| 摘要 |
The present invention provides a polypeptide of the formula (I): XX<1>TrpX<2>X<3>X<4>X<5>X<6>X<7>NH2, wherein X is a group X<8>Arg(or D-Arg)X<9>X<10> and X<8> is des NH2Pro,TyrPro,des NH2TyrPro, Ada, Pro, D-Pro or is deleted; X<9> is Gly, Ala, D-Ala or is deleted; X<10> 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 X<8>Arg(or D-Arg)X<9>X<10> as hereinbefore defined; X<1> is His, ThiAla or is deleted; X<2> is Ala, D-Ala, CPenc, D-tBuGly or Pro; X<3> is Val or Val substituted by one or more halo atoms; X<4> is Gly, Ala, D-Ala, Sarcosine, Pro, D-Pro or D-Phe; X<5> is His or ThiAla; X<6> is D-Pro psi , Pro psi , 2-pyrrolidinyl-3-hydroxypropionyl or D-Pro; X<7> 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. |
