GnRH ANTAGONISTS BEING MODIFIED IN POSITIONS 5 AND 6
作者： Graeme Semple , Guangcheng Jiang , Jean E. F. Rivier
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摘要: Peptides are provided which have improved duration of GnRH antagonistic properties. These antagonists may be used to regulate fertility and treat steroid-dependent tumors for other short-term long-term treatment indications. a derivative aminoPhe or its equivalent in the 5- 6- positions. This is modified so as contain carbamoyl group heterocycle, including urea moiety side chain. Particularly effective decapeptides, continue exhibit very substantial suppression LH secretion at 96 hours following injection, formulae: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-hydroorotyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-hydroorotyl)-D-4Amf(Q2)-Leu-Lys(isopropyl)-Pro-Xaa10, wherein Q2 Cbm MeCbm Xaa10 D-Ala-NH2, D-Ala-ol Ala-ol.
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