Irreversible bombesin antagonists.

摘要

A peptide of the formula I: R-A-B-C-Trp-Ala-Val-X-Y-T-W I wherein 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), <CHEM> CH=C-CO-, ClCH2CH2CH2N(NO)CO-, or ClCH2CO-CH(R1)NHCO(CH2)2CO-; A = valence bond, or Gly, Leu-Gly, Arg-Leu-Gly, Gln-Arg-Leu-Gly; B = valence bond or Asn or Thr; C = Gln or His; X = 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; W 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.