The Medicines Company (leipzig) Gmbh

Dsm IP Assets B.v.

Curacyte Ag

The Medicines Company

Jörg Stürzebecher

Torsten Steinmetzer

Andrea Schweinitz

Hugo Ziegler

Peter Wikstroem

Claudia Reichelt

Alexander Schulze

Friedrich-Alexander Ludwig

Mohammed Daghish

Jochen Heinicke

Silke Nicklisch

Anne Stürzebecher

Daniel Dönnecke

Mohammed Daghisch

Kerstin Uhland

Dagmar Prasa

Sebastian Künzel

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 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 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 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 invention relates to compounds of general formula (I) and acid addition salts thereof, where the various symbols have the meanings given in the description and claims, the production and use thereof as substrate for the detection of TAFIa, a fibrinolysis inhibiting enzyme. The detection occurs by using the absorption between 400 and 412 nm, arising as a result of the formation of 3-carboxy-4-nitrothiophenol from Ellman's reagent as a function of time. 

Substrates for TAFI (A)

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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Erfurt, Germany

Jörg Stürzebecher