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US 5,693,612 AGranted
Cyclopeptides of the formula I
AssigneeMerck Patent GmbH
InventorsAlfred Jonczyk, Gunter Holzemann, Simon Goodman, Horst Kessler, Roland Haubner, Jochen Wermuth
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Abstract
The invention relates to novel cyclopeptides of the formula I cyclo-(Arg-A-Asp-R.sup.1 -R.sup.2) I in which A, R.sup.1 and R.sup.2 have the meaning given in claim 1, 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, bones and in tumour therapy, and as antimicrobial and antiviral active compounds.
Claims9
A cyclopeptide compound according to formula I
- cyclo-(Arg-A-Asp-R.sup.1 -R.sup.2) I
- wherein
- A is Gly or Ala;
- R.sup.1 is a 2-carboxy-8-amino-4-thiapiperolidin-9-one (Btd) group;
- o-aminomethyl-o'-carboxybiphenyl (Biph) group;
- 2-aminomethyl-5-carboxymethyl-thiophene (Act) group;
- 2-(1,7-diazaspiro-4,4!nonan-7-yl)-4-methylpentanoic acid ((S,S)spiro-Pro-Leu) group;
- or 2-(3-amino-1-pyrrolid-2-onyl)-4-methyl-pentanoic (S)GlyANC-2!-Leu or (R)GlyANC-2!-Leu) group;
- where the R.sup.1 group is bonded by a peptide bond to the Asp
- and
- R.sup.2 is absent, or else is Val, or a physiologically acceptable salt.
8 more elements
Dependencies are inferred from the claim text.