Polyphor AG
Backbone-cyclized peptidomimetics with GLP-1R modulating activity

Abstract:

Novel backbone-cyclized peptidomimetics of the general formula cyclo[-P.sup.1-P.sup.2-P.sup.3-P.sup.4-P.sup.5-P.sup.6-P.sup.7-P.sup.8-T.- sup.1-T.sup.2-] (I) wherein the single elements T or P are .alpha.-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--and solution phase synthetic strategy.