LONG-ACTING GONADOTROPIN-RELEASING HORMONE ANALOGS AND METHODS OF USE THEREOF

摘要

The present invention relates to the design, synthesis and biologicalevaluation of potent long-acting gonadotropin-releasing hormone (GnRH) analogsincluding agonists and antagonists comprising a GnRH peptide conjugated toemodic acid or an emodic acid derivative. These long acting analogs bind toGnRH receptors with high affinity and are devoid of any toxicity orantiproliferative effects. The present invention further relates totherapeutic uses of these GnRH analogs as contraceptives, in controllingfertility, and in treating and/or preventing sex-hormone dependent diseases orconditions.