| abstract |
The present invention is directed to a somatostatin antagonist according to formula (I): A 1 -cyclo {D-Cys-A 2 -D-Trp-A 3 -A 4 -Cys}-A 5 Y 1 , wherein A 1 is an optionally substituted aromatic a-amino acid; A 2 is an optionally substituted aromatic α-amino acid; A 3 is Dab, Dap, Lys or Om; A 4 is β-Hydroxyvaline, Ser, Hser, or Thr; A 5 is an optionally substituted D- or L-aromatic amino acid; and Y 1 is OH, NH 2 or NHR 1 ′ where R I is (C 1-6 )alkyl; wherein each said optionally substituted aromatic amino acid is optionally substituted with one or more substituents each independently selected from the group consisting of halogen, NO 2 , OH, CN, (C 1-6 ) alkyl, (C 2-6 ) alkenyl, (C 2-6 ) alkynyl, (C 1-6 )alkoxy, Bzl, O-Bzl, and NR 9 R 10 ′ wherein R 9 ad R 10 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 is directed to uses thereof. |