| 摘要 |
2088166 9202545 PCTABS00010 The present invention provides a polypeptide of the formula (I): XX1TrpX2X3X4X5X6X7NH2, wherein X is a group X8Arg(or D-Arg)X9X10 and X8 is des NH2Pro,TyrPro,des NH2TyrPro, Ada, Pro, D-Pro or is deleted; X9 is Gly, Ala, D-Ala or is deleted; X10 is Asn, Phe, D-Phe, or Phe or D-Phe substituted by one or more halo atoms; or X is a group A-(CH2)n-CO- in which A is a group containing 1 to 3 rings of which at least one ring is aromatic, each ring system being optionally substituted; and the alkylene group is optionally substituted by one to four groups selected from amino, hydroxy, C1-4 alkoxy and C1-4 alkyl optionally substituted by halo and n is 0 to 4; or X is cyclopentyl carbonyl substituted by a group X8Arg(or D-Arg)X9X10 as hereinbefore defined; X1 is His, ThiAla or is deleted; X2 is Ala, D-Ala, CPenc, D-tBuGly or Pro; X3 is Val or Val substituted by one or more halo atoms; X4 is Gly, Ala, D-Ala, Sarcosine, Pro, D-Pro or D-Phe; X5 is His or ThiAla; X6 is D-Pro.psi., Pro.psi., 2-pyrrolidinyl-3-hydroxypropionyl or D-Pro; X7 is Nle, Leu, Phe, Val, Mox, D-Phe, Phe, or D-Phe substituted by one or more halo atoms or naphthylAla or naphthyl D-Ala or a hydrophobic, substituted aromatic amino acid or aralkylamine or is deleted, and the pharmaceutically acceptable salts thereof. The polypeptides possess antagonist properties against bombesin-like peptides and are of value in the treatment of malignant disease. |
