发明公开
- 专利标题: LH- RH Antagonists
- 专利标题(中): LH / RH-Antagonisten。
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申请号: EP84201146.2申请日: 1984-08-06
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公开(公告)号: EP0145032A1公开(公告)日: 1985-06-19
- 发明人: Loozen, Hubert Jan Josef, Dr.
- 申请人: AKZO N.V.
- 申请人地址: Velperweg 76 NL-6824 BM Arnhem NL
- 专利权人: AKZO N.V.
- 当前专利权人: AKZO N.V.
- 当前专利权人地址: Velperweg 76 NL-6824 BM Arnhem NL
- 代理机构: Hermans, Franciscus G.M.
- 优先权: NL8302875 19830816; NL8400153 19840118
- 主分类号: C07K7/06
- IPC分类号: C07K7/06 ; A61K37/02
摘要:
The invention relates to novel peptides and peptide derivatives which act as antagonists of natural LH-RH and have the general formula:
X-R 1 -R 2 -R 3 -Ser-Tyr-R 4 -R 5 -R 6 -R 7 -R 8 -NH 2 wherein
X represents hydrogen or a lower acyl (1-6 C) group,
R' and R 2 represent either the same or different groups selected from D-Bal (2), D-Bal (3), D-Nal (1), D-Nal (2), D-Phe or D-Phe substituted at the phenyl moiety by one or more halogen, alkyl (1-4 C), alkoxy (1- 4 C) or nitro groups; R' represents D-Trp, D-Bal (2), D-Bal (3), D-Nal (1), D- Nal (2) or D-Pal, with the proviso that at least one of the symbols R' or R 3 represents a D-Bal (2) or D-Bal (3) group;
R 4 represents D-Arg, D-Lys, D-homo Arg or D-dialkyl (1-4 C)-homo Arg;
R 5 represents L-Leu, L-Met or the alkyl (1-4C) or phenylalkyl
(7-10C) ether of L-Cys, L-Ser or L-homo Ser;
R 6 represents L-Lys or L-Arg;
R 7 represents L-Pro or L-thiaprolyl, and
R 8 represents D-Ala or Gly.
The invention also includes the acid addition salts of the above defined peptides.
X-R 1 -R 2 -R 3 -Ser-Tyr-R 4 -R 5 -R 6 -R 7 -R 8 -NH 2 wherein
X represents hydrogen or a lower acyl (1-6 C) group,
R' and R 2 represent either the same or different groups selected from D-Bal (2), D-Bal (3), D-Nal (1), D-Nal (2), D-Phe or D-Phe substituted at the phenyl moiety by one or more halogen, alkyl (1-4 C), alkoxy (1- 4 C) or nitro groups; R' represents D-Trp, D-Bal (2), D-Bal (3), D-Nal (1), D- Nal (2) or D-Pal, with the proviso that at least one of the symbols R' or R 3 represents a D-Bal (2) or D-Bal (3) group;
R 4 represents D-Arg, D-Lys, D-homo Arg or D-dialkyl (1-4 C)-homo Arg;
R 5 represents L-Leu, L-Met or the alkyl (1-4C) or phenylalkyl
(7-10C) ether of L-Cys, L-Ser or L-homo Ser;
R 6 represents L-Lys or L-Arg;
R 7 represents L-Pro or L-thiaprolyl, and
R 8 represents D-Ala or Gly.
The invention also includes the acid addition salts of the above defined peptides.
公开/授权文献
- EP0145032B1 LH- RH Antagonists 公开/授权日:1987-11-04
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