Boehringer Ingelheim International Gmbh

Other

Boehringer Ingelheim Pharma Gmbh & Co Kg

Thomas Gabriel Tampone

Rogelio Perez Frutos

Jason Alan Mulder

Chris Hugh Senanayake

Peter Nickolaus

Soojin Kim

Xudong Wei

Ulrike Werthmann

Bing-Shiou Yang

Nitinchandra D Patel

Sonia Rodriguez

Pascale A J Pouzet

Dhileepkumar Krishnamurthy

Jon Charles Lorenz

Pengtao Zhang

Phouvieng Beyer

Kanwar Pal Singh Sidhu

Jolaine Savoie

Joshua D Sieber

Li Feng Zhang

Jun Wang

Jun Li Wang

Weitong Dong

Zhulin Tan

Laurence John Nummy

Joshua Daniel Sieber

Laurence J Nummy

Li Mei Zhang

Jason Brazzillo

Magnus C Eriksson

Pascale Arielle Jane-Josee Pouzet

Bjoern Stahl

Michael Klumb

Frederic Gerard Buono

Bernd Werner

Andrew T Brusoe

Tobias Alt

Magnus Eriksson

Jason A Brazzillo

Chris Hugh Sananayake

June Wang

The present invention relates to compounds of (II) and an acceptable salt or hydrate thereof method of making same.

Intermediate compounds and methods

This invention relates to a novel continuous process for making alkyl 7-amino-5-methyl-[1,2,5]-oxadiazolo¬[3,4-b]pyridine-carboxylate, wherein R is C-alkyl. The process of the invention present invention overcomes disadvantages of processes of the prior art by avoiding the highly energetic intermediates, using readily available and inexpensive starting materials and reagents, and avoiding the isolation of intermediates. The process according to the invention is suitable for use on industrial scale.

Continuous process for manufacturing alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-carboxylate

The present invention relates to compounds of (II) and an acceptable salt or hydrate thereof method of making same. 

Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein:

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

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 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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Southbury, CT, United States of America

Thomas Gabriel Tampone