Polyphor Ag

Polyphor Ltd.

Unversität Zürich

Universitaet Zuerich

Janssen Pharmaceutica Nv

Other

Takeda Pharmaceutical Company Limited

University of Zürich

Spexis Ag

Daniel Obrecht

Frank Gombert

Christian Ludin

Barbara Romagnoli

Steven J Demarco

Alexander Lederer

John Anthony Robinson

Anatol Luther

Jan Wim Vrijbloed

Kerstin Moehle

Heiko Henze

Reshmi Mukherjee

Frank Otto Gombert

Francesca Bernardini

Philipp Ermert

Christian Bisang

Johann Zimmermann

Peter Zbinden

John-Anthony Robinson

Françoise Jung

Wim Vrijbloed

Ricardo Dias

Nityakalyani Srinivas

Jürg Zumbrunn

Lieven Meerpoel

Gustaaf Maria Boeckx

Christophe Francis Robert Nestor Buyck

Guy Rosalia Eugeen Van Lommen

Jean-Pierre André Marc Bongartz

Sergio Lociuro

Sergio Locurio

Odile Sellier-Kessler

Sophie Barthélémy

Odile Sellier

Francoise Jung

Glenn E Dale

Said Oumouch

Ralf Löwe

Steffen Weinbrenner

Eric Chevalier

Kerstin Möhle

Christian Oefner

Steve J DeMarco

Guillaume Lemercier

Franck Lach

Karsten Marx

Martin Eberle

Felix Bachmann

Marc Thommen

Alessandro Strebel

Kalpana Patel

Jurg Zumbrunn

Grégory Upert

Gildas Deniau

Nicolas Desjonqueres

Steven J DeMarco

Arnaud Piettre

Jean-François Gosalbes

Christian Steuer

William J Drury, Iii

Krystyna Patora-Komisarska

Anne Descours

Manuella Schmitt-Billet

Emile Brabet

Tobias Remus

Shivaprasad Shankaramma

Ralf Loewe

Frank Lach

Allessandro Strebel

Marc Kessler

Kerstin Mohle

Ralf Lowe

Juerg Zumbrunn

William J Drury Iii

Reshimi Mukherjee

Steve J Demarco

Markus Seitz

Ludovic T Maillard

Roba Mounme

Steven J De Marco

Barbara Romanoli

Alex Lederer

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.

The template-fixed &#x3b2;-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-Pro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-Pro-Pro), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.

Template-fixed peptidomimetics

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.

Novel backbone-cyclized peptidomimetics of the general formulacyclo[-P-P-P-P-P-P-P-P-T-T-]&#x2003;&#x2003; (I)wherein the single elements T or P are &#x3b1;-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to modulate the GLP-1 receptor. They can be used as medicaments to treat, prevent, or delay the onset of diseases, disorders or conditions in which modulation of the human GLP-1 receptor is beneficial, such as type 2 diabetes. These backbone-cyclized peptidomimetics can be manufactured by a process which is based on a mixed solid&#x2014;and solution phase synthetic strategy.

Backbone-cyclized peptidomimetics with GLP-1R modulating activity

Template-fixed &#x3b2;-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 &#x3b1;-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 formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These &#x3b2;-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

Template-fixed peptidomimetics with antimicrobial activity

&#x3b2;-Hairpin peptidomimetics of the general formula cyclo(-Xaa-Xaa-Thr-Xaa-Ser-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-) and pharmaceutically acceptable salts thereof, with Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaaand Xaabeing amino acid residues which are defined in the description and the claims, have elastase inhibitory properties, especially against human neutrophil elastase, and can be used for preventing infections or diseases related to such infections in healthy individuals or for slowing infections in infected patients. The compounds of the invention can further be used where cancer, or immunological diseases, or pulmonary diseases, or cardiovascular diseases, or neurodegenerative diseases, or inflammation, or diseases related to inflammation, are mediated or resulting from elastase activity. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Beta-hairpin peptidomimetics as selective elastase inhibitors

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

Template-fixed &#x3b2;-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 &#x3b1;-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These &#x3b2;-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

Template-fixed beta-hairpin peptidomimetics with protease inhibitory activity

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.

&#x3b2;-Hairpin peptidomimetics of the general formula cyclo(-Tyr-His-Xaa-Cys-Ser-Xaa-Pro-Xaa-Arg-Tyr-Cys-Tyr-Xaa-Xaa-Xaa-Pro-), disulfide bond between Cysand Cys, and pharmaceutically acceptable salts thereof, with Xaa, Xaa, Xaa, Xaa, Xaaand Xaabeing amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

&#x3b2;-Hairpin peptidomimetics of the general formula cyclo(-Xaa-Xaa-Thr-Xaa-Ser-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-) and pharmaceutically acceptable salts thereof, with Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaaand Xaabeing amino acid residues of certain types which are defined in the description and the claims, have elastase inhibitory properties, especially against human neutrophil elastase, and can be used for preventing infections or diseases related to such infections in healthy individuals or for slowing infections in infected patients. The compounds of the invention can further be used where cancer, or immunological diseases, or pulmonary diseases, or cardiovascular diseases, or neurodegenerative diseases, or inflammation, or diseases related to inflammation, are mediated or resulting from elastase activity. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

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Bättwil, Switzerland

Daniel Obrecht