Publication number: 20020032306
Abstract: The invention relates to compounds of the formula (I) R1 Q1 XQ2 R2, in which: Q1, Q2, each independent of one another, are missing or are NH(CH2)n CO; R1, R2, each independent of one another, are missing or are cyclo(ArgGlyAspZ), wherein Z is missing in the side chain of Q1 or Q2 or if Q1 and/or Q2 are missing, is bound to X, at least one of the groups R1 or R2 always having to be included; X is COR 18 CO, and if R1 Q1 or R2 Q2 are missing is R10, R13, R16, HetCO or a fluorescent pigment residue linked through a CONH, COO, NHC (═S)NH, NHC(═O)NH, SO2 NH or NHCO bond; and Z, R10, R13, R16, R18, Het and n have the meanings given in claim 1. The invention also relates to the salts of said compounds. Said compounds and their salts can be used as integrin inhibitors, in particular for the prevention and treatment of circulatory diseases, thrombosis, heart infarct, coronary heart diseases, arteriosclerosis, angiogenic diseases and in tumor therapy.
Type:
Application
Filed:
August 18, 1998
Publication date:
March 14, 2002
Inventors:
ALFRED JONCZYK, SIMON LAWRENCE GOODMAN, BEATE DIEFENBACH, ARNE SUTTER, HORST KESSLER
Patent number: 6001961
Abstract: The invention relates to novel cyclopeptides of the formula Icyclo-(nArg-nGly-nAsp-nD-nE) I,in whichD 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(AcNH.sub.2), 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.
Type:
Grant
Filed:
September 16, 1996
Date of Patent:
December 14, 1999
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
Alfred Jonczyk, Simon Goodman, Beate Diefenbach, Arne Sutter, Gunter Holzemann, Horst Kessler, Michael Dechantsreiter