Sepracor, Inc.

Boehringer Ingelheim International Gmbh

Apsinterm LLC

Sunovion Pharmaceuticals Inc.

Zhengxu Han

Dhileepkumar Krishnamurthy

Chris Hugh Senanayake

Derek Pflum

Li Feng Zhang

Frank Himmelsbach

Matthias Eckhardt

Qun Kevin Fang

Chrisantha Hugh Senanayake

Xiao-Jun Wang

Wenjun Tang

Xiufeng Sun

Harold Scott Wilkinson

Zhi-Hui Lu

Christopher Hugh Senanayake

Roger P Bakale

H Scott Wilkinson

Mark A Varney

Thomas Wessel

Surendra Singh

Judy Caron

Stefan G Koenig

Karim Lalji

Xiping Su

Surendra P Singh

Stephen G Koenig

Wilkinson Scott

Stephan G Koenig

The present invention relates to processes for preparing the compounds of general formula I, wherein the groups Rand Rare defined according to claim. Furthermore this inventions relates to intermediates obtained in these processes.

Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein

Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivates and intermediates therein

Disclosed are methods for making chiral phosphorus ligands including chiral phosphines, chiral phosphine oxides, phosphonamides, and aminophosphines. The chiral phosphorus ligands prepared by the methods of the invention are useful as components of chiral catalysts, e.g., transition metal complexes.

Process for making novel chiral phosphorus ligands

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine or trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.

Process for preparation of trans 4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1Napthalenamine

This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.

Method of preparing amine stereoisomers

This invention encompasses novel methods of preparing sulfinamides and sulfoxides, particularly stereomerically pure sulfinamides and sulfoxides. The invention further encompasses novel compounds from which sulfinamides and sulfoxides can be prepared.

Methods of preparing sulfinamides and sulfoxides

This invention provides a method of preparing amine stereoisomers, which comprises stereoselectively reducing a sulfinylimine that bears on the sulfinyl group a residue of an alcohol, thiol or amine, or reacting a sulfinylimine stereoisomer that bears on the sulfinyl group a residue of an alcohol, thiol or amine with a source of a nucleophile, to afford a sulfinylamine stereoisomer, followed by contacting the sulfinylamine stereoisomer with a reagent suitable for the cleavage of a sulfur-nitrogen bond, to afford an amine stereoisomer. It also provides novel intermediates useful in the method, and the use of certain of the intermediates in the preparation of sulfoxide and sulfinylamine stereoisomers.

Methods of making and using racemic and optically pure metabolites of sibutramine, and pharmaceutically acceptable salts, solvates, and clathrates thereof, are disclosed. Pharmaceutical compositions and dosage forms are also disclosed which comprise a dopamine reuptake inhibitor, such as a racemic or optically pure sibutramine metabolite, and optionally an additional pharmacologically active compound.

Methods of treating or preventing pain using sibutramine metabolites

This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.

Methods of preparing didesmethylsibutramine and other sibutramine derivatives

Methods of treating or preventing neuropathic pain using sibutramine metabolites

Salts of sibutramine metabolites, methods of making sibutramine metabolites and intermediates useful in the same, and methods of treating pain

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Shrewsbury, MA, United States of America

Zhengxu Han