Sanofi-a Ventis Deutschland Gmbh

Solvay Pharmaceuticals, Gmbh

Bernd Junker

Wendelin Frick

Guenter Billen

Gerhard Jaehne

David William Will

Javier Manero

Timo Heinrich

Andreas Lindenschmidt

Jochen Antel

Wolfgang Holla

Ulf Preuschoff

Heiner Jendralla

Joachim-Heiner Jendralla

Frank Zocher

Stephane Mutti

Berndt Kulitzscher

Jochen Hachtel

Andreas Burgard

Thomas Stuedemann

Theodor Andreas Wollmann

Christoph Tappertzhofen

Christophe Salagnad

Claus-Jügen Maier

Theodor Andreas Wollman

Rolf Hoerlein

David Rigal

Michael Reggelin

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

Provided are compounds of formula A and formula I: A compound of formula A: wherein n is an integer from 6 to 17 anda compound of formula I: 

Esters of pentahydroxyhexylcarbamoyl alkanoic acids

The present invention is a process for the preparation of diphenylazetidinone derivatives of the formula (I) or forms thereof comprising the substituents X, Rand/or Ras defined herein. More specifically, the invention comprises methods for the preparation of these compounds by cyclization of certain &#x3b2;-amino carboxamides or &#x3b2;-amino carboxylic esters. These diphenylazetidinone compounds are useful in the treatment of high blood serum cholesterol levels and the maintenance of the reduced cholesterol levels achieved thereby. 

Process for the preparation of diphenyl azetidinone derivatives

The present invention is directed to the preparation of novel compounds useful in the treatment of hyperlipidemia, arteriosclerosis, hypercholesterolemia, and other related metabolic disorders. More specifically, the present invention is a novel process for the preparation of 1,4-diphenylazetidinone derivatives from &#x3b2;-substituted amino amides which are protected in the presence of silylating agents and at least one cyclization catalyst whose structural formula is represented by one of the general formula: wherein the various R-groups are defined herein.

Method for producing 1,4-diphenyl azetidinone derivatives

A method for stereochemically controlled production of azacyclic compounds of general formula (I)in which the substituents have the meanings given in the specification. The invention also relates to intermediate products of this method and to novel azacyclenes.

Method for stereochemically controlled production of isomerically pure highly substituted azacyclic compounds

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Bad Soden, Germany

Bernd Junker