发明授权
- 专利标题: GNRH antagonists XIII
- 专利标题(中): GNRH拮抗剂十三
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申请号: US210627申请日: 1994-03-18
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公开(公告)号: US5506207A公开(公告)日: 1996-04-09
- 发明人: Jean E. F. Rivier , John S. Porter , Carl A. Hoeger , Guangcheng Jiang , Catherine L. Rivier
- 申请人: Jean E. F. Rivier , John S. Porter , Carl A. Hoeger , Guangcheng Jiang , Catherine L. Rivier
- 申请人地址: CA San Diego
- 专利权人: The Salk Institute for Biological Studies
- 当前专利权人: The Salk Institute for Biological Studies
- 当前专利权人地址: CA San Diego
- 主分类号: A61K38/00
- IPC分类号: A61K38/00 ; A61P13/02 ; A61P15/00 ; A61P29/00 ; A61P31/12 ; A61P35/00 ; A61P37/04 ; C07K7/06 ; C07K7/23 ; A61K38/04 ; C07K7/00
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-.beta.-D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(Q.sub.1)(3-amino-1,2,4 triazole)-D-Aph(Q.sub.2)(3-amino 1,2,4-triazole)-Leu-Lys (isopropyl)-Pro-D-Ala-NH.sub.2,where Q.sub.1 and Q.sub.2 are amino acids, such as Gly, .beta.-Ala, Ala, D-Ala, Ser, Aib, Ahx and Gab. Examples of other GnRH antagonists includeAc-.beta.-D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(Atz)-D-Aph(Ac)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub.2,Ac-.beta.-D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(.beta.-Ala)(3-amino-1,2,4 triazole)-D-Aph(.beta.-Ala)(3-amino-1,2,4 triazole)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub.2,Ac-.beta.-D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(Ac-D-Ser)-D-Aph(Ac-D-Ser)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub.2, andAc-.beta.-D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(Ac)-D-Aph(Ac)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub.2.
公开/授权文献
- US6163124A Robot controller 公开/授权日:2000-12-19
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