Bayer Aktiengesellschaft

Gerd Reinhardt

Eugen Schnabel

Werner Schroder

Wolfgang Bruns

Ernst-August Auerswald

Dietrich Horlein

Ernst Truscheit

Horst D Schlumberger

Michael Kotick

Elisabeth Perzborn

Friedel Seuter

Horst Boshagen

Ulrich Horlein

Harald Tschesche

Harold Tschesche

Peptides having essentially the sequence of bovine pancreatic trypsin inhibitor (aprotinin) wherein one or more of the amino acids at positions 15, 16, 17, 18, 34, 39 and 52 are replaced by any naturally occurring amino acid produced by recombinant DNA technology, process, expression vector and recominant host therefor and pharmaceutical use thereof. Such peptides being useful as therapeutic agents in diseases connected with the presence of excessive amounts of proteinases.

Variants of bovine pancreatic trypsin inhibitor produced by recombinant

Variants of bovine pancreatic trypsin inhibitor and pharmaceutical use

Microbially produced aprotinin and aprotinin homologs used for treating patients suffering from an excess release of pancreatic elastase, serum elastase or leukocyte elastase.

Homologs of aprotinin produced from a recombinant host, process,

Homologs of aprotinin produced from a recombinant host, process

An ether derivative of a dihydroxybenzene of the formula ##STR1## in which R.sup.1 is 1 to 3 identical or different substituents selected from hydrogen, halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto and carbalkoxy, with in each case 1 to 4 carbon atoms in the alkyl and alkoxy groups, and

Thrombin inhibitory new dihydroxybenzene ether derivatives

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 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

Gerd Reinhardt