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US 5,849,692 AGranted
Cyclic peptides containing Arg-Gly-Asp, and derivatives thereof, as adhesion inhibitors
AssigneeMerck Patent GmbH
InventorsAlfred Jonczyk, Gunter Holzemann, Brunhilde Felding-Habermann, Friedrich Rippmann, Beate Diefenbach, Horst Kessler, Roland Haubner, Jochen Wermuth
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Abstract
The invention relates to novel cyclopeptides of the formula I cyclo-(Arg-B-Asp-D-E) I in which B, D, and E have the meanings defined herein, and their salts. These compounds act as integrin inhibitors and can be used, in particular, for the prophylaxis and treatment of disorders of the circulation and in tumor therapy.
Claims18
A cyclopeptide compound of formula I
- cyclo-(Arg-B-Asp-D-E) I,
- wherein:
- B is Gly, Ala, or--HN--Q--CO--;
- D is Phe, 4-Hal-Phe, Nal, or Phig;
- E is Gly, Ala, Lys, Lys(Ac), Lys(AcNH.sub.2), or Lys(AcSH);
- Hal is F, Cl, Br, or I;
- Q is alkylene having 1-6 C atoms;
- and
- Ac is alkanoyl having 1-10 C atoms,
- wherein critically active amino acids or amino acid derivatives can be in either the D or L form, or a physiologically acceptable salt thereof, with the proviso that said compound is not cyclo-(Arg-Gly-Asp-Phe-Val) or cyclo-(Arg-Ala-Asp-Phe-Val) in which optically active amino acids can be in either the D or L form.
7 more elements
A cyclopeptide compound, wherein said compound is:
- (a) cyclo-(Arg-Gly-Asp-D-Phe-Gly) or a physiologically acceptable salt thereof,
- (b) cyclo-(Arg-Gly-Asp-D-Phe-Lys) or a physiologically acceptable salt thereof,
- (c) cyclo-(Arg-Gly-Asp-D-Phe-Phe) or a physiologically acceptable salt thereof,
- or
- (d) cyclo-(Arg-Gly-Asp-Phe-Gly) (SEQ ID:NO;1) or a physiologically acceptable salt thereof.
2 more elements
Dependencies are inferred from the claim text.