Polyphor Ag

Ralf Löwe

Daniel Obrecht

Johann Zimmermann

Frank Gombert

Barbara Romagnoli

Alexander Lederer

Frank Otto Gombert

Kalpana Patel

Françoise Jung

Eric Chevalier

Guillaume Lemercier

Novel template-fixed &#x3b2;-hairpin peptidomimetics of the general formula (I): cyclo[P-P-P-P-P-P-P-P-P-P-P-P-P-P-T-T] 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 of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions, immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. 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 as inhibitors of FPR1

Novel template-fixed &#x3b2;-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are &#x3b1;-amino acid residues connected from the carbonyl (C&#x2550;O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these &#x3b2;-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells.

Template-fixed peptidomimetics with CXCR7 modulating activity

Novel template-fixed &#x3b2;-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are &#x3b1;-amino acid residues connected from the carbonyl (C&#x2550;O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these &#x3b2;-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells. 

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Arlesheim, Switzerland

Ralf Löwe