Acylated 4-amidino- and -4-guanidinobenzylamines for inhibition of plasma kallikrein

US9365613B2 · kind B2 · utility

Assignee

• THE MEDICINES COMPANY (LEIPZIG) GMBH · DE

Inventors

• Jörg Stürzebecher · Erfurt, DE
• Torsten Steinmetzer · Jena, DE
• Andrea Schweinitz · Jena, DE

Key dates

• Filing date: Jan 15, 2004
• Grant date: Jun 14, 2016
• Expiry date: Mar 11, 2027

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K5/06095
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to the use of acylated 4-amidino- or 4-guanidinobenzylamine in accordance with the general formula IP4-P3-P2-P1  (I),where P4 is a monosubstituted or polysubstituted or unsubstituted benzylsulfonyl group, P3 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural α-amino acid or α-imino acid in the D configuration, P2 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural α-amino acid or α-imino acid in the L configuration, and P1 is a monosubstituted or polysubstituted or unsubstituted 4-amidino- or 4-guanidinobenzylamine group, for inhibiting plasma kallikrein (PK), factor XIa and factor XIIa, in particular for preventing the activation of coagulation at synthetic surfaces and for systemic administration as anticoagulants/antithrombotic agents, in particular for preventing the activation of coagulation at synthetic surfaces for the purpose of averting thromboembolic events.