US 7,541,018 B2
Treatment process using somatostatin analogues
Helmut Robert Maecke, Loerrach (Germany); Jean Claude Reubi, Wabern (Switzerland); Hans Rink, Bubendorf (Switzerland); and Klaus-Peter Eisenwiener, Bern (Switzerland)
Assigned to University of Bern, Bern (Switzerland)
Filed on Mar. 08, 2007, as Appl. No. 11/683,734.
Application 11/683734 is a continuation of application No. 10/486310, granted, now 7,192,570, previously published as PCT/EP02/09004, filed on Aug. 07, 2002.
Claims priority of application No. 01203033 (EP), filed on Aug. 10, 2001.
Prior Publication US 2007/0154392 A1, Jul. 05, 2007
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 38/12 (2006.01); C07K 14/655 (2006.01)
U.S. Cl. 424—1.41  [514/11] 46 Claims
 
1. A method for treating a cancerous disease, comprising:
exposing one or more somatostatin receptors within a cancerous cell to a pharmaceutical composition comprising a somatostatin analogue, wherein the somatostatin analogue binds to the one or more somatostatin receptors and has the general formula:

OG Complex Work Unit Drawing
wherein:
Z is optionally present or absent and when present is selected from the group consisting of DOTA-based chelators, DTPA-based chelators, NOTA-based chelators carbonyl compounds, hydrazino nicotinamide, N4-chelators, desferrioxamine, NXSY-chelators, tyrosine for halogenation, a fluorescent dye, and biotin;
L is optionally present or absent and when present is a linker molecule;
X1 is a symmetric or asymmetric diamino acid containing 3 or 4 consecutive carbon atoms;
X2 is a positively charged natural or unnatural amino acid, an arginine mimic, citrulline, or a neutral amino acid;
X3 is phenylalanine, Ala-[3-(2-thienyl)], α-naphthylalanine, or β-naphthylalanine;
X4 is an aromatic amino acid;
X5 is threonine or serine; and
X6 is phenylalanine, Ala-[3-(2-thienyl)], α-naphthylalanine, or β-naphthylalanine.