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    • 5. 发明授权
    • Cyclooctapeptides
    • 环肽
    • US4358439A
    • 1982-11-09
    • US216353
    • 1980-12-15
    • Peter SieberBruno KamberHans Rink
    • Peter SieberBruno KamberHans Rink
    • C07K7/56A61K38/00A61K38/04A61P5/00A61P5/02C07K1/113C07K14/575C07K14/655A61K37/00C07C103/52
    • C07K14/6555A61K38/00Y10S514/806Y10S930/16
    • Cyclic peptides of the formula ##STR1## in which trp represents L-Trp, D-Trp, or an analogous radical which carries a halogen atom in the indole nucleus, Ac.sub.A represents hydrogen, or an acyl radical Ac of a carboxylic acid present at the .epsilon.-amino group, A represents L-Phe, D-Phe, L-Phg or D-Phg, or a corresponding radical having a substituted or saturated phenyl ring, and B represents the residue of a .gamma.- or .delta.-amino-lower alkanecarboxylic acid which may carry an optionally substituted cyclic hydrocarbyl radical Ar, and also pharmacologically tolerable salts and therapeutically acceptable complexes thereof can be used as an antidiabetic in an analogous manner to somatostatin. They can be obtained by conventional processes of peptide chemistry, especially by cyclisation of corresponding linear peptides.
    • 其中trp表示L-Trp,D-Trp或在吲哚核中携带卤素原子的类似基团的式(I)的环肽,AcA表示氢或羧酸的酰基Ac 存在于ε-氨基,A表示L-Phe,D-Phe,L-Phg或D-Phg或具有取代或饱和的苯环的相应基团,B表示γ或δ- 可以携带任选取代的环状烃基Ar的氨基 - 低级链烷羧酸,以及其药理学上可耐受的盐和其可治疗可接受的复合物可以以与生长抑素类似的方式用作抗糖尿病剂。 它们可以通过肽化学的常规方法获得,特别是通过相应的线性肽的环化获得。