Janssen Pharmaceutica Nv

Joannes Josephus Maria Willems

Bart Petrus Anna Maria Jozef Medaer

Jan Heeres

Jérôme Emile Georges Guillemont

Paul Adriaan Jan Janssen

Elisabeth Therese Jeanne Pasquier

Ruben Gerardus George Leenders

Didier Philippe Robert Schils

Johan Erwin Edmond Weerts

Sigrid Carl Maria Stokbroekx

Yves Georges Ruysschaert

Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: in the presence of a suitable solvent; with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent;

Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile

Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise:  

Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-2pyrimidinyl]amino]benzonitrile

The object of the present invention is a novel mandelate salt of a substituted tetracyclic tetrahydrofuran derivative according to Formula (I) the N-oxide forms and the stereochemically isomeric forms thereof, wherein Rand Reach independently are hydrogen or Calkyl and Rand Reach independently are hydrogen or halogen. In the foregoing definitions Calkyl defines straight and branched saturated hydrocarbon radicals having from 1 to 6 carbon atoms such as, for example, methyl, ethyl, propyl, butyl, 1-methylpropyl, 1,1-dimethylethyl, pentyl or hexyl. The novel mandelate salt is not light-sensitive and is far more stable than the prior art salts at room temperature, enhanced temperature and at relative high humidities and in aqueous media. Also disclosed are pharmaceutical compositions comprising mandelate salts according to the invention, mandelate salts according to the invention for use as a medicine, a process for preparing the mandelate salts according to the invention and the use of the mandelate salts and pharmaceutical compositions comprising mandelate salts according to the invention for the treatment or the prevention of CNS disorders, cardiovascular disorders and gastrointestinal disorders.

Mandelates salts of substituted tetracyclic tetrahydrofuran derivatives

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Oud-Turnhout, Belgium

Joannes Josephus Maria Willems