| abstract |
A peptide of the formula I: nR-A-B-C-Trp-Ala-Val-X-Y-T-W I nwherein R is a group of the formula 4-(ClCH₂CH₂)₂N-C₆H₄-CO-, 3-(ClCH₂CH₂)₂N-C₆H₄-CO-, ClCH₂CH₂NHCO-, ClCH=CH-CO-, BrCH=CH-CO-, CH₂=CClCO-, CH₂=CBrCO- (cis/trans isomers),n CH=C-CO-, ClCH₂CH₂CH₂N(NO)CO-, or ClCH₂CO-CH(R₁)NHCO(CH₂)₂CO-; nA = valence bond, or Gly, Leu-Gly, Arg-Leu-Gly, Gln-Arg-Leu-Gly; nB = valence bond or Asn or Thr; C = Gln or His; nX = Gly or ala; Y = valence bond or His(R₂), his(R₂), Phe, phe, Ser, ser, Ala or ala; T = valence bond or Leu, leu, Phe or phe; nW is a group of the formula OH, NH₂, NH(CH₂)₄CH₃, H(CH₂)₂C₆H₅, Met-R₃, Leu-R₃, Ile-R₃, or Nle-R₃; R₁ = H, linear or branched alyphatic chain having for 1 to 11 carbon atoms, benzyl or phenyl group; R₂ = H or Tos, Dnp or Bzl and R₃ = NH₂, OH, OCH₃ or NHNH₂ and pharmaceutically acceptable salts are bombesin antagonists. Their preparation and pharmaceutical compositions containing them are also described. |