Derivatives, having an inhibitory action against protease and an antiphlogistic action, of the trypsin-kallikrein inhibitor obtained from cattle organs (BPTI), their preparation and their use as medicaments

US4153687A · kind A · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

• Eugen Schnabel · Wuppertal, DE
• Gerd Reinhardt · Kelkheim, DE
• Horst D. Schlumberger · Wuppertal, DE
• Ernst Truscheit · Häger, DE
• Harold Tschesche · Siegen, DE

Key dates

• Filing date: Nov 2, 1977
• Grant date: May 8, 1979
• Expiry date: Nov 2, 1997

Classification

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

Abstract

The invention provides derivatives of kallikrein-trypsin inhibitor (BPTI) in which one or both of the 10- or 21-tyrosine residues are linked, in the o-position relative to the phenolic hydroxyl group, to an aptionally substituted carbocyclic or heterocyclic aromatic radical via an azo group and the other if only one of the said residues is substituted is either unsubstituted or carries a nitro group or an amino group in the o-position relative to the phenolic hydroxyl group. The azo-BPTI derivatives of the invention can be used, as medicaments for the therapy of diseases which are caused either by over-production of proteases as a result of increased liberation from the zymogens or of release during cell decomposition or by a deficiency or lack of natural indogenous inhibitors of these enzymes in organs and tissue fluids. Diseases which have this type of etiology are the various forms of shock and post-traumatic or post-operative complications, disorders in blood clotting and acute and chronic inflammatory reactions and, in particular, also chronic inflammatory reactions with necrotic and degenerative damage to connective tissue, such as pancreatitis and also vasculitides, glomerul…