Polyphor Ag

Polyphor Ltd.

Unversität Zürich

Odile Sellier-Kessler

Daniel Obrecht

Christian Ludin

Alexander Lederer

Frank Gombert

John Anthony Robinson

Barbara Romagnoli

Heiko Henze

Reshmi Mukherjee

Frank Otto Gombert

Christian Bisang

Francoise Jung

Steffen Weinbrenner

Françoise Jung

Kerstin Möhle

Steve J DeMarco

Manuella Schmitt-Billet

Markus Seitz

Ludovic T Maillard

Roba Mounme

Steve J Demarco

Barbara Romanoli

Alex Lederer

&#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

&#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.

Template-fixed &#x3b2;-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 4 &#x3b1;-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, 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 agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory diseases, haematological diseases and cancer. These &#x3b2;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Template-fixed peptidomimetics

Template-fixed &#x3b2;-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 4 &#x3b1;-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, 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 agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory diseases, haematological diseases and cancer. These &#x3b2;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy. 

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Baldersheim, France

Odile Sellier-Kessler