Compositions of somatostatin analogues

Details Compositions of somatostatin analogues Compositions of somatostatin analogues

2007-03-20

2007-03-20

Russel, Jeffrey Edwin (Department: 1654)

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

Attached to lymphokine, cytokine, or other secreted growth...

C514S011400, C530S311000

Reexamination Certificate

active

10486310

ABSTRACT:
In one embodiment, a composition of somatostatin analogues having the general formula:is provided wherein Z may be absent or present and when present is selected from DOTA- and DTPA-based chelators, NOTA-based chelators, carbonyl compounds, hydrazino nicotinamide, N4-chelators, desferrioxamine, NxSy-chelators, optionally complexed or labeled with a radioisotope, tyrosine for halogenation, a fluorescent dye, or biotin. The composition further provides that L may or may not be present and when present is a linker molecule, X1 is glutamic acid or a symmetric or asymmetric diamino acid containing 3 or 4 consecutive C 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.

REFERENCES:
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patent: 6930088 (2005-08-01), Hornik et al.
International Search Report, Based on PCT/EP02/09004, Dated Nov. 29, 2002.
Scicinski, J. J., et al., “The solid phase synthesis of a series of tri-substituted hydantoin ligands for the somatostatin SST5 receptor,” Bioorganic & Medicinal Chemistry Letters, Oxford, GB, vol. 8, No. 24, Dec. 15, 1998, pp. 3609-3614, XP004150376.
Reubi, J. C., et al., “A selective analog for the somatostatin SST1-receptor surtype expressed by human tumors,” European Journal of Pharmacology, Amsterdam, NL, Mar. 12, 1998, pp. 103-110, XP000876543.
Hoyer, D., et al., “Classification and nomenclature of somatostatin receptors,” Trends in Pharmacological Sciences, Elsevier Trends Journal, Cambridge, GB, vol. 16, No. 3, Mar. 1995, pp. 86-88, XP004207465.

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