Cilag International Gmbh

Ethicon, Gmbh

Janssen Pharmaceutica Nv

Michael Justus

Karl Reuter

Benjamin D Fitz

Adrian Maurer

Christopher M Westergom

Tobias Wedel

Rainer Heck

Oliver Floegel

Roland Müller

Tobias Strittmatter

Thomas Otten

Martin Rettig

Rolf Hänseler

Cheng Yi Chen

The present invention is directed to processes for the preparation of esketamine. The present invention is further directed to processes for the resolution of S-ketamine from a racemic or enantiomerically enriched mixture of ketamine. The present invention is further directed to an (S)-CSA salt of S-ketamine, more particularly a monohydrate form of the (S)-CSA salt of S-ketamine; and to an (R)-CSA salt of R-ketamine.

(S)-CSA salt of S-ketamine, (R)-CSA salt of S-ketamine and processes for the preparation of S-ketamine

Method for preparing (S)(+)phenyl acetic acid derivatives having the general formula (I): wherein Ris a linear or branched alkyl group with 1-6 carbon atoms or substituted benzyl group, and Ris methyl, ethyl or propyl group said method, characterised in that a compound of the general formula (II): wherein Ris as given above, and Ris a nucleofuge, or a suitable salt of a compound of the general formula (II) is reacted with a compound having the general formula (III): wherein Ris as given above, and Ris hydrogen or a nucleofuge that can be removed hydrolytically, and the protective group Rthat may be present, may be subsequently removed hydrolytically.

Method for preparing phenyl acetic acid derivatives

A novel macromer or mixture thereof is described herein, comprising benzoyl isocyanate terminal moieties and at least two residues of a water-soluble polymer having a molecular weight ranging from 80 to 10,000 adjacent to the carbonyl group of the benzoyl isocyanate moieties, thereby forming at least two ester linkages in the macromer or mixture thereof. A method for making a diisocyanate macromer is also described herein.

Method of making a diisocyanate terminated macromer

The present invention refers to a method for making iron(III)gluconate complex, preferably alkali iron(III)gluconate complex. The method includes the following steps: (i) mixing a water soluble iron(III)salt in aqueous solution, simultaneously or in any desired sequence, with a member selected from gluconic acid, a water soluble salt of gluconic acid and combinations thereof, and a member selected from an alkali hydroxide, an alkali carbonate, an alkali hydrogen carbonate and combinations thereof, so that the reaction mixture has an acid value (pH-value) within the range of from 7.0 to 12, provided that when alkali hydroxide is used, gluconic acid or a water soluble salt of gluconic acid is provided at the beginning of the reaction or is added to the reaction mixture simultaneously with the alkali hydroxide; (ii) heating the reaction mixture until the iron(III)gluconate complex has formed; and (iii) adding an organic solvent which is miscible with water until the iron(III)gluconate complex is precipitated. The present invention also refers to pharmaceutical compositions including the iron(III)gluconate complex and methods of treating anemic conditions.

Method of making iron(III)gluconate complex

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Schaffhausen, Switzerland

Michael Justus