发明授权
- 专利标题: GnRH analogs
- 专利标题(中): GnRH类似物
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申请号: US6729申请日: 1993-01-21
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公开(公告)号: US5296468A公开(公告)日: 1994-03-22
- 发明人: Carl A. Hoeger , Jean E. F. Rivier , Paula G. Theobald , John S. Porter , Catherine L. Rivier , Wylie W. Vale, Jr.
- 申请人: Carl A. Hoeger , Jean E. F. Rivier , Paula G. Theobald , John S. Porter , 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: A61K38/00
- IPC分类号: A61K38/00 ; C07C279/24 ; C07C279/28 ; C07C313/30 ; C07D249/14 ; C07K7/02 ; C07K7/23 ; A61K37/38 ; C07K7/06 ; C07K7/20
摘要:
Peptides which include unnatural amino acids and which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The antagonists may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions. Such unnatural amino acids are useful in the synthesis of peptides and have the formula U.sup.* : ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; and j=1, 2 or 3. Preferably, either Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pridyl or ##STR3## where R.sub.11 is H or acyl.
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