Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Jason Alan Mulder

Rogelio Perez Frutos

Thomas Gabriel Tampone

Chris Hugh Senanayake

Nitinchandra D Patel

Peter Nickolaus

Soojin Kim

Xudong Wei

Ulrike Werthmann

Bing-Shiou Yang

Pascale A J Pouzet

Dhileepkumar Krishnamurthy

Joe Ju Gao

Xingzhong Zeng

Jinhua Jeff Song

Sonia Rodriguez

Chris H Senanayake

Jean-Nicolas Desrosiers

Keith R Fandrick

Pascale Arielle Jane-Josee Pouzet

Chris Hugh Sananayake

Rogelio P Frutos

Pascale Aj Pouzet

Nitinchandra Patel

Thomas G Tampone

Keith R Fandrik

Jinhau J Song

Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein:

Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma

The present invention relates to a process of making a compound of formula (XII) or (XIIA): wherein R,R, Rand X are as defined herein. 

Process for preparing carboxylic acids

The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms andwherein R is Cl andwherein R may be located either in the para-, meta- or ortho-position of Ring A,wherein S* is a sulphur atom that represents a chiral center,and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.

The present invention relates to a process of making a compound of formula (I): Wherein, R, R, Rand X are as defined herein.

Process for preparing carboxamidine compounds

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 invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, 

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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New Milford, CT, United States of America

Jason Alan Mulder