Patent ID: 6610826
Filing Date: 2003-08-26
Classification: A61K,A61P,C07K,Y02P

Abstract:
A compound of the formula IRâ€”Qâ€”Xâ€ƒâ€ƒI in whichR is cyclo-(Arg-Gly-Asp-Z), where Z is bonded via a side chain to Q, or if Q is absent, to X, Q is absent, or is â€”(COâ€”R1â€”NHâ€”)m, â€”(NHâ€”R1â€”COâ€”)m, â€”(COâ€”R1â€”COâ€”)m, â€”(COâ€”CH2â€”Oâ€”CH2CH2â€”Oâ€”CH2CH2â€”NHâ€”)n, â€”(NHâ€”CH2â€”Oâ€”CH2CH2â€”Oâ€”CH2CH2â€”COâ€”)n, â€”(NHâ€”CH2CH2â€”Oâ€”CH2CH2â€”Oâ€”CH2â€”COâ€”)n or â€”(COâ€”CH2â€”Oâ€”CH2CH2â€”Oâ€”CH2CH2â€”NHâ€”)nâ€”(COâ€”R1â€”NHâ€”)m, X is â€”COâ€”CH&boxH;CH2, â€”COâ€”C(CH3)&boxH;CH2, â€”NHâ€”CH&boxH;CH2, â€”NHâ€”C(CH3)&boxH;CH2 or â€”NHâ€”(CH2)pSR10, Z is in each case independently of one another an amino acid residue or a di- or tripeptide residue, where the amino acids independently of one another are selected from a group consisting of Ala, Asn, Asp, Arg, Cys, Gln, Glu, Gly, His, Homo-Phe, Ile, Leu, Lys, Met, Phe, Phg, Pro, Ser, Thr, Trp, Tyr, Val and M, wherein said amino acids can be derivatized, and the amino acid residues are linked to one another in peptide fashion via the &agr;-amino- and &agr;-carboxyl groups, and where M is always present, M is a residue of NH(R8)â€”CH(R3)â€”COOH, R1 is absent or is R2, R9, R2â€”R9â€”R2, or phenylene which is unsubstituted or mono- or disubstituted by R5, where the chain length of R5 is in each case independent of one another, R2 is alkylene having 1-10 C atoms, where 1 or 2 methylene groups can be replaced by S, â€”CH&boxH;CHâ€” or â€”Câ‰¡Câ€”, R3 is â€”R5â€”R4, â€”R6â€”R4 or â€”R7â€”R4, R4 is OH, NH2, SH or COOH, R5 is alkylene having 1-6 C atoms, R6 is alkylenephenylene having 7-14 C atoms, R7 is alkylenephenylalkylene having 8-15 C atoms, R8 is H, A or alkylenephenyl having 7-12 C atoms, R9 is cycloalkylene having 3-7 C atoms, R10 is H or an S protective group, A is alkyl having 1-6 C atoms, Hal is F, Cl, Br or I m and n in each case independently of one another are 0, 1, 2 or 3 and p is 1,2, or 3, where each optically active amino acid or amino acid derivative that is present is in either the D or L form; or a salt thereof.