Somatostatin antagonists

Details Somatostatin antagonists Somatostatin antagonists

2007-08-20

2008-08-05

Carlson, Karen Cochrane (Department: 1656)

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Somatostatin ; related peptides

C530S345000, C530S300000, C514S002600, C514S806000

Reexamination Certificate

active

07408024

ABSTRACT:
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 A1is an optionally substituted aromatic a-amino acid; A2is an optionally substituted aromatic α-amino acid; A3is Dab, Dap, Lys or Om; A4is β-Hydroxyvaline, Ser, Hser, or Thr; A5is an optionally substituted D- or L-aromatic amino acid; and Y1is OH, NH2or NHR1′ where RIis (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 NR9R10′ wherein 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 is directed to uses thereof.

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