Bayer Aktiengesellschaft

Horst D Schlumberger

Ernst Truscheit

Eugen Schnabel

Gerd Reinhardt

Robert Bierling

Harald Tschesche

Harold Tschesche

Herbert F Oettgen

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, glomerulonephritides, rheumatoid arthritis and other collagenoses caused by immune complexes and also arthritides caused by deposits due to metabolic processes (gout), but also degenerative changes in the elastic elements of vascular walls (arterioscleroses) or in the lung (pulmonary emphysema).

Derivatives, having an inhibitory action against protease and an

A water soluble immunopotentiating agent is derived from yeast cell wall material, including mechanically disrupted yeast cell walls, proteolyzed yeast cell wall material and carbohydrate-protein complexes found in yeast cell wall material, through extraction with a water-phenol mixture. The water soluble agent is isolated from the water phase and can be further purified, as through dialysis, to remover low molecular weight components.

Process for the preparation of immunopotentiating agents from components

A demaino kallikrein-trypsin inhibitor obtained from cattle organs is characterized by (a) 0 to 3 lysine residues and/or 3 to 6 arginine residues and/or 1 to 4 tyrosine residues; (b) the 10- and/or 21-tyrosine residues being unsubstituted or substituted by at least one nitro, nitroso or amino in the ortho position relative to the phenolic hydroxy group; and (c) having protease inhibitory activity of BPTI and elastase inhibition activity.

Deamino derivatives of the kallikrein-trypsin inhibitor

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Wuppertal, Germany

Horst D Schlumberger