| 摘要 |
The present invention is directed to a somatostatin antagonist according to formula (I), wherein A<1 >is an optionally substituted aromatic ∝-amino acid; A<2 >is an optionally substituted aromatic ∝-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 -amino acid; and Y<1 >is OH, NH2 or NHR<1>, where R<1 >is (C1-6)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, (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.
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