Sanofi

Volker Kraft

Kai Rossen

Gerhard Kretzschmar

Klaus Wirth

Werngard Czechtizky

Olaf Ritzeler

John Weston

Hermut Wehlan

Petra Arndt

Nils Rackelmann

Heinz Goegelein

Oliver Plettenburg

Antony Bigot

Gary Mccort

Guenter Billen

Thomas Olpp

Simon Gessler

Joachim Graeser

Patrice Bellevergue

Michael Podeschwa

Veronique Crocq-Stuerga

Joachim Gräser

Véronique Crocq-Stuerga

The present invention relates to substituted chroman-6-yloxy-cycloalkanes of the formula (I) in which Ar, R1 to R4, p and q are as defined in the claims. The compounds of the formula (I) are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them. 

Substituted chroman-6-yloxy-cycloalkanes and their use as pharmaceuticals

The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals

The present invention relates to a process for the preparation of a compound of the formula I,  

Process for the preparation of a compound useful as an inhibitor of TAFIa

The present invention relates to a process for making 6-substituted-1-(2H)-isoquinolinone derivatives of formula (I) wherein R1 and n are as described in the specification. The present invention further relates to novel intermediates which are used in the process according to the invention and to processes for preparing such intermediates.

Process for the preparation of 6-substituted-1-(2H)-isoquinolinones

A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.

Process for the production of benzofurans

A process for the production of Dronedarone intermediates of the formula (I), by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-(4-methoxyphenyl)-ethanone, subsequent treatment of the ester with bases and a zeolite (alumosilicate) catalyst and optional subsequent demethylation. This process can be used for the production of Dronedarone. 

Process for the production of dronedarone intermediates

This application relates to a process for the production of (2R)-dihydroartemisinic acid or (2R)-dihydroartemisinic acid esters from artemisinic acid or artemisinic acid esters, respectively, by diimine hydrogenation of the exocyclic CC-double bond, and use of said process in the production of the antimalarial drug artemisinin.

Process for the production of artemisinin intermediates

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Frankfurt am Main, Germany

Volker Kraft