Actelion Pharmaceuticals Ltd

Xavier Leroy

Sylvaine Cren

Daniel Bur

Sylvia Richard-Bildstein

Olivier Corminboeuf

Corinna Grisostomi

Davide Pozzi

Heinz Fretz

Julien Pothier

Oliver Corminboeuf

The present invention relates to benzimidazolyl-methyl urea derivatives of formula (I), wherein n, D, E, R, R, R, R, R, R, Rand Rare as defined in the description, their preparation and their use as pharmaceutically active compounds.

Benzimidazolyl-methyl urea derivatives as ALX receptor agonists

The invention relates to hydroxylated aminotriazole derivatives of formula (I), wherein Q, R, R, Rand Rare as defined in the description, their preparation and their use as pharmaceutically active compounds.

Hydroxylated aminotriazole derivatives as ALX receptor agonists

The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.

Bridged Spiro[2.4]heptane ester derivatives

The invention relates to the identification of Neuropeptide Q as ligand of the GALR2 GPCR (G-protein coupled receptor). The invention encompasses the use of the interaction of GALR2 polypeptides and Neuropeptide Q polypeptides as the basis of screening assays for agents that modulate the activity of the GALR2 receptor. The invention also encompasses diagnostic assays based upon the GALR2/Neuropeptide Q polypeptide interaction, as well as kits for performing diagnostic and screening assays.

Neuropeptide Q as modulator of GPCR GALR2 and uses thereof

The invention relates to oxazolyl-methylether derivatives of formula (I), wherein R, R, R, Rand Rare as defined in the description, their preparation and their use as pharmaceutically active compounds.

Oxazolyl-methylether derivatives as ALX receptor agonists

The invention relates to the identification of Humanin and derivatives thereof as ligands of the GPR1 GPCR (G-protein coupled receptor). The invention encompasses the use of the interaction of GPR1 polypeptides and Humanin polypeptides as the basis of screening assays for agents that modulate the activity of the GPR1 receptor. The invention also encompasses diagnostic assays based upon the GPR1/Humanin polypeptide interaction, as well as kits for performing diagnostic and screening assays.

Method for identifying modulators of GPCR GPR1 function

The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, Rand Rare as defined in the description, their preparation and their use as pharmaceutically active compounds. 

Oxazole and thiazole derivatives as ALX receptor agonists

The invention relates to fluorinated aminotriazole derivatives of formula (I), wherein A, Rand Rare as defined in the description, their preparation and their use as pharmaceutically active compounds. 

Fluorinated aminotriazole derivatives

The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, Rand Rare as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases. 

Bridged spiro [2.4] heptane derivatives as ALX receptor and/or FPRL2 agonists

The invention relates to aminotriazole derivatives of formula (I), wherein A, E, Rand Rare as defined in the description, their preparation and their use as pharmaceutically active compounds.

Aminotriazole derivatives as ALX agonists

The invention relates to aminopyrazole derivatives of formula (I), wherein A, E, Rand Rare as defined in the description, their preparation and their use as pharmaceutically active compounds.

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Allschwil, Switzerland

Xavier Leroy