Boehringer Ingelheim International Gmbh

Centrexion Therapeutics Corporation

Markus Ostermeier

Guenther Huchler

Ulrike Werthmann

Peter Sieger

Marco Santagostino

Juergen Daeubler

Eugene R Hickey

Doris Riether

David S Thomson

Waldemar F Pfrengle

Renee M Zindell

Lifen Wu

Alessandra Bartolozzi

Achim Sauer

Angela Kay Berry

Monika Ermann

Stephen East

Innocent Mushi

Nigel James Blumire

Patricia Amouzegh

Someina Khor

Stephan Kling

Frank Himmelsbach

Birgit Jung

Stefan Peters

Guenter Linz

Tobias Wunberg

Werner Rall

Anke Baum

Heiner Ebel

Juergen Ramharter

Heinz Stadtmueller

Rolf Schmid

Ralf Lotz

Janus Schreiber Larsen

Gerd Kraemer

Christiane Kofink

Dorothea Ingrid Rudolph

Markus Frank

Stefan Goepper

Annika Gille

Joerg Jung

Yunhai Cui

Oliver Hucke

Florian Binder

Torsten Busch

Marco Hans Hofmann

Michael Gmachl

Riccardo Giovannini

Eugene Richard Hickey

Stephen Peter East

Zeno A Leuter

Julian Wippich

Radoslaw Lipinski

Fabio Savarese

Alexandre Perera

Sven Anklam

Stefan Braith

Claudia Ochs

Waldermar Pfrengle

Florian Montel

Stefan Scheurer

Sara Frattini

David Smith Thomson

The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, pharmaceutical compositions containing the same, processes for preparing the same, and methods of medical treatment using the same.

(4-((3R,4R)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone citrate

The present invention encompasses compounds of formula (1) wherein the groups Rto R, A and p have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors

(4-((3R,4R)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p- tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone citrate

The present invention relates to difluoromethyl-phenyl triazoles of general formula (I) which are modulators of GABAreceptors containing the &#x3b1;5 subunit, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

Difluoromethyl-phenyl triazoles

(4-((3R,4R)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-y1)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-citrate

The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.

Fumaric acid salt of 9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one, its use as a medicament and the preparation thereof

Disclosed is a method for the synthesis of spiro[2.5]octane-5,7-dione useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed are novel intermediates used in the synthesis of this compound.

Process for preparing spiro[2.5]octane-5,7-dione

The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.

Stereoselective synthesis of bicyclic heterocycles

9-[4-(3-chloro-2-fluoro-phenylamino-7-methoxy-quinazoline-6-yloxy]-1,4-diaza-spiro[5.5]undecane-5-one dimaleate, use thereof as a medicament and method for the production thereof

9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazoline-6-yloxy]-1,4-diaza-spiro[5.5] undecane-5-one dimaleate, use thereof as a medicament and method for the production thereof

The present invention encompasses a process for preparing compounds of formula (1), wherein a compound of formula (2) is reacted in the presence of a catalyst and a solvent under hydrogen pressure to form a compound of formula (1) and wherein A and R&#x2014;Rare defined herein.

Method of preparing chiral cyclic &#x3b2;-aminocarboxamides

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Therapeutic uses of compounds which selectively modulate the CB2 receptor

The present invention relates to a process for the stereoselective preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.

Process for the stereoselective preparation of bicyclic heterocycles

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Biberach an der Riss, Germany

Markus Ostermeier