Merck Patent Gmbh

Poxel

David Maillard

Clemens Kuehn

Michael Lange

Edoardo Burini

Andreas Waechtler

Christian Jasper

Thomas Fuchss

Marco Poma

Ewgenij Wakaresko

Detlef Pauluth

Werner Mederski

Andreas Taugerbeck

Hanns Wurziger

Axel Jansen

Stefan Lehmann

Marcel Breuning

Tobias Schlueter

Guntram Koller

Sebastian Haertner

Marc Dittmann

Serge Gerbaut

Renaud Poli

Camille Correia

Sabine Gottburg-Reininger

Jeremy Maurin

Joern Kolb

Hadia Saleh-Kassim

Luc Eberhardt

Marcel Breuníng

Beate Kretschmer

Markus Kriegbaum

Ralf Schäfer

Andreas Wächtler

Philipp Krattinger

A solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methy}-4-fluoro-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, is useful as a BTK inhibitor.

Crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, salt forms thereof, and processes to obtain

The present invention relates to an improved process for the preparation of metformin hydrochloride, an important drug in the first line treatment of Type II Diabetes.

Process for the preparation of metformin

A crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be prepared as a pharmaceutical composition.

Crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol

An anhydrous disordered crystalline (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be used in pharmaceutical compositions.

Solid form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol

The present invention provides methods of preparing Praziquantel, in particular (R)-Praziquantel and analogues thereof in a stereoselective manner. One method involves asymmetric hydrogenation of the following intermediate compound and subsequent cyclization.

Method for the production of praziquantel and precursors thereof

The present invention relates to a method for the racemization of enantiomerically pure or enantiomerically enriched Praziquantel under basic conditions and a method for the production of (R)-Praziquantel in enantiopure or enantiomerically enriched form, which comprises the racemization method.

Method for the production of praziquantel

The present invention relates to methods for the production of enantiopure or enantioenriched Praziquantel precursors and to methods for the production of enantiopure or enantioenriched Praziquantel comprising the methods for the production of the Praziquantel precursors. The present invention further relates to compounds or intermediates useful in such methods.

Method for the production of Praziquantel and precursors thereof

The present invention discloses a process for isolating enantiomer components from a mixture of enantiomers through particle-size-controlled crystallization, comprising the steps of: (a) forming a solution of a mixture of enantiomers (R) and (S) in a solvent in the absence of any further additives or agents; (b) seeding the solution of step (a) simultaneously or consecutively with seed crystals of enantiomer (R) and with seed crystals of enantiomer (S), wherein the seed crystals of enantiomer (R) differ in size and/or in quantity from the seed crystals of enantiomer (S) to allow separation of the crystals composed of a mixture enriched with enantiomer (R) from the crystals composed of a mixture enriched with enantiomer (S); (c) inducing simultaneous crystallization of enantiomer (R) and enantiomer (S); and (d) isolating crystals composed of a mixture enriched with enantiomer (R) from crystals composed of a mixture enriched with enantiomer (S) through size separation of the crystals, preferably through sieving, melting or sedimentation, in particular through sieving.

Process of isolating enantiomer components from enantiomer mixtures by particle-size-controlled crystallization

The invention relates to compounds of the formula (I), in which R, R, R, R, Y and A have the meanings indicated, and to processes for the preparation thereof and to the use thereof for the preparation of medicaments. 

Oxaphenanthrene derivatives

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Darmstadt, Germany

David Maillard