SHORT CHAIN PEPTIDOMIMETICS BASED ORALLY ACTIVE GLP-1 AGONIST AND GLUCAGON RECEPTOR ANTAGONIST

摘要

The present invention provides novel short chain peptidomimetics, which act as GLP-1 receptors agonist and glucagon receptor antagonist. These dual acting peptidomimetics exhibit increased stability to proteolytic cleavage, especially against DPP-IV (Dipeptidyl peptidase-IV) enzyme, GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, these short chain peptidomimetics can be delivered by oral routes of administration, for the treatment or prevention of diabetes and related metabolic disorders, such as obesity, hyperlipidemia and eating disorders.