GnRH antagonists

专利名称：GnRH antagonists

发明人：Graeme Semple,Guangcheng Jiang申请号：US08/837042申请日：19970411公开号：US05925730A公开日：19990720

摘要：Peptides are provided which have improved duration of GnRH antagonisticproperties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. Theseantagonists 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 sidechain. Particularly effective decapeptides, which continue to exhibit very substantialsuppression 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-NH.sub.2, and Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(hydroorotyl)-D-4Amf(Q.sub.2)-Leu- Lys(isopropyl)-Pro-D-Ala-NH.sub.2, wherein Q.sub.2 is Cbm or MeCbm.

申请人：FERRING BV

代理机构：Fitch, Even, Tabin & Flannery

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