SOMATOSTATIN ANTAGONISTS

摘要

The present invention is directed to a somatostatin antagonist according to formula (I), wherein A<1> is an optionally substituted aromatic PROPORTIONAL -amino acid; A<2> is an optionally substituted aromatic PROPORTIONAL -amino acid; A<3> is Dab, Dap, Lys or Orn; A<4> is beta -Hydroxyvaline, Ser, Hser, or Thr; A<5> is an optionally substituted D- or L-aromatic W-amino acid; and Y<1> is OH, NH2 or NHR<1>, where R<1> is (C1-6)alkyl; wherein each said optionally substituted aromatic W-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<9>R<10>, where R<9> ad R<10> each is independently H, O, or (C1-6)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.