Cyclic adhesion inhibitors

Details Cyclic adhesion inhibitors Cyclic adhesion inhibitors

C - Chemistry, Metallurgy

07

K

C07K 7/64 (2006.01) A61K 38/12 (2006.01) C07K 1/22 (2006.01) C07K 14/705 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2185489

The invention relates to novel cyclopeptides of the formula I cyclo-(nArg-nGly-nAsp-nD-nE) I, in which D and E in each case independently of one another are Gly, Ala, .beta.-Ala, Asn, Asp, Asp (OR), Arg, Cha, Cys, Gln, Glu, His, Ile, Leu, Lys, Lys(Ac), Lys (AcNH2), Lys (AcSH), Met, Nal, Nle, Orn, Phe, 4-Hal-Phe, homo-Phe, Phg, Pro, Pya, Ser, Thr, Tia, Tic, Trp, Tyr or Val, which amino acid residues can also be derivatized, R is alkyl having 1-18 carbon atoms, Hal is F, Cl, Br, I, Ac is alkanoyl having 1-10 carbon atoms, aroyl having 7-11 carbon atoms or aralkanoyl having 8-12 carbon atoms, n denotes no substituent or an alkyl radical R, benzyl or an aralkyl radical having 7-18 carbon atoms on the alpha-amino function of the relevant amino acid residue, with the proviso that at least one amino acid residue has a substituent n and that, where residues of optically active amino acids and amino acid derivatives are involved, both the D and the L forms are included, and also their physiologically acceptable salts. These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation, angiogenic disorders, microbial infections and in tumour therapy.

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