发明授权
- 专利标题: Peptides with para-substituted phenylalanine
- 专利标题(中): 具有对位取代苯丙氨酸的肽
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申请号: US967505申请日: 1978-12-07
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公开(公告)号: US4211693A公开(公告)日: 1980-07-08
- 发明人: Jean E. F. Rivier , Marvin R. Brown , Wylie W. Vale, Jr.
- 申请人: Jean E. F. Rivier , Marvin R. Brown , 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 ; C07K14/655 ; C07C103/52 ; A61K37/00
摘要:
Somatostatin peptides are modified by substitution of para-methoxylated Phe or para-halogenated Phe for any Phe in the peptide. The modified somatostatin peptide analogs have the formulae: ##STR1## wherein R is hydrogen or an acyl group; R.sub.1 is selected from the group consisting of Lys or Des R.sub.1 ; R.sub.2 is selected from the group consisting of Asn, Ala or Des R.sub.2. The amino acids of the R.sub.2 group can be either the L-form or the D-form; R.sub.3 is selected from the group consisting of Trp or D-Trp; R.sub.4 is selected from the group consisting of Thr or Des R.sub.4 ; R.sub.5 is selected from the group consisting of Ser, D-Ser, Phe, X or Des R.sub.5 ; and X is selected from the group consisting of Phe, para-halogenated Phe and para-methoxylated Phe. Provided that at least one X is either para-halogenated Phe or para-methoxylated Phe.
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