Preparation of C-amidated peptides, useful as pharmaceuticals, by reaction between precursor peptides in presence of enzyme with activity of trypsin, also new reaction products

摘要

Method for preparing C-terminally amidated di- or poly-basic peptides (I). Method for preparing C-terminally amidated di- or poly-basic peptides of formula (I) comprises reacting peptide (II) and amine (III) in presence of an enzyme (E) with trypsin activity, optionally followed by purification of (I) by methods used in protein chemistry. (AS) n-X m-NH 2 (I) (AS) n-Xp (II) (X) q-NH 2 (III) AS : amino acid, or its analog or derivative; X : basic amino acid or its analog or derivative; n : 3-2000; m : 2-15; p and q : integers and p+q = m . An independent claim is also included for new peptides of formula His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-(Glu) 3-Ala-Val-Arg- Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-Z-NH 2 where Z = LysLys (Seq. (2)); LysArg (Seq. (3)); (Lys) 5Arg (Seq. (4)) or ArgLys (Seq. (5)). ACTIVITY : Antidiabetic; Anorectic; Anticoagulant; Thrombolytic. No details of tests for these activities are given. MECHANISM OF ACTION : GLP-1 agonist; Extendin agonist; Hirudin agonist.