Sanofi-a Ventis Deutschland Gmbh

Roche Diagnostics Operations, Inc.

Roche Diagnostics Gmbh

F. Hoffmann-la Roche Ag

Frank Zocher

Paul Habermann

Christophe Salagnad

Erhard Kopetzki

Rainer Mueller

Wolfgang Holla

Sebastian Rissom

Stephane Mutti

Frank Geipel

Heinrich Decker

Berndt Kulitzscher

Stephan Glaser

Bernd Junker

Jochen Hachtel

Andreas Burgard

Thomas Stuedemann

Wolfgang Laux

Christoph Tappertzhofen

Rainer Gauler

Oliver Maneg

Claus Lattemann

Christoph Hoh

Rolf Hoerlein

Claus-Jügen Maier

Rudolf Lehnert

Hans-Wolfram Flemming

Holger Berk

Laure Landric-Burtin

Laure Landric-Burtain

Stéphane Mutti

The invention relates to a method for producing C-terminal amidated dibasic or polybasic peptides, consisting in reacting two peptides in the presence of trypsin biologically active enzymes and, if necessary, in purifying the thus obtainable compounds of formula (I) by means of protein chemistry.

Method for amidating polypeptides with basic amino acid C-terminals by means of specific endoproteases

The invention relates to a method for producing a type of insulin by genetically engineering a precursor thereof and converting said precursor to the respective insulin in an enzyme-catalyzed ligation reaction with lysine amide or arginine amide, or by lysine or arginine which is modified by protective groups, and optionally subsequent hydrolysis.

Method for producing insulin analogs having a dibasic B chain terminus

An improved method for preparing ramipril is disclosed, and also an intermediate for use in the method.

Method for the production of ramipril

The invention relates to insulin glargine which is modified by amidation, especially Gly(A21), Arg(B31), Arg amide (B32) human insulin (insulin glargine amide).

Amidated insulin glargine

The present invention relates to the production of a variant of recombinant trypsin with increased substrate specificity for arginine versus lysine in non-animal host organisms. Moreover, the present invention relates to a variant of recombinant trypsin and their production. Also provided are use of recombinant porcine pancreatic trypsin variants for cleavage of precursors of insulins, and kits containing the variant of trypsin.

Cleavage of precursors of insulins by a variant of trypsin

The invention relates to the production of carboxy-terminal (C-terminal) amidified peptides with C-terminal amidified lysin, in particular with the biological activity of GLP-1, the chemical and/or biotechnological precursors and intermediate products thereof. The invention also relates to a method for the production and use thereof for producing pharmaceutical products.

Method for producing carboxy-terminal-amidified peptides

The invention relates generally to a process for preparing diarylcycloalkyl derivatives of the formula (I). wherein the respective R-group substituents are defined herein. These compounds of formula (I) are activators for peroxisome proliferator-activated receptors (PPAR activators) which are useful in the therapeutic treatment of a number of diseases and disorders of the central nervous system such as multiple sclerosis, Parkinson's Disease, psychiatric disorders and the like. The present invention is a novel process for preparing PPAR activators of the formula (I) which do not have the disadvantages of the processes known in the prior art. In particular, a process is provided with which the PPAR activators of formula (I) can be prepared in a suitable enantiomeric excess, i.e. high enantioselectivity, without the need for subsequent chiral chromatography.

Method for the production of diarylcycloalkyl derivatives

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Frankfurt am Main, Germany

Frank Zocher