Patent number: 6127335
Abstract: The invention concerns cyclopeptides of formula (I): Cyclo-(Arg-Gly-Asp-X-Y) in which X is Cha, Nal, Phe, 2-R.sup.1 -Phe, 3-R.sup.1 -Phe, 4-R.sup.1 -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, R.sup.1 is NH.sub.2, NO.sub.2, I Br, Cl, F, alkyl with 1-18 C-atoms, Ar, Ar--O or.sup.3 H, Y is Gly in which the .alpha. N-atom may be substituted by R.sup.2 and/or the .alpha. C-atom may be substituted by R.sup.3 and/or R.sup.4, 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 NH.sub.2, NO.sub.2, I, Br, Cl, F, alkyl with 1-6 C-atoms or .sup.3 H, R.sup.2, R.sup.3 or R.sup.4, independently of each other, are alkyl with 1-18 C-atoms or R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 together in each case are a branched or unbranched alklyene chain with 3 to 18 C-atoms so that either the .
Type:
Grant
Filed:
April 8, 1999
Date of Patent:
October 3, 2000
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Alfred Jonczyk, Simon Goodman, Beate Diefenbach, Horst Kessler, Marcus Koppitz
