Spatially-defined macrocycles incorporating peptide bond...

Details Spatially-defined macrocycles incorporating peptide bond... Spatially-defined macrocycles incorporating peptide bond...

C - Chemistry, Metallurgy

07

K

C07K 5/00 (2006.01) C07K 1/04 (2006.01) C07K 5/08 (2006.01)

Patent

CA 2533820

Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.

L'invention concerne des nouveaux composés macrocycliques définis spatialement incorporant des substituts de liaison peptidique. Des bibliothèques desdits macrocycles sont ensuite utilisées pour sélectionner une ou plusieurs espèces de macrocycles présentant une interaction spécifique avec une cible biologique particulière. En particulier, les composés de l'invention sont des agonistes ou des antagonistes d'un récepteur de la motiline humaine et un récepteur de la ghréline humaine.

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