Polyphor Ag

Spexis Ag

Francesca Bernardini

Daniel Obrecht

Anatol Luther

Peter Zbinden

Alexander Lederer

Glenn E Dale

Sophie Barthélémy

Grégory Upert

Emile Brabet

Nicolas Desjonqueres

Gildas Deniau

Beta-hairpin peptidomimetics of the general formula (I), cyclo[P-P-P-P-P-P-P-P-P-P-P-P-T-T], and pharmaceutically acceptable salts thereof, with Pto P, Tand Tbeing 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 asand/orand/or 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.

Beta-hairpin peptidomimetics

Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, X, Q., and optionally L 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 asand/orand/orand/orand/or. 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.

Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, T, Q, and optionally L 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 asand/orand/orand/or 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.

Beta-hairpin peptidomimetics of the general formula (I), cyclo[P-P-P-P-P-P-P-P-P-P-P-P-T-T] and pharmaceutically acceptable salts thereof, with Pto P, Tand Tbeing elements as defined in the description and the claims, have Gramnegative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such asand/orand/or. 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.

&#x3b2;-hairpin peptidomimetics

Beta-hairpin peptidomimetics of the general formula (I), cyclo[P-P-P-P-P-P-P-P-P-P-P-P-T-T], and pharmaceutically acceptable salts thereof, with Pto P, Tand Tbeing 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 asand/orand/or. 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.

Beta-hairpin peptidomimetics of the general formula (I), cyclo[P&#x2014;P&#x2014;P&#x2014;P&#x2014;P&#x2014;P&#x2014;P&#x2014;P&#x2014;P&#x2014;P&#x2014;P&#x2014;P-T-T], and pharmaceutically acceptable salts thereof, with Pto P, Tand Tbeing elements as defined in the description and the claims, have broad spectrum Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such asand/orand/or 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.

Beta-hairpin peptidomimetics of the general formula (I), cyclo[P-p-p-p-p-p-p-p-p-p-p-p-T-T], and pharmaceutically acceptable salts thereof, with Pto P, Tand Tbeing 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 asand/orand/or. 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.

Beta-hairpin peptidomimetics of the general formula (I), cyclo(P-p-p-p-p-p-ppp-p-p-p-T-T], and pharmaceutically acceptable salts thereof, with Pto P, Tand Tbeing elements as defined in the description and the claims, have broad spectrum Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such asand/orand/or. 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.

A novel combination comprising a &#x3b2;-hairpin peptidomimetic of the formula cyclo(-Thr-Trp-Ile-Dab-Orn-Dab-Dab-Trp-Dab-Dab-Ala-Ser-Pro-Pro) (I), and a further compound with antibiotic activity, that enable therapeutic control of specific bacterial infections in human or animals at doses of the individual compounds lower than either of the compounds administered alone. The combination can be used as a medicament to treat e.g. skin or soft tissue infections; eye, ear, blood stream, or intra-abdominal infections; infections related to respiratory diseases, to bone diseases, to cardiovascular diseases, to genitourinal diseases, or to gastrointestinal diseases.

Combinations with a backbone-cyclized peptide

A novel combination comprising a &#x3b2;-hairpin peptidomimetic of the formula cyclo(-Thr-Trp-Ile-Dab-Orn-Dab-Dab-Trp-Dab-Dab-Ala-Ser-Pro-Pro) (I), and a compound of the glycylcycline class, especially tigecycline, that enable therapeutic control of specific bacterial infections in human or animals at doses of the individual compounds lower than either of the compounds administered alone. The combination can be used as a medicament to treat e.g. skin or soft tissue infections; eye, ear, blood stream, or intra-abdominal infections; infections related to respiratory diseases, to bone diseases, to cardiovascular diseases, to genitourinal diseases, or to gastrointestinal diseases.

Growing community of inventors

Hésingue, France

Francesca Bernardini