Tranzyme Pharma Inc.

Ocera Therapeutics, Inc.

Sylvie Beaubien

Hamid R Hoveyda

Mark L Peterson

Luc Ouellet

Kamel Benakli

Éric Marsault

Graeme Lovat Fraser

Mahesh Ramaseshan

Yves Dory

Sophie Beauchemin

Pierre Deslongchamps

Carl St-Louis

Gérald Villeneuve

Daniel Fortin

Eric Marsault

Ruoxi Lan

Shigui Li

Hamid Hoveyda

Robert Deziel

Luc Oullet

Martin Vezina

Robert Dèziel

Martin Vézina

Gerald Villeneuve

Graeme Fraser

The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R, R, R, R, R, R, n, m, p Z, Z, and Zare as described in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

Intermediates for macrocyclic compounds

The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R, R, R, R, R, R, n, m, p Z, Z, and Zare as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

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.

Spatially-defined macrocycles incorporating peptide bond surrogates

Processes for intermediates for macrocyclic compounds

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.

Spatially-defined macrocyclic compounds useful for drug discovery

Macrocyclic antagonists of the motilin receptor

Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists

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Sherbrooke, Canada

Sylvie Beaubien