发明授权
- 专利标题: GnRH antagonists IX
- 专利标题(中): GnRH拮抗剂IX
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申请号: US732531申请日: 1985-05-09
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公开(公告)号: US4661472A公开(公告)日: 1987-04-28
- 发明人: Jean E. F. Rivier , Janos I. Varga , Arnold T. Hagler , R. Scott Struthers , Marilyn H. Perrin , Catherine L. Rivier , Wylie W. Vale, Jr.
- 申请人: Jean E. F. Rivier , Janos I. Varga , Arnold T. Hagler , R. Scott Struthers , Marilyn H. Perrin , Catherine L. Rivier , Wylie W. Vale, Jr.
- 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: A61K38/04
- IPC分类号: A61K38/04 ; A61K38/00 ; A61K38/22 ; A61K38/27 ; A61P5/00 ; C07K7/06 ; C07K7/23 ; C07K14/00 ; C07K14/575 ; A61K37/43
摘要:
Peptides which 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. These peptides may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are cyclic analogs of the decapeptide GnRH wherein there is a covalent bond between the residue in the 4-position and the residue in the 10-position. Examples of such bonds include the disulfide linkage between Cys residues, an amide linkage between a side chain amino group and a side chain carboxyl group, a dicarba linkage between side-chain alkyl groups, and a carba linkage between a side-chain alkyl group and a side-chain sulfhydryl group.
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