Patent ID: 6342479
Filing Date: 2002-01-29
Classification: A61K

Abstract:
A method of prolonging the survival of pancreatic cells transplanted in a patient said method comprising administering a therapeutically effective amount of a somatostatin agonist selected from the group consisting ofD-&bgr;-Nal-Cys-Tyr-D-Trp-Lys-Thr-Cys-Thr-NH2, D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-&bgr;-Nal-NH2, D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Cys-&bgr;-Nal-NH2, D-&bgr;-Nal-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2, D-Phe-Cys-Phe-D-Trp-Lys-Thr-Pen-Thr-NH2, D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-OH, D-Phe-Cys-Phe-D-Trp-Lys-Thr-Pen-Thr-OH, Gly-Pen-Phe-D-Trp-Lys-Thr-Cys-Thr-OH, Phe-Pen-Tyr-D-Trp-Lys-Thr-Cys-Thr-OH, Phe-Pen-Phe-D-Trp-Lys-Thr-Pen-Thr-OH, H-D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-ol, H-D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, H-D-Trp-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2, H-D-Trp-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2, H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Trp-NH2, H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2, Ac-D-Phe-Lys*-Tyr-D-Trp-Lys-Val-Asp-Thr-NH2 (an amide bridge formed between Lys* and Asp), Ac-hArg(Et)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(Et)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(Bu)-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(Et)2-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-L-hArg(Et)2-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(CH2CF3)2-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(CH2CF3)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(CH2CF3)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Phe-NH2, Ac-D-hArg(CH2CF3)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NHEt, Ac-L-hArg(CH2CF3)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(CH2CF3)2-Gly-Cys-Phe-D-Trp-Lys(Me)-Thr-Cys-Thr-NH2, Ac-D-hArg(CH2CF3)2-Gly-Cys-Phe-D-Trp-Lys(Me)-Thr-Cys-Thr-NHEt, Ac-hArg(CH3, hexyl)-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, H-hArg(hexyl2)-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(Et)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NHEt, Ac-D-hArg(Et)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Phe-NH2, Propionyl-D-hArg(Et)2-Gly-Cys-Phe-D-Trp-Lys(iPr)-Thr-Cys-Thr-NH2, Ac-D-&bgr;-Nal-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Gly-hArg(Et)2-NH2, Ac-D-Lys(iPr)-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(CH2CF3)2-D-hArg(CH2CF3)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-D-hArg(CH2CF3)2-D-hArg(CH2CF3)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Phe-NH2, Ac-D-hArg(Et)2-D-hArg(Et)2-Gly-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-NH2, Ac-Cys-Lys-Asn-4-Cl-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-Ser-D-Cys-NH2, Bmp-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2, Bmp-Tyr-D-Trp-Lys-Val-Cys-Phe-NH2, Bmp-Tyr-D-Trp-Lys-Val-Cys-p-Cl-Phe-NH2, Bmp-Tyr-D-Trp-Lys-Val-Cys-&bgr;-Nal-NH2, H-D-&bgr;-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