Bayer Aktiengesellschaft

Miles Inc.

Miles Laboratories, Inc.

Eugen Schnabel

Gerd Reinhardt

Werner Schroder

Wolfgang Bruns

Ernst-August Auerswald

Herbert Hugl

Dietrich Horlein

Ernst Truscheit

Horst D Schlumberger

Harald Tschesche

Michael Kotick

Gerhard Wolfrum

James Travis

Hans-Volker Runzheimer

A Christopher Skjold

Rainer Schmuck

Herbert Wenzel

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

The present invention relates to new chromogenic amino acid esters and peptide esters of hydroxyisoquinolines and hydroxyquinolines, processes for their preparation and the use of the new esters as substrates for the analytical detection of esterolytic and/or proteolytic enzymes, for example in body fluids, the esters being incorporated into test agents, in particular test strips, in a suitable manner. The new esters are particularly used for the detection of leukocytes, in particular in urine.

Method for detecting esterolytic and proteolytic enzymes

The present invention relates to new chromogenic amino acid esters and peptide esters of hydroxybenzo(iso)thiazoles and hydroxybenzopyrazoles and the use of the new esters as substrates for the analytical detection of esterolytic and/or proteolytic enzymes, for example in body fluids, the esters being incorporated into test agents, in particular test strips, in a suitable manner. The new esters are preferably used for the detection of leukocytes, in particular in urine.

Agents and process for the detection of esterolytic and/or proteolytic

Agent for the detection of esterolytic and/or proteolytic enzymes, containing (a) an amino acid ester or peptide ester of a phenol, as the chromogenic enzyme substrate, and (b) an alcohol as the substance which accelerates the enzymatic cleavage of the amino acid ester bond or peptide ester bond of component (a), characterized in that it contains a salt as the accelerating substance.

Analytical process and agents for the detection of esterolytic and/or

Agent for the detection of esterolytic and/or proteolytic enzymes, containing (a) an amino acid ester or peptide ester of a phenol, as the chromogenic enzyme substrate, and (b) a substance which accelerates the enzymatic cleavage of the amino acid ester or peptide ester bond of component (a), characterized in that it contains a polyamino acid with a molecular weight of between 1,000 and 2,000,000 as the accelerating substance.

The present invention relates to new chromogenic amino acid esters and peptide esters of hydroxybenzo(iso)thiazoles and hydroxybenzopyrazoles, processes for their preparation and the use of the new esters as substrates for the analytical detection of esterolytic and/or proteolytic enzymes, for example in body fluids, the esters being incorporated into test agents, in particular test strips, in a suitable manner. The new esters are preferably used for the detection of leukocytes, in particular in urine.

Chromogenic amino acid esters and peptide esters

The invention relates to homologs of aprotinin with, in place of lysine, other amino acid moieties in position 15, methods for their preparation and their use as proteinase inhibitors.

Homologues of aprotinin with, in place of lysine, other aminoacids in

The invention relates to N-carboxyacylaminoacid esters, a process for their production and their use as chromogenic substrates for the continuous and discontinuous determination of enzymes with a chymotrypsin-like specificity, in particular catheepsin G.

N-Carboxyacylaminoacid esters, processes for their production and their

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.

Growing community of inventors

Wuppertal, Germany

Eugen Schnabel