Boehringer Ingelheim International Gmbh

Sepracor, Inc.

Apsinterm LLC

Boehringer Ingelheim Pharmaceuticals, Inc.

Boehringer Ingelheim Pharma Gmbh & Co Kg

Dhileepkumar Krishnamurthy

Zhengxu Han

Chris Hugh Senanayake

Li Feng Zhang

Xiao-Jun Wang

Rogelio Perez Frutos

Derek Pflum

Frank Himmelsbach

Matthias Eckhardt

Qun Kevin Fang

Chrisantha Hugh Senanayake

Wenjun Tang

Xiufeng Sun

Harold Scott Wilkinson

Zhi-Hui Lu

Sonia Rodriguez

Thomas Gabriel Tampone

Jason Alan Mulder

Christopher Hugh Senanayake

Richard John Varsolona

Thomas Nicola

Nitinchandra D Patel

Laurence John Nummy

Thomas Wirth

Yibo Xu

Jutta Kroeber

Magnus Carl Arne Eriksson

Diana Reeves

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

The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO, preferably SO, and wherein R, R, R, R, Rand Rhave the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product. 

Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein

The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.

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The present invention is related to a process of preparing substituted 2-amino-5-(5-(heterocyclemethyl)pyridin-2-yloxy)benzoic acid compound of formula (I) or a salt thereof, 

Process for preparation of substituted 2-amino-5-(5-(heterocyclemethyl)pyridin-2-yloxy)benzoic acid

Disclosed are processes for making compounds containing 4- and 5-imidazolyl rings, also disclosed are the intermediates useful in the processes disclosed herein.

Process for making cytokine inhibiting compounds containing 4- and 5-imidazolyl rings and the intermediates thereof

Disclosed is a multi-step process for preparing a compound of Formula I: wherein Rto Rare as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.

Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides

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

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Brookfield, CT, United States of America

Dhileepkumar Krishnamurthy