Sandoz Ag

Biochemie Gesellschaft M.b.h

Sandoz Gmbh

Biochemie Gesellschaft

Biochemie Gmbh

Hubert Sturm

Johannes Ludescher

Josef Wieser

Gerd Ascher

Peter Kremminger

Martin Albert

Dominic De Souza

Werner Veit

Siegfried Wolf

Kerstin Knepper

Ulrich Griesser

Arthur Pichler

Andreas Berger

Martin Decristoforo

Heinrich Thaler

Andreas Hotter

Christoph Langes

Bernhard C Prager

Hannes Lengauer

Thorsten Wilhelm

Martin Langner

Nolwenn Martin

Joerg Salchenegger

Robert Ziegert-Knepper

Michael Oberhuber

Roland Barth

Hans-Peter Spitzenstaetter

Katja Vorndran

Mairi Haddow

Ludwig Miller

Robert E Ziegert-Knepper

Elfriede Klingler

Jörg Salchenegger

Hans-Peter SPITZENSTÄTTER

The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of this process.

Process for preparing ceftaroline fosamil

The present invention relates to novel crystalline forms of ceftaroline fosamil and to methods for their preparation. Furthermore the present invention relates to the use of the novel forms of ceftaroline fosamil for the preparation of an antibiotic medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel forms of ceftaroline fosamil and to methods of preparing the same. Finally the present invention relates to pharmaceutical combinations comprising an effective amount of the novel forms of ceftaroline fosamil and &#x3b2;-lactamase inhibitors.

Crystalline forms of ceftaroline fosamil

The present invention relates to a novel process for preparing ceftaroline fosamil via intermediates of Formulae (1), (3) or (4) of this process. 

Provided are a crystalline dihydrate of Rivaroxaban, processes for the preparation thereof, pharmaceutical compositions containing the crystalline dihydrate and processes for preparing and storing the pharmaceutical compositions. Also provided are a crystalline formic acid solvate of Rivaroxaban, processes for the preparation of crystalline Rivaroxaban formic acid solvate and the use of the Rivaroxaban formic acid solvate in the manufacture of the crystalline dihydrate of Rivaroxaban.

Crystalline form of rivaroxaban dihydrate

The present invention relates to methods for the preparation of a compound having the formula (X). Individual reaction steps as well as intermediates are additionally claimed. 

Method for the preparation of substituted oxazolidinones

The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of Formulae (1), (3) or (4) of this process. 

The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1'-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3&#x2032;]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.

Method for the production of ceftobiprole medocaril

A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y&#x2014;NH; of formula (IIa) 0=C&#x2550;N&#x2014;Yand/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V). 

Process for the preparation of chiral triazolones

The present invention relates to a process for the purification of crude bimatoprost to obtain pure bimatoprost comprising a chromatography, preferably a chromatography using an achiral stationary phase and an eluent comprising an alcohol and an apolar solvent; and crystallization of the product obtained the chromatography to obtain pure bimatoprost.

Process for the production of bimatoprost

The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed. 

Method for the preparation of rivoraxaban

The present invention relates to an improved process for the production of prostaglandins and prostaglandin analogs. In particular, this invention relates to the production of prostaglandins of the PGF-series, including latanoprost, travoprost, and bimatoprost, which are active pharmaceutical ingredients used for the reduction of elevated intra-ocular pressure in patients with glaucoma and ocular hypertension.

Process for the production of prostaglandins and prostaglandin analogs

This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.

Carbonyl asymmetric alkylation

The present invention relates to acid addition salts of aripiprazole, a process for preparing said acid addition salts and their use to prepare or purify aripiprazole in the form of a free base or in the form of a pharmaceutically acceptable salt.

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Innsbruck, Austria

Hubert Sturm