Polypeptide bombesin antagonists

Details Polypeptide bombesin antagonists Polypeptide bombesin antagonists

C - Chemistry, Metallurgy

07

K

C07K 7/06 (2006.01) A61K 38/08 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2135787

Pseudopeptides comprising a peptide of formula (I): X-A1-A2-Trp-Ala-Val-Gly- His-Leu-psi-A9-Q wherein X is hydrogen, a single bond linking the alpha amino group of A1 to the gamma carboxyl moiety on the 3- priopionyl moiety of A2 when A2 is Glu, or a group of formula R1CO- wherein Ri is selected from the groups consisting of: a) hydrogen, C1-10alkyl, phenyl or phenyl-C1-10-alkyl, p-H1-phenyl, p-H1-phenyl-C1-10-alkyl, naphthyl, naphthyl-C1-10-alkyl, indolyl, indolyl-Cl1- 10-alkyl, pyridyl, pyridyl-C1-10,-alkyl, thienyl, thienyl-C1-10-alkyl, cyclohexyl or cyclohexyl-C1-10-alkyl, where H1 = F, Cl, Br, OH, CH3 or OCH3; b) N(R2)(R3)-, wherein R2 is hydrogen, C1-10alkyl, phenyl or phenyl-C1-10-alkyl, R3 is hydrogen or C1-10alkyl; c) R4O-, wherein R4 is C1- 10alkyl, phenyl or phenyl-C1-10-alkyl; A1 is a D- or L-amino acid residue selected from the group consisting of Phe, p-H1-Phe, pGlu, Nal, Pal, Tpi, unsubstituted Trp or Trp substituted in the benzene ring by one or more members selected from the group consisting of F, Cl, Br, NH2 or C1-3alkyl; or A1 is a peptide bond linking the acyl moiety of R1CO- to the alpha amino moiety of A2; A2 is Gln, Glu[-], Glu(Y) or His, wherein [-] is a single bond linking the gamma carboxyl group of A2 when A2 is Glu with the alpha amino group of A1 where X is a single bond, Y is -OR5 or -N(R5)(R6) wherein R5 is hydrogen, C1-3alkyl or phenyl; R6 is hydrogen or C1-3alkyl; and R7 is hydrogen, C1-3alkyl or -NHCONH2; Leu-psi- is a reduced form of Leu wherein the C = O moiety of Leu is instead -CHr such that the bond of this -CHr moiety with the alpha amino moiety of the adjacent A9 residue is a pseudopeptide bond; A9 is Tac, MTac, or DMTac; and Q is NH2 or OQ1 where Q1 is hydrogen, C1-10alkyl, phenyl or phenyl-C1-10-alkyl; and the pharmaceutically acceptable acids or salts thereof.

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