| 摘要 |
<p><P>PROBLEM TO BE SOLVED: To provide a peptide which has improved duration of GnRH (gonadotropin-releasing hormone) antagonistic properties. <P>SOLUTION: 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 a heterocycle including an urea moiety in its side chain. Especially effective decapeptides have formula: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-hydroorotyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH<SB>2</SB>, and Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-hydroorotyl)-D-4Amf(Q<SB>2</SB>)-Leu-Lys(isopropyl)-Pro-Xaa<SB>10</SB>, wherein Q<SB>2</SB>is Cbm or MeCbm, and Xaa<SB>10</SB>is D-Ala-NH<SB>2</SB>, D-Ala-ol or Ala-ol. <P>COPYRIGHT: (C)2005,JPO&NCIPI</p> |
