Somatostatin antagonists

Details Somatostatin antagonists Somatostatin antagonists

2008-05-27

2008-05-27

Carlson, Karen Cochrane (Department: 1656)

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Somatostatin ; related peptides

C530S317000, C514S001000

Reexamination Certificate

active

10469836

ABSTRACT:
The present invention is directed to a somatostatin antagonist according to formula (I), wherein A1is an optionally substituted aromatic ∝-amino acid; A2is an optionally substituted aromatic ∝-amino acid; A3is Dab, Dap, Lys or Orn; A4is β-Hydroxyvaline, Ser, Hser, or Thr; A5is an optionally substituted D- or L-aromatic -amino acid; and Y1is OH, NH2or NHR1, or NHR1, where R1is (C1-6)alkyl; wherein each said optionally substituted aromatic -amino acid is optionally substituted with one or more substituents 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 NR9R10, where R9ad R10each is independently H, O, or (C1-6)alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A1of 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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