The Administrators of the Tulane Educational Fund

Mcgill University

Gloria S Tannenbaum

David H Coy

Cyril Y Bowers

Simon J Hocart

The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A-A-A-Gly-Ser-A-Phe-Leu-A-A-A-A, wherein each of A, A, and Ais independently absent, an amino acid, or an amino protecting group; each of A, A, A, and Ais independently absent or an amino acid; and Ais a serine conjugated with a &#x2014;C(O)C-Calky or a diaminopropionic acid conjugated with a &#x2014;C(O)C-Calkyl group, provided that at least one of A, A, or Ais present.

Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof

The present invention provides novel peptides that can modulate the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and sub-types, isoforms and variants thereof). These peptides are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities 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, diabetes, central nervous system disorders, genetic disorders, and hyperpro-liferative disorders.

Growth hormone secretatogue receptor antagonists and uses thereof

The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A-A-A-Gly-Ser-A-Phe-Leu-A-A-A-A(SEQ ID NO: 93), wherein each of A, A, and Ais independently absent, an amino acid, or an amino protecting group; each of A, A, A, and Ais independently absent or an amino acid; and Ais a serine conjugated with a &#x2014;(O)C-Calky or a diaminopropionic acid conjugated with a &#x2014;C(O)C-Calkyl group, provided that at least one of A, A, or Ais present.

The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities 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, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.

Growing community of inventors

Hampstead, Canada

Gloria S Tannenbaum