The Medicines Company (leipzig) Gmbh

Curacyte Ag

Other

National Research Council of Canada

Philipps-Universität Marburg

Haemosys Gmbh

The Medicines Company

Jenaffin Gmbh

Torsten Steinmetzer

Andrea Schweinitz

Joerg Stuerzebecher

Jörg Stürzebecher

Claudia Reichelt

Alexander Schulze

Friedrich-Alexander Ludwig

Jochen Heinicke

Andreas Van De Locht

Anett Soeffing

Peter Steinmetzer

Silke Nicklisch

Mohammed Daghish

Sebastian Saupe

Anne Stürzebecher

John DiMaio

Feng Ni

Yasuo Konishi

Götz Nowak

J&ouml;rg St&uuml;rzebecher

Wolfgang Garten

Sebastian Künzel

Kerstin Uhland

Anne Stuerzebecher

Daniel Doennecke

Daniel Dönnecke

Mohammed Daghisch

Mikhail Matrosovich

Gero Becker

Daniel Donnecke

Frank Sielaff

Eva BÖTTCHER

Catharina Freuer

Tatyana Matrosovich

Sebastian Martin Saupe

Anett Söffing

The invention relates to the use of acylated 4-amidino- or 4-guanidinobenzylamine in accordance with the general formula IP4-P3-P2-P1&#x2003;&#x2003;(I),where P4 is a monosubstituted or polysubstituted or unsubstituted benzylsulfonyl group, P3 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural &#x3b1;-amino acid or &#x3b1;-imino acid in the D configuration, P2 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural &#x3b1;-amino acid or &#x3b1;-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.

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

The invention relates to peptide mimetics comprising the residues P4-P3-P2-P1, which were cyclized between the side chains of P3 and P2 amino acid and are, as inhibitors of the serine protease plasmin, suitable to be used to inhibit fibrinolysis and thus to reduce blood loss in hyperfibrinolytic conditions, for example during surgery.

Cyclic tripeptide mimetics as plasmin inhibitors

The invention relates to the novel base-substituted benzylamine analogs of general formula (I), wherein A represents P-Pwith P&#x2550;(A) and P&#x2550;(B), for use as coagulation factor Xa inhibitors. The invention also relates to the production and use of said analogs in the therapy and prophylaxis of cardiovascular diseases and thromboembolic events. 

Base-substituted benzylamine analogs for use as coagulation factor Xa inhibitors, the production and use thereof

The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives. 

Serine protease inhibitors

The invention refers to multibasic, N-terminally modified tetrapeptide mimetics with a C-terminal P1-arginine mimetic, methods for their production and use for therapy and prophylaxis of diseases, caused by bacterial pathogens or viruses, as well as for therapy and prophylaxis of diabetes, arteriosclerosis, cancer, Alzheimer's or the onset of obesity, as well as the use of these compounds as inhibitors of the proprotein convertases which cleave behind basic P1 residues, especially for inhibition of the protease furin.

N-terminally modified tetrapeptide derivatives having a C-terminal arginine mimetic

The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.

Meta-substituted phenyl sulfonyl amides of secondary amino acid amides, the production thereof, and use thereof as matriptase inhibitors

The invention relates to inhibitors of trypsin-like serine proteases, including those of the general formula (IV) which, as well as plasmin, also inhibit plasma kallikrien, and to their use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.

Trypsin-like serine protease inhibitors, and their preparation and use

The invention relates to novel inhibitors of urokinase and to their preparation and use for the therapy, prophylaxis and diagnosis of a tumor, in particular for reducing the formation of tumor metastases.

Urokinase inhibitors, production and use thereof

The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrein, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.

The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrien, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.

2-(Aminomethyl)-5-chlorobenzylamide derivatives and their use as inhibitors of coagulation factor Xa are provided. The compounds are suitable for the treatment and prophylaxis of cardiovascular and thrombotic events.

2-(aminomethyl)-5-chlorobenzylamide derivatives and their use as inhibitors of the clotting factor Xa

The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.

N-sulphonylated amino acid derivatives, method for the production and use thereof

The present invention relates to novel covalent oligo and polyalkylene glycol conjugates with synthetic inhibitors of trypsin-type serine proteases, in particular inhibitors of the hemocoagulation protease thrombin, synthetic intermediates stages required in their production and their use for producing active ingredients for the treatment or prophylaxis of thrombotic complications.

Oligo or polyalkylene glycol-coupled thrombin inhibitors

The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for treating cardiovascular diseases and thrombotic events.

Inhibitors for the blood-clotting factor Xa

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Jena, Germany

Torsten Steinmetzer