Dsm IP Assets B.v.

Wilex Ag

Pentapharm Ag

Peter Wikstroem

Hugo Ziegler

Helmut Vieweg

Jonathan Alan Medlock

Christine Mendrok-Edinger

Lars G Svendsen

Eileen Jackson

Dominik Imfeld

Jörg Stürzebecher

Jürgen H Vollhardt

Stéphanie Boudon

Eliane Ursula Wandeler

Rainer Voegeli

Rolf Schuetz

Dominic Imfeld

Dagmar Prasa

Christian Ludin

Andreas Schulze

Christoph Adler

Joerg Stuerzebecher

Jürgen Herbert Vollhardt

Christine Mendrok-edinger

This invention relates to compounds that are selective inhibitors of Matrix Metalloprotease-12 (MMP-12), to cosmetic and pharmaceutical compositions containing them, and to their use in the prevention and/or treatment of ailments associated with MMP-12. Formula (I). 

Phosphinic peptide derivatives for use as MMP-12 inhibitors

The present invention is related to a novel and improved process for the manufacture of compounds of formula (I) or salts thereof herein designated as benzylsulfonyl-Ser-X-4-amidinobenzylamide, wherein R is a Cto Clinear or branched aliphatic hydrocarbon chain optionally substituted with a Cto Caromatic group. 

Process for the production of a dipeptide derivative

The present invention relates to the use of p-hydroxybenzylamine or a salt thereof as antimicrobial agent as well as to composition comprising said agent.

Compositions comprising P-hydroxybenzylamine

The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (Hor ammoniumformiateformate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

Method for producing 3-amidinophenylalanine derivatives

The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (Hor ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

Topical application agents against mimic and age-related wrinkles

The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidinophenylalanine derivatives under gentle conditions (Hor ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

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 present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidinophenylalanine derivatives under gentle conditions (Hor ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H, Pd/C, AcOH or HOI/ethanol, 1&#x2013;3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

The invention relates to oligopeptide derivatives whose C-terminal amino acid is arginine which is linked to the remainder of an electroactive aniline or aminoquinoline derivative by an amide bond. The oligopeptide derivatives are split by enzymes of the class of peptide hydrolases, especially proteinases and their inhibitors, of the coagulation system, the fibrinolytic system and the complement system. These oligopeptide derivatives serve as substrates for quantitatively determining such enzymes, especially thrombin, in complex sample liquids, especially capillary blood. This determination is carried out by measuring the increase in the water-soluble amperogenic aniline or aminoquinoline compound. The oligopeptide derivatives and their salts can be produced according to usual methods in peptide chemistry.

Growing community of inventors

Gipf-Oberfrick, Switzerland

Peter Wikstroem