Reduced irreversible bombesin antagonists

Details Reduced irreversible bombesin antagonists Reduced irreversible bombesin antagonists

C - Chemistry, Metallurgy

07

K

C07K 7/04 (2006.01) A61K 38/08 (2006.01) C07K 7/08 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2045494

(57) Abstract A peptide of the formula (1) R-A B-C-Trp-Ala-Val-X-Y-T-W, wherein R represents a group or the formula 4-(ClCH2CH2)2N-C6H4-CH2CH(NHR1)CO-;3-(ClCH2CH2)2N-C6H4-CH2CH(NHR1)CO-;4-(ClCH2CH1)2N-C6H4-CO- : 3-(ClCH2CH2),N-C6H4-CO-; ClCH2CH2NHCO-; ClCH=CH-CO-, BrCH=CH-CO-, CH2=CCICO-, CH2=BrCO- (either cis or trans isomers); (a); CH=C-CO-; ClCH2CH2CH2N(NO)CO-; ClCH2CO-CH(R2)NHCO(CH2)2CO-; A repres- ents a valence bond, or a Gly, Leu-Gly, Arg-Leu-Gly, or Gln-Arg-Leu-Gly residue, B represents a valence bond or a Asn, Phe or Thr residue C represents a Gln or His residue, X represents a Gly or ala residue; Y represents a valence bond or a His(R3), his(R3). Phe, phe, Ser, ser. Ala or ala residue; T represents a valence bond, or a Leu, leu, Phe or phe residue; W represents a group of the formula OR2, NH2, NH(CH2)4)CH3, NH(CH2)2C6H5, Met-R4, Leu-R4, Ile-R4 or Nle-R4; R1 re- presents a hydrogen atom, a Boc group or an acyl group, R2 represents a hydrogen atom, a linear or branched alyphatic chain having from 1 to 11 carbon atoms, a benzyl or a C1-C21 phenyl group, R3 represents a hydrogen atom or a Tos, Dnp or Bzl group, R4 represents NH2, NH-NH2 or OR2, one or more peptide bonds (CONH) are replaced by reduced peptide bonds (CH2, NH), and the pharmaceutically acceptable salts thereof and pharmaceutically acceptable salts are bombesin antagonists. Their preparation and pharmaceutical compositions containing them are also described.

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