Boehringer Ingelheim International Gmbh

Other

Bing-Shiou Yang

Peter Nickolaus

Soojin Kim

Xudong Wei

Rogelio Perez Frutos

Ulrike Werthmann

Nitinchandra D Patel

Thomas Gabriel Tampone

Jason Alan Mulder

Chris Hugh Senanayake

Pascale A J Pouzet

Frank Himmelsbach

Matthias Eckhardt

Beat Theodor Weber

Xiao-Jun Wang

Joe Ju Gao

Chutian Shu

Stefan Sahli

Monika Brink

Ka Yip

Peter Sieger

Fredrik Lars Nordstrom

Manabu Nakatani

Gisela Bodenbach

Albert Josef Barta

Pascale Arielle Jane-Josee Pouzet

Michael Wiese

Masashi Adachi

Chris Hugh Sananayake

Kenji Egusa

Katrin Baer

Julia Regina Grimm

Roman Christian Messerschmid

Daniela Maria Schroeder

The invention describes a process for reworking of a crystallization product comprising drying and homogenization. The crystallization product is crystalline [5-(methylsulfonyl)-2-{[(2R)-1,1,1-trifluoropropan-2-yl]oxy}phenyl]{(1R,5R)-1-[5-(trifluoromethyl)-1,2-oxazol-3-yl]-3-azabicyclo[3.1.0]hex-3-yl}methanone. The product is dried in a tray dryer or in a pan dryer and subsequently homogenized.

Process of reworking a crystalline form of a glycine transport inhibitor

Intermediate compounds are described herein and which are used to manufacture a crystalline compound 1-cyano-2-(4-cyclopropyl-benzyl)-4-(&#x3b2;-D-glucopyranos-1-yl)-benzene L-proline monohydrate.

Synthesis of 1:1:1 co-crystal of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(&#xdf;-d-glucopyranos-1-yl)-benzene, L-proline and water

Disclosed are solid forms of an inhibitor of glycine transporter-1 (GlyT1). The invention also relates to methods of making these solid forms, pharmaceutical compositions comprising these solid forms, and their use for medical conditions responsive to treatment with an inhibitor of glycine transporter-1.

Solid forms of a GlyT1 inhibitor

The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.

Synthesis of 1:1:1 co-crystal of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(&#x3b2;-D-glucopyranos-1-yl)-benzene, L-proline and water

Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein:

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

This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: 

Crystalline salts of a potent HCV inhibitor

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 novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, 

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Southbury, CT, United States of America

Bing-Shiou Yang