Peptidic sulfonamides
AssigneeMerck Patent GmbH
InventorsAlfred Jonczyk, Ulrich Groth, Gunther Zischinsky
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Abstract
The invention relates to novel peptides which are biologically active as ligands of blood platelet integrin GPIIbIIIa and the αv integrins, preferably the αvβs and αvβ3 integrin, having the formula (I): R1-Arg-X-Asp-Leu-Asp-Ser-Leu-Arg-R2 (I), in which R1 denotes H, acetyl or acyl and R2 denotes -Oh, OR3 NH2,NHR3, N(R3)2 R3 denotes atkyl, aralkyl, aryl, Het and X denotes an amino acid of the formula (II), in which A denotes (CH2)n R4 denotes H, alkyl, aralkyl or aryl, and n denotes 1, 2, 3, 4, 5 or 6, and the amino acid of the formula (II) is bonded to the adjacent Arg via a peptide bond of the α-amino group and to the α-amino group of the adjacent Asp via a peptide bond of the α-carboxyl group.
Claims9
Peptidic compounds of the formula I
- R1-Arg-X-Asp-Leu-Asp-Ser-Leu-Arg-R2 I
- in which
- R1 denotes H, acetyl or acyl and
- R2 denotes —OH, OR3 NH2,NHR3, N(R3)2
- R3 denotes alkyl, aralkyl, aryl, Het and
- X denotes an amino acid of the formula II
- in which
- A denotes (CH2)n
- R4 denotes H, alkyl, aralkyl or aryl, and
- n denotes 1, 2, 3, 4, 5 or 6,
- and the amino acid of the formula II is bonded to the adjacent Arg via a peptide bond of the α-amino group and to the α-amino group of the adjacent Asp via a peptide bond of the α-carboxyl group, and pharmaceutically usable prodrugs, derivatives, solvates, stereoisomers thereof and salts thereof, including mixtures thereof in all ratios.
Dependencies are inferred from the claim text.