The Administrators of the Tulane Educational Fund

Mcgill University

Simon J Hocart

David H Coy

Cyril Y Bowers

Gloria S Tannenbaum

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.

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

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.

Ghrelin/growth hormone releasing peptide/growth hormone secretatogue receptor antagonists and uses thereof

This invention features a method for the solid phase synthesis of non-peptide bonds (CH.sub.2 --NH) in polypeptide chains. These polypeptides ae synthesized by standard procedures and the non-peptide bond synthesized by reacting an amino aldehyde and an amino acid in the presence of NaCNBH.sub.3. This invention also features somatostatin analogs with non-peptide bonds. This invention further features a solid phase method of chemically modifying a peptide. The method involves synthesizing .alpha.-N-R and side group N-R analogs of peptides, where R is an alkyl or aryl group, by reacting a carbonyl-containing compound and an amino acid in the presence of NaCNBH.sub.3.

Method for synthesizing a peptide containing a non-peptide bond

This invention features a method for the solid phase synthesis of non-peptide bonds (CH.sub.2 --NH) in polypeptide chains. These polypeptides are synthesized by standard procedures and the non-peptide bond synthesized by reacting an amino aldehyde and an amino acid in the presence of NaCNBH.sub.3. This invention also features somatostatin analogs with non-peptide bonds. This invention further features a solid phase method of chemically modifying a peptide. The method involves synthesizing .alpha.-N-R and side group N-R analogs of peptides, where R is a an alkyl or aryl group, by reacting a carbonyl-containing compound and an amino acid in the presence of NaCNBH.sub.3.

This invention features a method for the solid phase synthesis of non-peptide bonds (CH.sub.2 --NH) in polypeptide chains. These polypeptides are synthesized by standard procedures and the non-peptide bond synthesized by reacting an amino aldehyde and an amino acid in the presence of NaCNBH.sub.3. This invention also features somatostatin analogs with non-peptide bonds. This invention further features a solid phase method of chemically modifying a peptide. The method involves synthesizing .alpha.-N-R and side group N-R analogs of peptides, where R is an alkyl or aryl group, by reacting a carbonyl-containing compound and an amino acid in the presence of NaCNBH.sub.3.

Growing community of inventors

New Orleans, LA, United States of America

Simon J Hocart