| abstract |
The present invention is directed to a somatostatin antagonist according to formula (I), wherein A1 is an optionally substituted aromatic ≡-amino acid; A2 is an optionally substituted aromatic ≡-amino acid; A3 is Dab, Dap, Lys or Orn; A4 is β-Hydroxyvaline, Ser, Hser, or Thr; A5 is an optionally substituted D- or L-aromatic Χ-amino acid; and Y1 is OH, NH¿2? or NHR?1¿, where R1 is (C¿1-6?)alkyl; wherein each said optionally substituted aromatic Χ-amino acid is optionally substituted with one or more substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6)alkyl, (c2-6)alkenyl, (c2-6)alkynyl, (C1-6)alkoxy, Bzl, O-Bzl, and NR?9R10¿, where R?9 ad R10¿ each is independently H, O, or (C¿1-6?)alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A?1¿ of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof, and to uses thereof. |