| 摘要 |
PCT No. PCT/EP97/01657 Sec. 371 Date Apr. 8, 1999 Sec. 102(e) Date Apr. 8, 1999 PCT Filed Apr. 2, 1997 PCT Pub. No. WO97/38009 PCT Pub. Date Oct. 16, 1997The invention concerns cyclopeptides of formula (I): Cyclo-(Arg-Gly-Asp-X-Y) in which X is Cha, Nal, Phe, 2-R1-Phe, 3-R1-Phe, 4-R1-Phe, homo-Phe, Phg, Thi, Trp, Tyr or derivatives of Tyr, whereby the OH group can be etherified by alkyl groups containing 1-18 C-atoms and the amino-acid groups given can also be derivatives, R1 is NH2, NO2, I Br, Cl, F, alkyl with 1-18 C-atoms, Ar, Ar-O or3H, Y is Gly in which the alpha N-atom may be substituted by R2 and/or the alpha C-atom may be substituted by R3 and/or R4, with the provision that Gly has at least one of the substituents specified, Ar is phenyl which may be substituted by one or two of groups NH2, NO2, I, Br, Cl, F, alkyl with 1-6 C-atoms or 3H, R2, R3 or R4, independently of each other, are alkyl with 1-18 C-atoms or R2 and R3 or R3 and R4 together in each case are a branched or unbranched alklyene chain with 3 to 18 C-atoms so that either the alpha N-atom or the alpha C-atom together with the alkylene chain, or the alpha C-atom alone, forms a ring with alkylene chain, whereby, when optically active amino-acid or amino-acid-derivative groups are involved, both the D- and the L-form are included, plus derivatives, in particular the beta -ester of aspartic acid or N-guanidine acyl derivatives of arginine or prodrug as well as their physiologically acceptable salts. These compounds act as integrin inhibitors and may be used particularly for the prophylaxis and treatment of circulatory and angiogenic conditions and microbial infections as well as in tumor therapy. |
