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    GNRH ANTAGONISTS
    2.
    发明公开
    GNRH ANTAGONISTS 失效
    促性腺激素释放激素拮抗剂

    公开(公告)号：EP0804471A1

    公开(公告)日：1997-11-05

    申请号：EP95912043.0

    申请日：1995-03-03

    申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES

    发明人： RIVIER, Jean E.F. ,  PORTER, John S. ,  HOEGER, Carl A. ,  JIANG, Guangcheng ,  RIVIER, Catherine L.

    IPC分类号： A61K38 ,  A61P13 ,  A61P15 ,  A61P29 ,  A61P31 ,  A61P35 ,  A61P37 ,  C07K7

    CPC分类号： C07K7/23 ,  A61K38/00

    摘要： Analogs of the decapeptide GnRH which include two significantly modified amino acids at positions 5 and 6 inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads and may be used to treat steroid-dependent tumors. Particularly effective peptides which are soluble in water at physiologic pH and which have a low tendency to gel when administered in vivo have the following formula: Ac-β-D-2NAL-(4C1)D-Phe-D-3PAL-Ser-Aph(Q1)(3-amino-1,2,4-triazole)-D-Aph(Q2)(3-amino-1,2,4-triazole)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, where Q1 and Q2 are amino acids, such as Gly, β-Ala, Ala, D-Ala, Ser, Aib, Ahx and Gab. Examples of other GnRH antagonists include Ac-β-D-2NAL-(4C1)D-Phe-D-3PAL-Ser-Aph(Atz)-D-Aph(Ac)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, Ac-β-D-2NAL-(4C1)D-Phe-D-3PAL-Ser-Aph(β-Ala)(3-amino-1,2,4-triazole)-D-Aph(β-Ala)(3-amino-1,2,4-triazole)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, Ac-β-D-2NAL-(4C1)D-Phe-D-3PAL-Ser-Aph(Ac-D-Ser)-D-Aph(Ac-D-Ser)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, and Ac-β-D-2NAL-(4C1)D-Phe-D-3PAL-Ser-Aph(Ac)-D-Aph(Ac)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2.