PEPTIDE DERIVATIVES

• Main Authors: STEVEN W.J. LAMBERT, ERIC P. KRENNING, JANOS PLESS, RAINER ALBERT
• Format: Patent
• Language: English
• Published: 28.08.1991
• Edition: 5
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

1. Method for producing new somatostatine peptide derivatives including a chelating group capable of creating a complex with detectable metal ion, optionally in the form of salt or in the form of a complex with detectable metal ion, which group is directly or indirectly attached to the terminal amine group, whereas the somatostatine peptide is natural somatostatine or a compound of formula 1 where A stands for a group of formula RCO, where RCO-stands for:a) an L- or D-phenylalanine residue optionally ring-substituted by F, Cl, Br, NO2, NH2, OH, C1-3 alkyl and/or C1-3 alkoxy;b) the residue of a natural or synthetic α-amino acid other than defined under a) above or of a corresponding D-amino acid, orc) a dipeptide residue in which the individual amino acid residues are the same or different and are selected from those defined under a) and/or b) above, A' stands for hydrogen, Y1 and Y2 represent together a direct bond or each of Y1 and Y2 is independently hydrogen, B stands for -Phe - optionally ring-substituted by halogen, NO2, NH2, OH, C1-3alkyl and/or C1-3 alkoxy (including pentafluoroalanine, or Β-naphthyl-Ala, C stands for (L)-Trp- or (D)-Trp-, D stands for Lys, E stands for Thr, Ser, Val, Phe, Ile or an aminoisobutyric or aminobutyric acid residue, G stands for group of formula 10 wherein R11 stands for hydrogen, C1-3 alkyl, R12 stands for hydrogen, C1-3 alkyl or a group of formula -CH(R13)-X1.