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Last Updated: December 12, 2025

Claims for Patent: 5,925,730

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Summary for Patent: 5,925,730

Title:	GnRH antagonists
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(isopropyl)-Pro-D-Ala-NH2, and Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(hydroorotyl)-D-4Amf(Q2)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, wherein Q2 is Cbm or MeCbm.
Inventor(s):	Graeme Semple, Guangcheng Jiang
Assignee:	Ferring BV
Application Number:	US08/837,042
Patent Claims:

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