The Administrators of the Tulane Educational Fund

Walajapet G Rajeswaran

David H Coy

William A Murphy

The present invention is directed to a somatostatin antagonist according to formula (I): A-cyclo {D-Cys-A-D-Trp-A-A-Cys}-AY, wherein Ais an optionally substituted aromatic a-amino acid; Ais an optionally substituted aromatic &#x3b1;-amino acid; Ais Dab, Dap, Lys or Om; Ais &#x3b2;-Hydroxyvaline, Ser, Hser, or Thr; Ais an optionally substituted D- or L-aromatic amino acid; and Yis OH, NHor NHR' where Ris (C)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, OH, CN, (C) alkyl, (C) alkenyl, (C) alkynyl, (C)alkoxy, Bzl, O-Bzl, and NRR&#x2032; wherein Rad Reach is independently H, O, or (C) alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of Aof 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.

Somatostatin antagonists

The present invention is directed to a somatostatin antagonist according to formula (I), wherein Ais an optionally substituted aromatic &#x221d;-amino acid; Ais an optionally substituted aromatic &#x221d;-amino acid; Ais Dab, Dap, Lys or Orn; Ais &#x3b2;-Hydroxyvaline, Ser, Hser, or Thr; Ais an optionally substituted D- or L-aromatic -amino acid; and Yis OH, NHor NHR, or NHR, where Ris (C)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, NO, OH, CN, (C)alkyl, (c)alkenyl, (c)alkynyl, (C)alkoxy, Bzl, O-Bzl, and NRR, where Rad Reach is independently H, O, or (C)alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of Aof 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.

Claimed are a series of somatostatin agonists and uses thereof, according to formula (I),A-cyclo[Cys-A-D-Trp-A-A-Cys]-A-Y, &#x2003;&#x2003;(I)wherein A, A, A, A, Aand Yare as defined in specification provided that the amine nitrogen of at least one peptide bond is substituted with a methyl group or pharmaceutically acceptable salts thereof.

Growing community of inventors

Kalamazoo, MI, United States of America

Walajapet G Rajeswaran