Inhibitors for urokinase receptor
    7.
    发明授权
    Inhibitors for urokinase receptor 失效
    尿激酶受体抑制剂

    公开(公告)号:US06528619B1

    公开(公告)日:2003-03-04

    申请号:US09402641

    申请日:2000-01-10

    IPC分类号: C07K708

    CPC分类号: C12N9/6462 C12Y304/21073

    摘要: The present invention provides peptides as inhibitors of the binding of urokinase to the urokinase receptor. The peptides have the general structural formula (I): X1-[X2]n-X3-X4-K-Y-F-X5-X6-I-X7-W-[X8]m  (I) in which X1, X2, X3, X4, X5, X6, X7 and X8 each denote an aminocarboxylic acid, n and m are each independently 0 or 1, K denotes an aminocarboxylic acid with a lysine side chain, Y denotes an aminocarboxylic acid with a tyrosine side chain, F denotes an aminocarboxylic acid with a phenyl-alanine side chain, I denotes an aminocarboxylic acid with an isoleucine side chain, W denotes an aminocarboxylic acid with a tryptophan side chain, and the monomeric building blocks are linked by —CONR1— or —NR1CO— bonds where R1 in each case independently denotes hydrogen, methyl or ethyl, and pharmaceutically compatible salts and derivatives thereof.

    摘要翻译: 本发明提供肽作为尿激酶与尿激酶受体结合的抑制剂。 肽具有通式结构式(I):其中X 1,X 2,X 3,X 4,X 5,X 6,X 7和X 8各自表示氨基羧酸,n和m各自独立地为0或1,K表示氨基羧酸, 赖氨酸侧链,Y表示具有酪氨酸侧链的氨基羧酸,F表示具有苯基 - 丙氨酸侧链的氨基羧酸,I表示具有异亮氨酸侧链的氨基羧酸,W表示具有色氨酸侧链的氨基羧酸, 并且单体结构单元通过-CONR1-或-NR1CO-键连接,其中R 1在每种情况下独立地表示氢,甲基或乙基,以及其药学上相容的盐和衍生物。