(-Ile-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-DDab-Arg-);
cyclo(-Ile-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-DDab-Ala-);
cyclo(-Ile-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-DDab-Pro-);
cyclo(-Val-Cys-Tyr-Dab-Dap-Dab-Dab-Trp-Dab-
tBuGly-Cys-Thr-DTyr-Pro-);
cyclo(-Ile-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Cys-Ser-DAla-Tyr-);
cyclo(-Leu-Cys-Tyr-Ala-Orn-DDab-Dab-Trp-Ala-Tyr-
Cys-Tyr-DDab-Arg-);
cyclo(-Leu-Cys-Val-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Ala-Orn-DDab-Dab-Phe-Ala-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Val-Val-Orn-DDab-Dab-Trp-Tyr-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Val-Orn-DDab-Dab-Trp-Tyr-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Val-Orn-DDab-Dab-Trp-Tyr-Tyr-
Cys-Tyr-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Ala-Orn-DDab-Dab-Trp-Ala-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Phe-Cys-Val-Thr-Orn-DDab-Dab-Trp-Thr-Tyr-
Cys-Dab-DDab-Arg-);
cyclo(-Leu-Cys-Val-Thr-Orn-DDab-Dab-Trp-Thr-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Dab-);
cyclo(-Leu-Cys-Tyr-Ser-Orn-DDab-Dab-Trp-Asn-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Asn-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Asn-Tyr-
Cys-Val-DDab-Dab-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-Dab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Dab-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Val-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Cpa-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Cpg-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Nva-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Abu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Gln-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Leu-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-tBuGly-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DLys-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DArg-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Lys-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Dap-);
cyclo(-Val-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Leu-DDab-Arg-);
cyclo(-Ile-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Ala-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Dap-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Val-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Dab-Orn-DDab-Dab-Trp-Asn-Tyr-
Cys-Val-DAla-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-Tyr-
Cys-Thr-DDab-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Dab-Tyr-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Asn-Orn-DDab-Dab-Trp-Dab-Tyr-
Cys-Val-DAla-Arg-);
cyclo(-Leu-Pen-tBuGly-Dab-Orn-DDab-Dab-Trp-Dab-
Chg-Pen-Ser-DPro-Pro-);
cyclo(-Leu-Dab-Tyr-Dab-Dab-Dab-Dab-Trp-Dab-
tBuGly-Asp-Ser-DAla-Pro-);
cyclo(-Val-Dab-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Asp-Ser-DAla-Pro-);
cyclo(-Val-Dab-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-Val-
Asp-Thr-DAla-Pro-);
cyclo(-Val-Dab-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Asp-Thr-DThr-Pro-);
cyclo(-Val-Dab-Tyr-Dab-Dab-DDab-Dab-Trp-Dab-
tBuGly-Asp-Ser-DAla-Ala-);
cyclo(-Val-Dab-Tyr-Dab-Dap-DDab-Dab-Trp-Dap-
tBuGly-Asp-Ser-DAla-Tyr-);
cyclo(-Val-Dab-Tyr-Dab-Dab-Dab-Dab-Trp-Dab-
tBuGly-Asp-Ser-Sar-Pro-);
cyclo(-Leu-Asp-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-
tBuGly-Dab-Thr-DDab-Arg-);
cyclo(-Leu-Asp-Tyr-Asn-Orn-DDab-Dab-Trp-Ser-
tBuGly-Dab-Thr-DDab-Dab-);
cyclo(-Leu-Asp-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-Tyr-
Dab-Ser-DAla-Pro-);
cyclo(-Val-Pra-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Abu(4N3)-Ser-DPro-Pro-);
or a pharmaceutically acceptable salt thereof;
and/or
the group consisting of β-hairpin peptidomimetics of general formula (I) having a disulfide linkage; or a lactam linkage between P4 and P9; or disulfide linkages between P2 and P11, and P4 and P9:
cyclo(-Leu-Thr-Tyr-Cys-Dab-Dab-Dab-Trp-Cys-Val-
Thr-Val-DPro-Arg-);
cyclo(-Leu-Thr-Tyr-Cys-Dab-DDab-Dab-Trp-Cys-Val-
Thr-Val-DPro-Arg-);
cyclo(-Leu-Thr-Tyr-Cys-Dab-DDab-Dab-Trp-Cys-Val-
Thr-Val-DPro-Dab-);
cyclo(-Leu-Ser-Tyr-Cys-Orn-DDab-Dab-Trp-Cys-Tyr-
Ala-Ser-DDab-Dab-);
cyclo(-Leu-Ser-Tyr-Cys-Orn-DDab-Dab-Phe-Cys-Val-
Ser-Val-DDab-Arg-);
cyclo(-Leu-Ser-Tyr-Cys-Orn-Gly-Dab-Trp-Cys-Val-
Ala-Val-DDab-Arg-);
cyclo(-Leu-Tyr-Tyr-Dab-Orn-DDab-Dab-Trp-Asp-
tBuGly-Val-Ser-DDab-Pro-);
cyclo(-Leu-Cys-Tyr-Cys-Dab-Dab-Dab-Trp-Cys-Tyr-
Cys-Val-DPro-Arg-);
cyclo(-Leu-Cys-Tyr-Cys-Dab-DDab-Dab-Trp-Cys-Tyr-
Cys-Val-DPro-Arg-);
or a pharmaceutically acceptable salt thereof;
and/or
the group consisting of β-hairpin peptidomimetics of general formula (I)
cyclo(-Val-Ser-Tyr-Dab-Dap-DDab-Dab-Trp-
Dab-tBuGly-Ala-Ser-DPro-NMeAla-);
cyclo(-Val-Dap-Tyr-Dab-Dap-DDab-Dab-Trp-Dab-
tBuGly-Ser-Thr-DAla-Pro-);
cyclo(-Val-Dap-Tyr-Dab-Dab-DDab-Dab-Trp-Dab-
tBuGly-Ser-Thr-DAla-Pro-);
cyclo(-Ile-Thr-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DPro-Tyr-);
cyclo(-Ile-Thr-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DDab-Pro-);
cyclo(-Ile-Thr-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DAla-Tyr-);
cyclo(-Phe-Dap-Tyr-Dab-Orn-DDab-Dab-Trp-Dab-
tBuGly-Ala-Ser-DDab-Pro-);
or a pharmaceutically acceptable salt thereof;
wherein said composition contains said compound of the general formula (I) or a mixture of compounds of general formula (I) and at least one pharmaceutically inert carrier.