Spatially-defined macrocyclic compounds useful for drug discovery
AssigneeTranzyme Pharma Inc.
InventorsÉric Marsault, Kamel Benakli, Hamid R. Hoveyda, Mark L. Peterson, Sylvie Beaubien, Luc Ouellet, Carl St-Louis, Sophie Beauchemin
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Abstract
Novel spatially-defined macrocyclic compounds containing specific conformational control elements 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.
Claims6
A compound of formula W-T-X, wherein T is selected from the group consisting of
- wherein:
- W is selected from the group consisting of —OH, —NH2 and —NHR3, wherein R3 is lower alkyl and X is —NH2 or —NHR3, wherein R3 is lower alkyl, or X is —OH and W is —NHR3, wherein R3 is lower alkyl;
- Y is hydrogen, alkyl, benzyl or acyl;
- (W) indicates the point of attachment of T to W;
- and (X) indicates the point of attachment of T to X, and
- W, X and/or —OY may be optionally protected by one or more protecting groups.
Dependencies are inferred from the claim text.