DERIVATIVES OF PEPTIDES AND MIMETICS OF PEPTIDES WITH INTEGRINE INHIBITOR PROPERTIES III.

摘要

Procedure for the preparation of a compound of formula I ** (See formula) ** BQ-X1 I in which B is a bioactive molecule that confers cell adhesion, Q is missing or is an organic spacer molecule and X1 is an anchor molecule selected from the group -W (i) -VW (ii) -V- [V-W2] 2 (iii) or -V- [V- (V-W2) 2] 2 (iv), where W means * * (See formula) ** and V Lys, Asp or Glu, YY is a carboxyl group, a free amino group of group B being peptically linked with a free carboxyl group of the spacer molecule Q or the anchor molecule X1, or a free amino group of the Q moiety with a free carboxyl group of the X1 moiety, or its salts, characterized in that the bioactive molecule B, which may be provided with protective groups, and the spacer-anchor molecule (Q-X1) or the molecule anchoring (X1) provided with protective groups and phosphonic ester groups are peptically linked to each other and then the protective groups dissociate simultaneously with phosphonic ester groups; and / or because a basic or acidic compound of the formula I is transformed by treatment with an acid or base into one of its salts, the phosphonic ester groups being tetrabenzyl ester groups of the 5-carboxy-m-xylene-bisphosphonic acid.