Idorsia Pharmaceuticals Ltd

Novartis Ag

Isabelle Lyothier

Sylvia Richard-Bildstein

Olivier Corminboeuf

Heinz Fretz

Davide Pozzi

Thierry Sifferlen

Christoph Boss

Hervé Siendt

Julien Pothier

Lorenza Wyder Peters

Peter Herold

Robert Mah

Stefan Stutz

Aleksandar Stojanovic

Dirk Behnke

Herv Siendt

The present invention relates to derivatives of formula (I) wherein (R), R, R, R, R, R, Rand Arare as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

N-substituted indole derivatives as PGE2 receptor modulators

The present invention relates to pyrimidine derivatives of formula (I) wherein (R), R, R, R, R, Rand Arare as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (II) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

Pyrimidine derivatives as PGE2 receptor modulators

The present invention relates to phenyl derivatives of formula (I)

Phenyl derivatives as PGE2 receptor modulators

The present invention relates to pyrimidine derivatives of formula (I) wherein (R), R, R, R, R, Rand Arare as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (III) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

Pyrimidine derivatives

The present invention relates to benzofurane and benzothiophene derivatives of formula (I) wherein (R), R, R, R, R, R, Rand Arare as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (II) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

Benzofurane and benzothiophene derivatives as PGE2 receptor modulators

Process for preparing a compound of the formula (I) in which Rand Rare each independently H, C-C-alkyl, halogen, polyhalo-C-C-alkoxy, polyhalo-C-C-alkyl, C-C-alkoxy, C-C-alkoxy-C-C-alkyl, or C-C-alkoxy-C-C-alkoxy, where Rand Rare not both H, and Ris C-C-alkyl, which is characterized in that a) a compound of the formula (II) in which Rand Rare each as defined above and X is Br, I, triflate, toyslate or mesylate is reacted with prop-2-yn-1-ol to give the compound of the formula (III), b) the compound of the formula (III) is reacted with an alkyl-metal compound in which 'alkyl' is as defined above for Rto give a compound of the formula (I). 

Process for preparing organic compounds

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Allschwil, Switzerland

Isabelle Lyothier