发明授权
US06214798B1 GnRH antagonists being modified in positions 5 and 6 有权
GnRH拮抗剂在5和6位修饰

  • 专利标题: GnRH antagonists being modified in positions 5 and 6
  • 专利标题(中): GnRH拮抗剂在5和6位修饰
  • 申请号: US09402698
    申请日: 2000-01-03
  • 公开(公告)号: US06214798B1
    公开(公告)日: 2001-04-10
  • 发明人: Graeme SempleGuangcheng Jiang
  • 申请人: Graeme SempleGuangcheng Jiang
  • 主分类号: A61K3800
  • IPC分类号: A61K3800
GnRH antagonists being modified in positions 5 and 6
摘要:
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- or the 5- and 6-positions. This derivative is modified so as to contain a carbamoyl group or heterocycle, including a urea moiety, in its side chain. Decapeptides having the formula: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-hydroorotyl)-D-4Amf(Q2)-Leu-Lys(isopropyl)-Pro-Xaa10, wherein Q2 is Cbm or MeCbm and Xaa10 is D-Ala-ol or Ala-ol are particularly effective and continue to exhibit very substantial suppression of LH secretion at 96 hours following injection.
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