Polyphor Ltd.

Unversität Zürich

Universitaet Zuerich

Polyphor Ag

Other

Frank Gombert

Daniel Obrecht

Christian Ludin

Steven J Demarco

Barbara Romagnoli

Jan Wim Vrijbloed

Heiko Henze

Kerstin Moehle

Reshmi Mukherjee

John Anthony Robinson

John-Anthony Robinson

Alexander Lederer

Nityakalyani Srinivas

Ricardo Dias

Wim Vrijbloed

Françoise Jung

Sergio Lociuro

Jürg Zumbrunn

Francoise Jung

Sergio Locurio

Christian Bisang

Odile Sellier

Johann Zimmermann

Odile Sellier-Kessler

Kerstin Möhle

Ralf Löwe

Kalpana Patel

Steve J DeMarco

Shivaprasad Shankaramma

Steven J DeMarco

Juerg Zumbrunn

Reshimi Mukherjee

Steve J Demarco

Steven J De Marco

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

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

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

The template-fixed &#x3b2;-hairpin peptidomimetics Cyclo(-Tyr-His-Cys-Ser-Ala-Pro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys--Pro-Pro), disulfide bond between Cys4 and Gysl1, 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 &#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.

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

The template-fixed B-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-Pro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys--Pro-Pro), disulfide bond between Cys4 and Gys11, 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 &#x3b2;-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of&#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 &#x3b2;-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 &#x3b1;-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 CXCR4 antagonizing properties These &#x3b2;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing 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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Huttingen, Germany

Frank Gombert