GnRH antagonists

US5925730A · kind A · utility

Assignee

• Ferring B.V. · NL

Inventors

• Graeme Semple · Mölndal, SE
• Guangcheng Jiang · Village of La Jolla, US

Key dates

• Filing date: Apr 11, 1997
• Grant date: Jul 20, 1999
• Expiry date: Apr 11, 2017

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/11
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Peptides are provided which have improved duration of GnRH antagonistic properties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. These antagonists have a derivative of aminoPhe or its equivalent in the 5- and/or 6-positions. This derivative contains a carbamoyl group or a heterocycle including a urea in its side chain. Particularly effective decapeptides, which continue to exhibit very substantial suppression of LH secretion at 96 hours following injection, have the formulae: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(hydroorotyl)-D-4Aph(acetyl)-Leu-Lys(isopr opyl)-Pro-D-Ala-NH.sub.2, and Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(hydroorotyl)-D-4Amf(Q.sub.2)-Leu-Lys(isop ropyl)-Pro-D-Ala-NH.sub.2, wherein Q.sub.2 is Cbm or MeCbm.