Irreversible peptide ligands for bombesin receptors

Details Irreversible peptide ligands for bombesin receptors Irreversible peptide ligands for bombesin receptors

C - Chemistry, Metallurgy

07

K

530/7.06, 167/10

C07K 7/06 (2006.01) C07K 7/08 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1331074

TITLE: Irreversible Peptide Ligands for Bombesin Receptors ABSTRACT: Peptides of formula A-B-C-D-Gln-Trp-Ala-Val-X-Y-T-W (either A=H, Boc; Ac; one of B and C = pMel, mMel; the other of B and C = valence bond, Gly, Leu-Gly, E -Leu-Gly, Gln- E -Leu-Gly,E,E-Gly with E-Arg(A), arg(A) Lys(A), lys(A), Orn(A), orn(A) or A=H, B-Glp-Arg-Leu-Gly, C=pMel or mMel; and D = sigma bond, Asn, Thr; X = Gly, ala; Y = valence bond, His(R1), his(R1), Phe, phe, Ser,ser, Ala, ala; T = valence bond, Leu, leu, Phe,phe; W = OH,NH2,NH(CH2)4CH3, NH(CH2)2C6H5, Met-R2, Leu-R2, Ile-R2, Nle-R2; R1 = H, Tos, Dnp, Bzl; R2 = NH2, OH, OCH3, NHNH2) and their pharmaceutically acceptable salts are irreversible peptide ligands for Bombesin receptors. Their preparation and pharmaceutical compositions containing them are also described.

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