Allergan, Inc.

Ocera Therapeutics, Inc.

Tranzyme Pharma Inc.

Sophie Beauchemin

Hamid R Hoveyda

Mark L Peterson

Kamel Benakli

Robert M Burk

Sylvie Beaubien

Carl St-Louis

Eric Marsault

Luc Ouellet

Éric Marsault

Luc Oullet

Graeme Lovat Fraser

Zhigang Wang

Luc Quellet

Martin Brassard

David Drutz

Hamid Hoveyda

Kamel Benkali

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 provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

Macrocyclic ghrelin receptor modulators and methods of using the same

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.

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

According to the invention there is provided a compound the formula I; wherein A, X, B, R, R, Rand Rare as defined in the specification.

Arylsulfanyl and heteroarylsulfanyl derivatives for treating pain

According to the invention there is provided a compound the formula I; 

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Sherbrooke, Canada

Sophie Beauchemin