Bayer Aktiengesellschaft

Bayer Pharma Aktiengesellschaft

Adverio Pharma Gmbh

Michal Sowa

Peter Fey

Britta Olenik

Werner Hoheisel

Daniel Gallenkamp

Markus Longerich

Julian Egger

Clemens Bothe

Guido Becker

Dirk Havekost

Anja Ehrig

Heike Neumann

Adrian Dobrowolski

Daniel Götz

Daniel Goetz

Elisabeth Kersten

Joerg Brockob

Eva Esser

Giovanni Maria Maggioni

Christoph Nueboldt

Ute Elias

Michael Ostendorf

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

Growing community of inventors

Wuppertal, Germany

Michal Sowa