Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Svenja Renner

Thomas Wirth

Carsten Reichel

Joern Merten

Dirk Weber

Thomas Fachinger

Simone Orlich

Tobias Fiedler

Rolf Schmid

Juergen Schnaubelt

Rainer Hamm

Burkhard Jaeger

Juergen Schroeder

Georg Dziewas

Christian Filser

Matthias Post

Guenter Linz

Werner Rall

Xiao-Jun Wang

Thomas Krueger

Michael Konrad

Emanuel Stehle

Cartsen Reichel

Xiao-Jung Wang

Bianca Werner

Robert Schiffers

The present invention relates to processes for preparing a glucopyranosyl-substituted benzyl-benzene derivative of general formula III, wherein Ris defined according to claim

Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives

The invention relates to a method for the preparation for a crystalline form of 1-chloro-4-(&#x3b2;-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene. In addition the invention relates to a crystalline form obtainable by this method, to a pharmaceutical composition and to the use thereof for preparing medicaments.

Method for the preparation of a crystalline form

The present invention relates to a process for the manufacture of a specific indolinone derivative and a pharmaceutically acceptable salt thereof, namely 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone and its monoethanesulfonate, to new manufacturing steps and to new intermediates of this process.

Process for the manufacture of an indolinone derivative

A process for preparing compounds of the formula (I) in which Rand Rare as defined in the description.

Preparation process

The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups R, R, Rand Rhave the meanings given in the claims, as well as sulphonyl derivatives of formula and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.

Process for preparing aminocrotonylamino-substituted quinazoline derivatives

The present invention relates to specific indolinone derivatives, namely the compounds of formula, in which Rrepresents an hydrogen atom or a group, and Rand Reach represent an hydrogen atom or Rand Rtaken together represent a group, with the proviso that when Rrepresents an hydrogen atom Rand Rtaken together represent a group, and to a process for their manufacture. 

Indolinone derivatives and process for their manufacture

The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups R, R, Rand Rhave the meanings given in the claims, as well as sulphonyl derivatives of formula (XIII) and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases. 

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Eckenroth, Germany

Svenja Renner