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Gnrh antagonist peptide, pharmaceutical composition to inhibit gonadotropin secretion in mammals, processes for in vivo or in vitro diagnosis of a condition where gnrh is causing excess tumor growth or hormonal secretion and to inhibit gonadotropin secretion in mammals, and, intermediate to make a gnrh antagonist peptide.
Gnrh antagonist peptide, pharmaceutical composition to inhibit gonadotropin secretion in mammals, processes for in vivo or in vitro diagnosis of a condition where gnrh is causing excess tumor growth or hormonal secretion and to inhibit gonadotropin secretion in mammals, and, intermediate to make a gnrh antagonist peptide.
"GNRH ANTAGONIST PEPTIDE, PHARMACEUTICAL COMPOSITION TO INHIBIT THE SECRETATION OF GONADOTROPINS IN MAMMALS, PROCESSES FOR IN VIVO DIAGNOSIS OR IN VITRO OF A CONDITION WHERE GNRH IS CAUSING HUMOROUS HUMOROUS CONDITION. , AND, INTERMEDIATE TO MAKE A PEPTIDE ANTAGONIST OF GNRH ". Peptides are provided that have improved duration of antagonistic properties of GnRH. These antagonists can be used to regulate fertility and to treat steroid-dependent tumors, and for other short-term and long-term treatment indications. These antagonists have an aminoPhe derivative or its equivalent in positions 5- or 6-. This derivative is modified to contain a carbamoyl or heterocycle group, including a portion of urea in its side chain. The particularly effective decapeptides, which continue to demonstrate very substantial suppression of LH secretion 96 hours after injection, in the formula: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph (L-hydroorotil) -D- 4Aph (acetyl) -Leu-Lys (isopropyl) -Pro-D-Ala-NH ~ 2 ~, and Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph (L-hydroorotyl) -D-4Amf (Q ~ 2 ~) -Leu-Lys (isopropyl) -Pro-Xaa ~ 10 ~, where Q ~ 2 ~ is Cbm or MeCbm and Xaa ~ 10 ~ is D-Ala-NH ~ 2 ~, D-Ala- ol or Ala-ol.
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