Ocera Therapeutics, Inc.

Luc Oullet

Hamid R Hoveyda

Eric Marsault

Mark L Peterson

Kamel Benakli

Sophie Beauchemin

Graeme Lovat Fraser

Sylvie Beaubien

Carl St-Louis

Zhigang Wang

Martin Brassard

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.

Intermediates for macrocyclic compounds

Growing community of inventors

Sherbrooke, Canada

Luc Oullet