Bayer Aktiengesellschaft

Bayer Pharma Aktiengesellschaft

Adverio Pharma Gmbh

Michal Sowa

Peter Fey

Britta Olenik

Werner Hoheisel

Daniel Gallenkamp

Julian Egger

Clemens Bothe

Guido Becker

Markus Longerich

Anja Ehrig

Dirk Havekost

Adrian Dobrowolski

Heike Neumann

Elisabeth Kersten

Daniel Götz

Joerg Brockob

Eva Esser

Giovanni Maria Maggioni

Michael Ostendorf

Christoph Nueboldt

Edith Beckmann

Daniel Goetz

Ute Elias

Valentina Paula Conty

What is described herein relates to a method for generating micro-particles comprising the steps of

Nano-seeding

The present invention relates to methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate in the form of a novel active compound product having improved properties, for example in respect of the isolability of the active compound product, the dischargeability of the active compound product after isolation and drying and also conveyability, sieveability and micronizability of the active compound product, and to processes for the production and formulation thereof.

Methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate active compound product having improved properties, production and formulation thereof

The present invention relates to a process for preparing 4-{[(2S)-2-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl}butanoyl]amino}-2-fluorobenzamide (I) or 4-({(2S)-2-[4-{5-chloro-2-[4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl]phenyl}-5-methoxy-2-oxopyridin-1(2H)-yl]butanoyl}amino)-2-fluorobenzamide (II) from 2,5-dimethoxypyridine (III), 1-(2-bromo-4-chlorophenyl)-4-chloro-1H-1,2,3-triazole (X-Cl) or 1-(2-bromo-4-chlorophenyl)-4-(trifluoromethyl)-1H-1,2,3-triazole (X-CF), 4-amino-2-fluorbenzamide (XIII) and (2R)-2-aminobutanoic acid (XVII).

Preparative process

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Wuppertal, Germany

Michal Sowa