Peptidic sulfonamides

US7759302B2 · kind B2 · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Alfred Jonczyk · Darmstadt, DE
• Ulrich Groth · Oettingen, DE
• Gunther Zischinsky · Berlin, DE

Key dates

• Filing date: Jan 14, 2004
• Grant date: Jul 20, 2010
• Expiry date: May 13, 2025

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to novel peptides which are biologically active as ligands of blood platelet integrin GPIIbIIIa and the αv integrins, preferably the avβs 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, OR3NH2, 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.