GnRH antagonist decapeptides,申请号US19970837041-传众专利搜索

GnRH antagonist decapeptides

申请公布号：US5821230(A)

申请号：US19970837041

申请日期：1997.04.11

申请公布日期：1998.10.13

申请人：

FERRING BV

发明人：JIANG, GUANGCHENG;SEMPLE, GRAEME

分类号：G01N33/74;A61K38/00;A61K38/04;A61P15/00;A61P35/00;A61P43/00;C07K7/23;(IPC1-7):A61K38/09;C07K7/06

主分类号：G01N33/74

摘要：Peptides are provided which have improved duration of GnRH antagonistic properties and/or which can be synthesized more economically. These antagonists may be used in the same manner as the compounds of which they are analogs to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. One particularly effective peptide, a decapeptide analog of the GnRH antagonist Acyline, has the formula: Ac-D-2Nal-D-4Cpa-D-Dpr(methylcarbamoyl)-Ser-4Aph(acetyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2. It continues to exhibit very substantial suppression of LH secretion at 96 hours following injection. Other economically attractive and pharmacologically effective analogs have the formulas: Ac-D-2Nal-D-4Cpa-Xaa3-Ser-4Aph(acetyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2; and Ac-D-2Nal-D-4Cpa-Xaa3-Ser-4Aph(hydroorotyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, wherein Xaa3 is D-Gln or Gln.