Somatostatin antagonists

摘要

The present invention is directed to a somatostatin antagonist according to formula (I): A¹-cyclo {D-Cys-A²-D-Trp-A³-A⁴-Cys}-A⁵Y¹, wherein A¹ is an optionally substituted aromatic a-amino acid; A² is an optionally substituted aromatic alpha-amino acid; A³ is Dab, Dap, Lys or Om; A⁴ is beta-Hydroxyvaline, Ser, Hser, or Thr; A⁵ is an optionally substituted D- or L-aromatic amino acid; and Y¹ is OH, NH₂ or NHR¹' 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, NO₂, OH, CN, (C_1-6) alkyl, (C_2-6) alkenyl, (C_2-6) alkynyl, (C_1-6)alkoxy, Bzl, O-Bzl, and NR⁹R¹⁰' wherein R⁹ 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 A¹ 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.