Bayer Pharma Aktiengesellschaft

Bayer Aktiengesellschaft

Ph Pharma Co., Ltd.

Philipp Rubenbauer

Heiko Schirmer

Britta Olenik

Kai Lovis

Julia Küsel

Peter Serno

Birgit Keil

Donald Bierer

Danja Grossbach

Tia Jacobs

Reinerus Gerardus Gieling

Anke Stroyer

Carmen Lobback

Johannes Platzek

Peter Fey

Felix Spindler

Franz-Josef Mais

Hans-Christian Militzer

Chantal Fürstner

Andreas Lender

Thomas Neubauer

Stefan Nikolaus Gradl

Kersten Matthias Gericke

Jorma Hassfeld

Juergen Stiehl

Maurus Marty

Marie-Pierre Collin-Kröpelin

Jan-Georg Peters

Hendricus Nicolaas Sebastiaan Van Der Haas

Sonja Elisabeth Hoogeveen

Jeroen Alexander Dekker

Matthijs Cornelis Maria Van Oers

Frank Süßmeier

Günter Weingärtner

Theodor Zweifel

Martin Seyfried

Danja Großbach

Daniel Götz

Henricus Nicolaas Sebastiaan Van Der Haas

Daniel Gotz

Gunter Weingartner

The present invention covers a method for preparing 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine (“the compound of formula (I)” in the following) as well as intermediate compounds useful in the preparation of the compound of formula (I). The present invention also covers polymorphic form B of the compound of formula (I) with very high purity.

Method for preparing 2-[(3R)-3-methylmorpholin-4-yl]-4-[1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine

The present invention provides methods for the preparation of Compound (I): Compound (I), the use of intermediates for the preparation of said compound and its crystalline form A. 

Method for the preparation of a 2,4,5-trisubstituted 1,2,4-triazolone

The present invention relates to orally administrable modified-release pharmaceutical dosage forms comprising sodium (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoate and to processes for preparing the dosage forms and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiac, renal and pulmonary disorders, disorders of the central nervous system, fibrotic and inflammatory disorders and metabolic disorders.

Orally administrable modified-release pharmaceutical dosage form

The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders.

Method for producing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4- chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclo-propylpropanoic acid and the crystalline form thereof for use as a pharmaceutical  ingredient

The present application relates to a novel and improved process for preparing 5-(hydroxyalkyl)-1-phenyl-1,2,4-triazole derivatives of the formula (I) 

Method for producing 5-hydroxyalkyl-substituted 1-phenyl-1,2,4-triazole derivatives

The invention relates to a new and improved method for preparation of (4S)-4-[4-cyano-2-(methyl sulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I), as well as the preparation and use of the crystal form (A) of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I).

Method for producing (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile

The present invention relates to a novel method of preparing copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride. The present invention also relates to copanlisib dihydrochloride hydrates as compounds.

Synthesis of copanlisib and its dihydrochloride salt

The present invention concerns a new and improved method for preparation of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluormethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I), as well as the preparation and use of the crystal form (A) of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluormethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I).

Method for producing (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrohydro pyrimidine-5-carbonitrile

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Bensheim, Germany

Philipp Rubenbauer