2, H-D-Phe-Cys-Tyr-D-Trp-Lys-Abu-Cys-Thr-NH2, H-D-Phe-Cys-Tyr-D-Trp-Lys-Abu-Cys-&bgr;-Nal-NH2, H-pentafluoro-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2, Ac-D-&bgr;-Nal-Cys-pentafluoro-Phe-D-Trp-Lys-Val-Cys-Thr-NH2, H-D-&bgr;-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-&bgr;-Nal-NH2, H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-&bgr;-Nal-NH2, H-D-&bgr;-Nal-Cys-Tyr-D-Trp-Lys-Abu-Cys-Thr-NH2, H-D-p-Cl-Phe-Cys-Tyr-D-Trp-Lys-Abu-Cys-Thr-NH2, Ac-D-p-Cl-Phe-Cys-Tyr-D-Trp-Lys-Abu-Cys-Thr-NH2, H-D-Phe-Cys-&bgr;-Nal-D-Trp-Lys-Val-Cys-Thr-NH2, H-D-Phe-Cys-Tyr-D-Trp-Lys-Cys-Thr-NH2, cyclo(Pro-Phe-D-Trp-N-Me-Lys-Thr-Phe), cyclo(Pro-Phe-D-Trp-N-Me-Lys-Thr-Phe), cyclo(Pro-Phe-D-Trp-Lys-Thr-N-Me-Phe), cyclo(N-Me-Ala-Tyr-D-Trp-Lys-Thr-Phe), cyclo(Pro-Tyr-D-Trp-Lys-Thr-Phe), cyclo(Pro-Phe-D-Trp-Lys-Thr-Phe), cyclo(Pro-Phe-L-Trp-Lys-Thr-Phe), cyclo(Pro-Phe-D-Trp(F)-Lys-Thr-Phe), cyclo(Pro-Phe-Trp(F)-Lys-Thr-Phe), cyclo(Pro-Phe-D-Trp-Lys-Ser-Phe), cyclo(Pro-Phe-D-Trp-Lys-Thr-p-Cl-Phe), cyclo(D-Ala-N-Me-D-Phe-D-Thr-D-Lys-Trp-D-Phe), cyclo(D-Ala-N-Me-D-Phe-D-Val-Lys-D-Trp-D-Phe), cyclo(D-Ala-N-Me-D-Phe-D-Thr-Lys-D-Trp-D-Phe), cyclo(D-Abu-N-Me-D-Phe-D-Val-Lys-D-Trp-D-Tyr), cyclo(Pr-Tyr-D-Trp-t-4-AchxAla-Thr-Phe), cyclo(Pro-Phe-D-Trp-t-4-AchxAla-Thr-Phe), cyclo(N-Me-Ala-Tyr-D-Trp-Lys-Val-Phe), cyclo(N-Me-Ala-Tyr-D-Trp-t-4-AchxAla-Thr-Phe), cyclo(Pro-Tyr-D-Trp-4-Amphe-Thr-Phe), cyclo(Pro-Phe-D-Trp-4-Amphe-Thr-Phe), cyclo(N-Me-Ala-Tyr-D-Trp-4-Amphe-Thr-Phe), cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Gaba), cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Gaba-Gaba), cyclo(Asn-Phe-D-Trp-Lys-Thr-Phe), cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-NH(CH2)4CO), cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-&bgr;-Ala), cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-D-Glu)-OH, cyclo(Phe-Phe-D-Trp-Lys-Thr-Phe), cyclo(Phe-Phe-D-Trp-Lys-Thr-Phe-Gly), cyclo(Phe-Phe-D-Trp-Lys-Thr-Phe-Gaba), cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Gly), cyclo(Asn-Phe-Phe-D-Trp(F)-Lys-Thr-Phe-Gaba), cyclo(Asn-Phe-Phe-D-Trp(NO2)-Lys-Thr-Phe-Gaba), cyclo(Asn-Phe-Phe-Trp(Br)-Lys-Thr-Phe-Gaba), cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe(I)-Gaba), cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Tyr(But)-Gaba), cyclo(Bmp-Lys-Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-Pro-Cys)-OH, cyclo(Bmp-Lys-Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-Pro-Cys)-OH, cyclo(Bmp-Lys-Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-Tpo-Cys)-OH, cyclo(Bmp-Lys-Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-MeLeu-Cys)-OH, cyclo(Phe-Phe-D-Trp-Lys-Thr-Phe-Phe-Gaba), cyclo(Phe-Phe-D-Trp-Lys-Thr-Phe-D-Phe-Gaba), cyclo(Phe-Phe-D-Trp(5F)-Lys-Thr-Phe-Phe-Gaba), cyclo(Asn-Phe-Phe-D-Trp-Lys(Ac)-Thr-Phe-NHâ€”(CH2)3â€”CO), cyclo(Lys-Phe-Phe-D-Trp-Lys-Thr-Phe-Gaba), cyclo(Lys-Phe-Phe-D-Trp-Lys-Thr-Phe-Gaba), cyclo(Orn-Phe-Phe-D-Trp-Lys-Thr-Phe-Gaba) and H-Cys-Phe-Phe-D-Trp-Lys-Thr-Phe-Cys-NH2 wherein a disulfide bond exists in the somatostatin agonists having two Cys residues.